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Opton
Esomeprazole
Opton
Esomeprazole
Indication detailsView
Esomeprazole is indicated:
- To relieve from chronic heartburn symptoms and other symptoms associated with GERD
- For the healing of erosive esophagitis
- For maintenance of healing of erosive esophagitis
- In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
- Zollinger-Ellison Syndrome
- Acid related Dyspepsia
- Duodenal & Gastric ulcer
PharmacologyView
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
DosageView
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don't heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.
Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.
AdministrationView
Esomeprazole tablet or capsule: should be swallowed whole and taken one hour before a meal.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Side effectsView
The most frequently occurring adverse events reported with Esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.
ContraindicationsView
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.
PrecautionsView
General: Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
InteractionsView
Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Esomeprazole does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.
Pediatric usageView
Paediatric Use: Safety and effectiveness in paediatric patients have not been established.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Overdose effectsView
A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Esomeprazole. No specific antidote for Esomeprazole is known. Since Esomeprazole is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.
ReconstitutionView
Infusion: Reconstitute one sterile single-dose vial of Esomeprazole IV Injection with 5 ml of the solvent (WFI) provided and further diluting the resulting solution within 0.9% Sodium Chloride solution or 5% Dextrose solution to make a final volume of 50 ml. The resultant infusion should be given intravenously over a period of 10-30 minutes. Chemical and physical in-use stability has been demonstrated for 12 hours after reconstitution with 0.9% Sodium Chloride solution or for 6 hours after reconstitution with 5% Dextrose solution. From a microbial point of view, the product should be used immediately. Any unused portion should be discarded.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.
Opton
Esomeprazole
Opton
Esomeprazole
Indication detailsView
Esomeprazole is indicated:
- To relieve from chronic heartburn symptoms and other symptoms associated with GERD
- For the healing of erosive esophagitis
- For maintenance of healing of erosive esophagitis
- In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
- Zollinger-Ellison Syndrome
- Acid related Dyspepsia
- Duodenal & Gastric ulcer
PharmacologyView
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
DosageView
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don't heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.
Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.
AdministrationView
Esomeprazole tablet or capsule: should be swallowed whole and taken one hour before a meal.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Side effectsView
The most frequently occurring adverse events reported with Esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.
ContraindicationsView
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.
PrecautionsView
General: Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
InteractionsView
Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Esomeprazole does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.
Pediatric usageView
Paediatric Use: Safety and effectiveness in paediatric patients have not been established.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Overdose effectsView
A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Esomeprazole. No specific antidote for Esomeprazole is known. Since Esomeprazole is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.
ReconstitutionView
Infusion: Reconstitute one sterile single-dose vial of Esomeprazole IV Injection with 5 ml of the solvent (WFI) provided and further diluting the resulting solution within 0.9% Sodium Chloride solution or 5% Dextrose solution to make a final volume of 50 ml. The resultant infusion should be given intravenously over a period of 10-30 minutes. Chemical and physical in-use stability has been demonstrated for 12 hours after reconstitution with 0.9% Sodium Chloride solution or for 6 hours after reconstitution with 5% Dextrose solution. From a microbial point of view, the product should be used immediately. Any unused portion should be discarded.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.
Opton
Esomeprazole
Opton
Esomeprazole
Indication detailsView
Esomeprazole is indicated:
- To relieve from chronic heartburn symptoms and other symptoms associated with GERD
- For the healing of erosive esophagitis
- For maintenance of healing of erosive esophagitis
- In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
- Zollinger-Ellison Syndrome
- Acid related Dyspepsia
- Duodenal & Gastric ulcer
PharmacologyView
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
DosageView
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don't heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.
Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.
AdministrationView
Esomeprazole tablet or capsule: should be swallowed whole and taken one hour before a meal.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Side effectsView
The most frequently occurring adverse events reported with Esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.
ContraindicationsView
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.
PrecautionsView
General: Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
InteractionsView
Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Esomeprazole does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.
Pediatric usageView
Paediatric Use: Safety and effectiveness in paediatric patients have not been established.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Overdose effectsView
A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Esomeprazole. No specific antidote for Esomeprazole is known. Since Esomeprazole is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.
ReconstitutionView
Infusion: Reconstitute one sterile single-dose vial of Esomeprazole IV Injection with 5 ml of the solvent (WFI) provided and further diluting the resulting solution within 0.9% Sodium Chloride solution or 5% Dextrose solution to make a final volume of 50 ml. The resultant infusion should be given intravenously over a period of 10-30 minutes. Chemical and physical in-use stability has been demonstrated for 12 hours after reconstitution with 0.9% Sodium Chloride solution or for 6 hours after reconstitution with 5% Dextrose solution. From a microbial point of view, the product should be used immediately. Any unused portion should be discarded.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.
Opzin
Cetirizine Hydrochloride
Opzin
Cetirizine Hydrochloride
Indications
Urticaria
Indication detailsView
It is indicated for the relief of symptoms associated with seasonal & perennial allergic rhinitis. It is also indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria and allergen induced asthma.
Therapeutic classView
Sedating Anti-histamine
PharmacologyView
Cetirizine Hydrochloride is a potent H1 receptor antagonist without any significant anticholinergic and antiserotonic effects. At pharmacologically active dose levels, it has almost no drowsiness effect and does not cause behavioral changes. It inhibits the histamine-mediated early phase of the allergic reaction and also reduces the migration of inflammatory cells and the release of mediators associated with the late phase of the allergic reaction.
Pharmacokinetics: Cetirizine 10 mg achieves peak plasma concentrations of 257 mcg/L within one hour of administration (980 mcg/L in children). Food does not affect the extent of absorption, but it may slightly reduce the rate. Peak blood levels 0.3 micrograms/ml are reached between thirty & sixty minutes after administration of 10 mg dose of Cetirizine. Its plasma half-life is approximately 11 hours. Absorption is very consistent from one subject to the next. Its renal clearance is 30 ml/minute and the excretion half-life is approximately nine hours.
Pharmacokinetics: Cetirizine 10 mg achieves peak plasma concentrations of 257 mcg/L within one hour of administration (980 mcg/L in children). Food does not affect the extent of absorption, but it may slightly reduce the rate. Peak blood levels 0.3 micrograms/ml are reached between thirty & sixty minutes after administration of 10 mg dose of Cetirizine. Its plasma half-life is approximately 11 hours. Absorption is very consistent from one subject to the next. Its renal clearance is 30 ml/minute and the excretion half-life is approximately nine hours.
DosageView
Adults and Children 6 years and older: 1 tablet or 2 teaspoonfuls daily (or 1 teaspoonful twice daily).
Children 2-6 years: 1 teaspoonful once daily or 1/2 teaspoonful twice daily.
Children 6 months to 2 years : 1/2 teaspoonful once daily. The dose in children 12-23 months of age can be increased to a maximum dose as 1/2 teaspoonful every 12 hours.
Children 2-6 years: 1 teaspoonful once daily or 1/2 teaspoonful twice daily.
Children 6 months to 2 years : 1/2 teaspoonful once daily. The dose in children 12-23 months of age can be increased to a maximum dose as 1/2 teaspoonful every 12 hours.
Side effectsView
The most common side effects that occurred more frequently on Cetirizine is somnolence.
ContraindicationsView
It is contraindicated in patients with a history of hypersensitivity to Cetirizine or hydroxyzine.
PrecautionsView
Caution should be exercised when driving a car or operating a heavy machinery.
InteractionsView
No clinically significant drug interactions have been found with Theophylline, Azithromycin, Pseudoephedrine, Ketoconazole or Erythromycin and with other drugs.
Pregnancy & lactationView
US FDA Pregnancy Category of Cetirizine Hydrochloride is B. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Cetirizine Hydrochloride has been shown to be excreted in human milk. So, caution should be exercised when Cetirizine Hydrochloride is administered to a nursing woman.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.
Opzin
Cetirizine Hydrochloride
Opzin
Cetirizine Hydrochloride
Indications
Urticaria
Indication detailsView
It is indicated for the relief of symptoms associated with seasonal & perennial allergic rhinitis. It is also indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria and allergen induced asthma.
Therapeutic classView
Sedating Anti-histamine
PharmacologyView
Cetirizine Hydrochloride is a potent H1 receptor antagonist without any significant anticholinergic and antiserotonic effects. At pharmacologically active dose levels, it has almost no drowsiness effect and does not cause behavioral changes. It inhibits the histamine-mediated early phase of the allergic reaction and also reduces the migration of inflammatory cells and the release of mediators associated with the late phase of the allergic reaction.
Pharmacokinetics: Cetirizine 10 mg achieves peak plasma concentrations of 257 mcg/L within one hour of administration (980 mcg/L in children). Food does not affect the extent of absorption, but it may slightly reduce the rate. Peak blood levels 0.3 micrograms/ml are reached between thirty & sixty minutes after administration of 10 mg dose of Cetirizine. Its plasma half-life is approximately 11 hours. Absorption is very consistent from one subject to the next. Its renal clearance is 30 ml/minute and the excretion half-life is approximately nine hours.
Pharmacokinetics: Cetirizine 10 mg achieves peak plasma concentrations of 257 mcg/L within one hour of administration (980 mcg/L in children). Food does not affect the extent of absorption, but it may slightly reduce the rate. Peak blood levels 0.3 micrograms/ml are reached between thirty & sixty minutes after administration of 10 mg dose of Cetirizine. Its plasma half-life is approximately 11 hours. Absorption is very consistent from one subject to the next. Its renal clearance is 30 ml/minute and the excretion half-life is approximately nine hours.
DosageView
Adults and Children 6 years and older: 1 tablet or 2 teaspoonfuls daily (or 1 teaspoonful twice daily).
Children 2-6 years: 1 teaspoonful once daily or 1/2 teaspoonful twice daily.
Children 6 months to 2 years : 1/2 teaspoonful once daily. The dose in children 12-23 months of age can be increased to a maximum dose as 1/2 teaspoonful every 12 hours.
Children 2-6 years: 1 teaspoonful once daily or 1/2 teaspoonful twice daily.
Children 6 months to 2 years : 1/2 teaspoonful once daily. The dose in children 12-23 months of age can be increased to a maximum dose as 1/2 teaspoonful every 12 hours.
Side effectsView
The most common side effects that occurred more frequently on Cetirizine is somnolence.
ContraindicationsView
It is contraindicated in patients with a history of hypersensitivity to Cetirizine or hydroxyzine.
PrecautionsView
Caution should be exercised when driving a car or operating a heavy machinery.
InteractionsView
No clinically significant drug interactions have been found with Theophylline, Azithromycin, Pseudoephedrine, Ketoconazole or Erythromycin and with other drugs.
Pregnancy & lactationView
US FDA Pregnancy Category of Cetirizine Hydrochloride is B. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Cetirizine Hydrochloride has been shown to be excreted in human milk. So, caution should be exercised when Cetirizine Hydrochloride is administered to a nursing woman.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.
Or-C
Vitamin C [Ascorbic acid]
Or-C
Vitamin C [Ascorbic acid]
Indications
Vitamin C deficiency
Indication detailsView
Vitamin C is indicated for prevention and treatment of scurvy. It may be indicated in pregnancy, lactation, infection, trauma, burns, cold exposure, following surgery, fever, stress, peptic ulcer, cancer, methaemoglobinaemia and in infants receiving unfortified formulas. It is also prescribed for haematuria, dental caries, pyorrhea, acne, infertility, atherosclerosis, fractures, leg ulcers, hay fever, vascular thrombosis prevention, levodopa toxicity, succinyl-choline toxicity, arsenic toxicity etc. To reduce the risk of stroke in the elderly, long-term supplementation with Vitamin C is essential.
Therapeutic classView
Vitamin-C Preparations
PharmacologyView
vitamin C, the water-soluble vitamin, is readily absorbed from the gastrointestinal tract and is widely distributed in the body tissues. It is believed to be involved in biological oxidations and reductions used in cellular respiration. It is essential for the synthesis of collagen and intracellular material. Vitamin C deficiency develops when the dietary intake is inadequate and when increased demand is not fulfilled. Deficiency leads to the development of well defined syndrome known as scurvy, which is characterized by capillary fragility, bleeding (especially from small blood vessels and the gums), anaemia, cartilage and bone lesions and slow healing of wounds.
DosageView
Oral administration-
- For the prevention of scurvy: 1 tablet daily
- For the treatment of scurvy: 1-2 tablets daily; but dose may be increased depending on the severity of the condition.
- For the reduction of risk of stroke in the elderly: 1-2 tablets daily.
- In other cases: 1 tablet daily or as directed by the physician.
- Maximum safe dose is 2000 mg daily in divided doses.
- Vitamin C is usually administered orally. When oral administration is not feasible or when malabsorption is suspected, the drug may be administered IM, IV, or subcutaneously. When given parenterally, utilization of the vitamin reportedly is best after IM administration and that is the preferred parenteral route.
- For intravenous injection, dilution into a large volume parenteral such as Normal Saline, Water for Injection, or Glucose is recommended to minimize the adverse reactions associated with intravenous injection.
- The average protective dose of vitamin C for adults is 70 to 150 mg daily. In the presence of scurvy, doses of 300 mg to 1 g daily are recommended. However, as much as 6 g has been administered parenterally to normal adults without evidence of toxicity.
- To enhance wound healing, doses of 300 to 500 mg daily for a week or ten days both preoperatively and postoperatively are generally considered adequate, although considerably larger amounts have been recommended. In the treatment of burns, doses are governed by the extent of tissue injury. For severe burns, daily doses of 1 to 2 g are recommended. In other conditions in which the need for vitamin C is increased, three to five times the daily optimum allowances appear to be adequate.
- Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever the solution and container permit.
Side effectsView
Vitamin C has little toxicity and only mega-doses of vitamin C may cause diarrhoea, abdominal bloating, iron over-absorption that is harmful in patients with thalassaemia, sideroblastic anemia, and haemochromatosis; hyperoxaluria, hyperuricosuria, and hemolysis in patients with glucose-6 phosphate dehydrogenase deficiency. A pregnant woman taking more than 5 gm/day may suffer fetal abortion.
PrecautionsView
Ingestion of megadose (more than 1000 mg daily) of vitamin C during pregnancy has resulted in scurvy in neonates. Vitamin C in mega-doses has been contraindicated for patients with hyperoxaluria. Vitamin C itself is a reactive substance in the redox system and can give rise to false positive reactions in certain analytical tests for glucose, uric acid, creatine and occult blood.
InteractionsView
Potentially hazardous interactions: Ascorbic acid is incompatible in solution with aminophylline, bleomycin, erythromycin, lactobionate, nafcillin, nitrofurantoin sodium, conjugated oestrogen, sodium bicarbonate, sulphafurazole diethanolamine, chloramphenicol sodium succinate, chlorthiazide sodium and hydrocortisone sodium succinate.
Useful interactions: Ascorbic acid increases the apparent half-life of paracetamol and enhances iron absorption from the gastrointestinal tract.
Useful interactions: Ascorbic acid increases the apparent half-life of paracetamol and enhances iron absorption from the gastrointestinal tract.
Pregnancy & lactationView
The drug is safe in normal doses in pregnant women, but a daily intake of 5 gm or more is reported to have caused abortion. The drug may be taken safely during lactation.
StorageView
Should be stored in a dry place below 30˚C.
Ora K
Phenoxymethyl Penicillin [Penicillin V]
Ora K
Phenoxymethyl Penicillin [Penicillin V]
Indications
Vincent’s infection
Indication detailsView
For the treatment of mild to moderately severe bacterial infections, if these are due to penicillin susceptible pathogens and respond to therapy with oral penicillin, such as:
- infections of the ear, nose and throat regions, e.g., tonsillitis, pharyngitis, laryngitis, otitis media, sinusitis.
- infections of the lower respiratory tract, e.g., bronchitis and pneumonia, bronchopneumonia.
- infections due to beta-hemolytic streptococci of group A, e.g., scarlet fever, erysipelas, rheumatic fever.
- skin infections, e.g., pyodermia, furunculosis, phlegmon, erysipeloid, erythema migrans, insofar as the micro-organisms are penicillin-susceptible.
- lymphadenitis and lymphangitis of bacterial origin.
- infections of the buccal cavity, gums or jaws, e.g., inflammatory infiltrates, delayed dentition stages II and III, antral fistulae, secondary bacterial infection with Gram-positive pathogens following virus-induced gingivitis or stomatitis.
Therapeutic classView
Benzylpenicillin & Phenoxymethyl penicillin
PharmacologyView
Phenoxymethyl penicillin or penicillin V is acid-stable and is absorbed from the upper part of the small intestine. Of different forms of Phenoxymethyl penicillin, the potassium salt of Phenoxymethyl penicillin is best absorbed. This may be given with meals but maximum absorption is achieved when drug is administered orally at least 1 hour before or 2 hours after the meal. Phenoxymethyl penicillin offers a very convenient means of treating Grampositive infections. Phenoxymethyl penicillin has the distinct advantage over penicillin G in resistance to inactivation by gastric acid.
DosageView
The dosage of Phenoxymethyl penicillin should be determined according to the sensitivity of the causative micro-organism and the severity of the infection, and adjusted to the clinical response of the patient.
Adults: 250-500 mg 6 hourly
Children (above 1 year):
Adults: 250-500 mg 6 hourly
Children (above 1 year):
- 125-250 mg 6 hourly
- 125 mg/5 ml powder for suspension: 1-2 teaspoonful (5-10 ml) 6 hourly
- 250 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly
- 62.5-125 mg 6 hourly.
- 125 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly, or as prescribed by the physician.
AdministrationView
Phenoxymethyl Penicillin is best taken on an empty stomach, preferably one hour before meals. The tablets are swallowed without chewing with sufficient amounts of liquid. Before each use of this syrup, the bottle has to be shaken vigorously.
Side effectsView
Occasionally, hypersensitivity reactions involving the skin (e.g. urticaria, morbilliform or scarlatiniform rashes, pruritus), eosinophilia or more serious allergic reactions, e.g. drug fever, vasculitis, serum sickness or interstitial nephritis, may develop. Anaphylactic or anaphylactoid reactions accompanied by, e.g- angioneurotic oedema, oedema of the larynx, bronchial spasm and shock may occur.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
ContraindicationsView
Phenoxymethyl Penicillin must not be administered in patients with hypersensitivity to penicillins or any of the excipients of this. Phenoxymethyl Penicillin must not be used to treat patients with severe gastrointestinal disorders accompanied by vomiting and diarrhea.
PrecautionsView
The possibility of cross-allergy between cephalosporins and penicillins must be considered. When treating patients with heart diseases or serious electrolyte disturbances of other origin, the potassium content of Phenoxymethyl Penicillin may have to be considered. Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
InteractionsView
Food: Concurrent intake of food leads to a reduction in the rate of absorption. Therefore, Phenoxymethyl penicillin is best taken on an empty stomach, preferably one hour before meals, in order to reach the highest possible rate of absorption.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Pregnancy & lactationView
Phenoxymethylpenicillin crosses the placenta. Given the appropriate indication, this may be used at any time throughout pregnancy. Phenoxymethylpenicillin passes into the breast milk in small amounts. This may be used during lactation; however, diarrhoea and yeast colonization of mucous membranes may occur in the infant.
Overdose effectsView
The toxicity of phenoxymethylpenicillin is low, and it has a broad therapeutic range. When a multiple therapeutic dose is taken orally once only, phenoxymethylpenicillin has no acute toxicity. There is a risk of encephalopathy in cases of administration of beta-lactam antibiotics, particularly in case of overdose or renal impairment. Special measures in the event of overdosage, other than discontinuation of the medication, are not required. Elimination of phenoxymethylpenicillin can be accomplished through haemodialysis.
StorageView
Store in a cool and dry place, protect from light.
Ora K
Phenoxymethyl Penicillin [Penicillin V]
Ora K
Phenoxymethyl Penicillin [Penicillin V]
Indications
Vincent’s infection
Indication detailsView
For the treatment of mild to moderately severe bacterial infections, if these are due to penicillin susceptible pathogens and respond to therapy with oral penicillin, such as:
- infections of the ear, nose and throat regions, e.g., tonsillitis, pharyngitis, laryngitis, otitis media, sinusitis.
- infections of the lower respiratory tract, e.g., bronchitis and pneumonia, bronchopneumonia.
- infections due to beta-hemolytic streptococci of group A, e.g., scarlet fever, erysipelas, rheumatic fever.
- skin infections, e.g., pyodermia, furunculosis, phlegmon, erysipeloid, erythema migrans, insofar as the micro-organisms are penicillin-susceptible.
- lymphadenitis and lymphangitis of bacterial origin.
- infections of the buccal cavity, gums or jaws, e.g., inflammatory infiltrates, delayed dentition stages II and III, antral fistulae, secondary bacterial infection with Gram-positive pathogens following virus-induced gingivitis or stomatitis.
Therapeutic classView
Benzylpenicillin & Phenoxymethyl penicillin
PharmacologyView
Phenoxymethyl penicillin or penicillin V is acid-stable and is absorbed from the upper part of the small intestine. Of different forms of Phenoxymethyl penicillin, the potassium salt of Phenoxymethyl penicillin is best absorbed. This may be given with meals but maximum absorption is achieved when drug is administered orally at least 1 hour before or 2 hours after the meal. Phenoxymethyl penicillin offers a very convenient means of treating Grampositive infections. Phenoxymethyl penicillin has the distinct advantage over penicillin G in resistance to inactivation by gastric acid.
DosageView
The dosage of Phenoxymethyl penicillin should be determined according to the sensitivity of the causative micro-organism and the severity of the infection, and adjusted to the clinical response of the patient.
Adults: 250-500 mg 6 hourly
Children (above 1 year):
Adults: 250-500 mg 6 hourly
Children (above 1 year):
- 125-250 mg 6 hourly
- 125 mg/5 ml powder for suspension: 1-2 teaspoonful (5-10 ml) 6 hourly
- 250 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly
- 62.5-125 mg 6 hourly.
- 125 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly, or as prescribed by the physician.
AdministrationView
Phenoxymethyl Penicillin is best taken on an empty stomach, preferably one hour before meals. The tablets are swallowed without chewing with sufficient amounts of liquid. Before each use of this syrup, the bottle has to be shaken vigorously.
Side effectsView
Occasionally, hypersensitivity reactions involving the skin (e.g. urticaria, morbilliform or scarlatiniform rashes, pruritus), eosinophilia or more serious allergic reactions, e.g. drug fever, vasculitis, serum sickness or interstitial nephritis, may develop. Anaphylactic or anaphylactoid reactions accompanied by, e.g- angioneurotic oedema, oedema of the larynx, bronchial spasm and shock may occur.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
ContraindicationsView
Phenoxymethyl Penicillin must not be administered in patients with hypersensitivity to penicillins or any of the excipients of this. Phenoxymethyl Penicillin must not be used to treat patients with severe gastrointestinal disorders accompanied by vomiting and diarrhea.
PrecautionsView
The possibility of cross-allergy between cephalosporins and penicillins must be considered. When treating patients with heart diseases or serious electrolyte disturbances of other origin, the potassium content of Phenoxymethyl Penicillin may have to be considered. Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
InteractionsView
Food: Concurrent intake of food leads to a reduction in the rate of absorption. Therefore, Phenoxymethyl penicillin is best taken on an empty stomach, preferably one hour before meals, in order to reach the highest possible rate of absorption.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Pregnancy & lactationView
Phenoxymethylpenicillin crosses the placenta. Given the appropriate indication, this may be used at any time throughout pregnancy. Phenoxymethylpenicillin passes into the breast milk in small amounts. This may be used during lactation; however, diarrhoea and yeast colonization of mucous membranes may occur in the infant.
Overdose effectsView
The toxicity of phenoxymethylpenicillin is low, and it has a broad therapeutic range. When a multiple therapeutic dose is taken orally once only, phenoxymethylpenicillin has no acute toxicity. There is a risk of encephalopathy in cases of administration of beta-lactam antibiotics, particularly in case of overdose or renal impairment. Special measures in the event of overdosage, other than discontinuation of the medication, are not required. Elimination of phenoxymethylpenicillin can be accomplished through haemodialysis.
StorageView
Store in a cool and dry place, protect from light.
Orabex
Vitamin B complex
Orabex
Vitamin B complex
Indications
Vitamin B deficiencies
Indication detailsView
Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi
Therapeutic classView
Specific combined vitamin preparations
PharmacologyView
Vitamin-B complex contains the most important members of the vitamin B group in pure form and in therapeutically balanced proportions. The members of the vitamin B group contained in Vitamin-B complex are components of enzyme systems that regulate various stages of carbohydrate, fat and protein metabolism, each of the components playing a specific biological role. Deficiency of B vitamin causes glossitis, stomatitis, cheilosis, polyneuritis, beriberi, pellagra and vascularisation of cornea.
DosageView
Tablet/ capsule: usual recommended dose is 1-2 tablet/capsule 3 times daily or as directed by the physician.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Side effectsView
Adverse reactions have been reported with specific vitamins and minerals, but generally at levels substantially higher than those in Vitamin-B complex. However, allergic and idiosyncratic reactions are possible at lower levels. Iron, even at the usual recommended level has been associated with gastrointestinal intolerance in some patients.
ContraindicationsView
Vitamin-B complex is contraindicated in patients hypersensitive to any of its components.
InteractionsView
As little as 5 mg pyridoxine daily can decrease the efficacy of levodopa in the treatment of parkinsonism. Therefore, Vitamin-B complex is not recommended for patients undergoing such therapy
Pregnancy & lactationView
It is safe to use Vitamin-B complex in pregnancy and lactation.
Orabex
Vitamin B complex
Orabex
Vitamin B complex
Indications
Vitamin B deficiencies
Indication detailsView
Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi
Therapeutic classView
Specific combined vitamin preparations
PharmacologyView
Vitamin-B complex contains the most important members of the vitamin B group in pure form and in therapeutically balanced proportions. The members of the vitamin B group contained in Vitamin-B complex are components of enzyme systems that regulate various stages of carbohydrate, fat and protein metabolism, each of the components playing a specific biological role. Deficiency of B vitamin causes glossitis, stomatitis, cheilosis, polyneuritis, beriberi, pellagra and vascularisation of cornea.
DosageView
Tablet/ capsule: usual recommended dose is 1-2 tablet/capsule 3 times daily or as directed by the physician.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Side effectsView
Adverse reactions have been reported with specific vitamins and minerals, but generally at levels substantially higher than those in Vitamin-B complex. However, allergic and idiosyncratic reactions are possible at lower levels. Iron, even at the usual recommended level has been associated with gastrointestinal intolerance in some patients.
ContraindicationsView
Vitamin-B complex is contraindicated in patients hypersensitive to any of its components.
InteractionsView
As little as 5 mg pyridoxine daily can decrease the efficacy of levodopa in the treatment of parkinsonism. Therefore, Vitamin-B complex is not recommended for patients undergoing such therapy
Pregnancy & lactationView
It is safe to use Vitamin-B complex in pregnancy and lactation.
Orabex
Vitamin B complex
Orabex
Vitamin B complex
Indications
Vitamin B deficiencies
Indication detailsView
Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi Vitamin-B complex is indicated for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi
Therapeutic classView
Specific combined vitamin preparations
PharmacologyView
Vitamin-B complex contains the most important members of the vitamin B group in pure form and in therapeutically balanced proportions. The members of the vitamin B group contained in Vitamin-B complex are components of enzyme systems that regulate various stages of carbohydrate, fat and protein metabolism, each of the components playing a specific biological role. Deficiency of B vitamin causes glossitis, stomatitis, cheilosis, polyneuritis, beriberi, pellagra and vascularisation of cornea.
DosageView
Tablet/ capsule: usual recommended dose is 1-2 tablet/capsule 3 times daily or as directed by the physician.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Syrup: 2-3 teaspoonful daily or as directed by the physician.
Injection: It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition with Thiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from contains D-Panthenol 5 mg.
Side effectsView
Adverse reactions have been reported with specific vitamins and minerals, but generally at levels substantially higher than those in Vitamin-B complex. However, allergic and idiosyncratic reactions are possible at lower levels. Iron, even at the usual recommended level has been associated with gastrointestinal intolerance in some patients.
ContraindicationsView
Vitamin-B complex is contraindicated in patients hypersensitive to any of its components.
InteractionsView
As little as 5 mg pyridoxine daily can decrease the efficacy of levodopa in the treatment of parkinsonism. Therefore, Vitamin-B complex is not recommended for patients undergoing such therapy
Pregnancy & lactationView
It is safe to use Vitamin-B complex in pregnancy and lactation.
Orabis
Bisoprolol Hemifumarate
Orabis
Bisoprolol Hemifumarate
Indications
Hypertension
Indication detailsView
Bisoprolol is indicated in-
- Hypertension
- Angina
- Moderate to severe heart failure
Therapeutic classView
Anti adrenergic agent (Beta blockers), Beta-adrenoceptor blocking drugs, Beta-blockers
PharmacologyView
Bisoprolol Hemifumarate is the most selective ß1 blocker. It displays highest level of affinity for the ß1 receptor than any other beta-blocker available up to now. Selectively blocks ß1 adrenergic receptor in the heart and vascular smooth muscle and reduces heart rate and cardiac output resulting in decrease of arterial hypertension. Lipid metabolism can be adversely affected by ß-blockers, in patients with non-ß1 selective ß1-blocker, but Bisoprolol does not cause any change in the cholesterol fraction including the cardioprotective HDL-cholesterol, in long-term therapy.
DosageView
Adult: In the treatment of mild to moderate hypertension, Bisoprolol fumarate must be individualized to the needs of the patient. The usual starting dose is 5 mg once daily either added to a diuretic or alone. If the response to 5 mg is inadequate, the dose may be increased to 10 mg and then, if necessary, to 20 mg once daily. An appropriate interval for dose titration is 2 weeks. Increasing the dose beyond 20 mg once daily produces only a small incremental benefit.
Children: Safety and effectiveness in children have not been established.
Patients With Renal or Hepatic Impairment: In patients with hepatic impairment (hepatitis or cirrhosis) or renal dysfunction (creatinine clearance less than 40 mL/min) as in other patients, the initial daily dose should be 5 mg. Because of the possibility of accumulation, caution must be used in dose titration. Since limited data suggest that bisoprolol fumarate is not dialysable, drug replacement is not necessary in patients undergoing dialysis.
Geriatrics: In the elderly, it is not usually necessary to adjust the dose, unless there is also significant renal or hepatic dysfunction
Children: Safety and effectiveness in children have not been established.
Patients With Renal or Hepatic Impairment: In patients with hepatic impairment (hepatitis or cirrhosis) or renal dysfunction (creatinine clearance less than 40 mL/min) as in other patients, the initial daily dose should be 5 mg. Because of the possibility of accumulation, caution must be used in dose titration. Since limited data suggest that bisoprolol fumarate is not dialysable, drug replacement is not necessary in patients undergoing dialysis.
Geriatrics: In the elderly, it is not usually necessary to adjust the dose, unless there is also significant renal or hepatic dysfunction
Side effectsView
Bisoprolol, like any medication, may have some side effects. It is important that you keep your doctor informed of all side effects especially if you experience one of the following for several days. The most common side effects, whether or not caused by Bisoprolol, are: headache, fatigue, urinary tract infection, rhinitis or sinusitis (inflammation in the nose), diarrhea, dizziness, peripheral edema (swelling of the ankles), joint pain, cough, insomnia (trouble sleeping), nausea (feeling like vomiting), and sore throat. You must seek medical attention immediately if you experience an allergic reaction with symptoms of rash, itching, swelling, dizziness or trouble breathing.
Medicines affect different people in different ways. Just because side effects have occurred in other patients does not mean you will get them. Discuss how you feel on Bisoprolol with your doctor or pharmacist. Do not stop or restart Bisoprolol on your own.
Medicines affect different people in different ways. Just because side effects have occurred in other patients does not mean you will get them. Discuss how you feel on Bisoprolol with your doctor or pharmacist. Do not stop or restart Bisoprolol on your own.
ContraindicationsView
In patients with cardiogenic shock, overt heart failure, second or third degree A-V block, right ventricular failure secondary to pulmonary hypertension and sinus bradycardia.
PrecautionsView
Monitoring of renal, hepatic and hematopoietic function should be performed at regular intervals during long-term treatment with bisoprolol.
InteractionsView
Other β-blocking Agents: Bisoprolol fumarate should not be combined with other β-blocking agents.
Catecholamine-Depleting Drugs: Patients receiving catecholamine-depleting drugs, such as reserpine or guanethidine, should be monitored closely because the added β-adrenergic blocking action of bisoprolol fumarate may produce excessive reduction of sympathetic activity.
Centrally Active Antihypertensive Agents: β-blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. If the two drugs are coadministered, the β-blocker should be withdrawn several days before discontinuing clonidine. If replacing clonidine by β-blocker therapy, the introduction of β-blockers should be delayed for several days after clonidine administration has stopped (see also prescribing information for clonidine).
Antiarrhythmic Agents: Bisoprolol fumarate should be used with care when myocardial depressants or inhibitors of A-V conduction, such as certain calcium antagonists (particularly of the phenyl alkylamine (verapamil) and benzothiazepine (diltiazem) classes), or antiarrhythmic agents, such as disopyramide, are used concurrently.
Calcium Channel Blockers: Combined use of β-blockers and calcium channel blockers with negative inotropic effects can lead to prolongation of S-A and A-V conduction, particularly in patients with impaired ventricular function or conduction abnormalities. This may result in severe hypotension, bradycardia and cardiac failure.
Catecholamine-Depleting Drugs: Patients receiving catecholamine-depleting drugs, such as reserpine or guanethidine, should be monitored closely because the added β-adrenergic blocking action of bisoprolol fumarate may produce excessive reduction of sympathetic activity.
Centrally Active Antihypertensive Agents: β-blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. If the two drugs are coadministered, the β-blocker should be withdrawn several days before discontinuing clonidine. If replacing clonidine by β-blocker therapy, the introduction of β-blockers should be delayed for several days after clonidine administration has stopped (see also prescribing information for clonidine).
Antiarrhythmic Agents: Bisoprolol fumarate should be used with care when myocardial depressants or inhibitors of A-V conduction, such as certain calcium antagonists (particularly of the phenyl alkylamine (verapamil) and benzothiazepine (diltiazem) classes), or antiarrhythmic agents, such as disopyramide, are used concurrently.
Calcium Channel Blockers: Combined use of β-blockers and calcium channel blockers with negative inotropic effects can lead to prolongation of S-A and A-V conduction, particularly in patients with impaired ventricular function or conduction abnormalities. This may result in severe hypotension, bradycardia and cardiac failure.
Pregnancy & lactationView
Pregnancy: Bisoprolol fumarate was not teratogenic in rats at doses up to 150 mg/kg/day, which is 375 times the maximum recommended human daily dose. Bisoprolol fumarate was fetotoxic (increased late resorptions) at 50 mg/kg/day and maternotoxic (decreased food intake and body-weight gain) at 150 mg/kg/day. Bisoprolol fumarate was not teratogenic in rabbits at doses up to 12.5 mg/kg/day, which is 31 times the maximum recommended human daily dose, but was embryolethal (increased early resorptions) at 12.5 mg/kg/day. There are no studies in pregnant women. Bisoprolol fumarate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Small amounts of bisoprolol fumarate (<2% of the dose) have been detected in the milk of lactating rats. It is not known whether this drug is excreted in human milk. If use of bisoprolol fumarate is considered essential, then mothers should stop nursing.
Lactation: Small amounts of bisoprolol fumarate (<2% of the dose) have been detected in the milk of lactating rats. It is not known whether this drug is excreted in human milk. If use of bisoprolol fumarate is considered essential, then mothers should stop nursing.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.
Orabis
Bisoprolol Hemifumarate
Orabis
Bisoprolol Hemifumarate
Indications
Hypertension
Indication detailsView
Bisoprolol is indicated in-
- Hypertension
- Angina
- Moderate to severe heart failure
Therapeutic classView
Anti adrenergic agent (Beta blockers), Beta-adrenoceptor blocking drugs, Beta-blockers
PharmacologyView
Bisoprolol Hemifumarate is the most selective ß1 blocker. It displays highest level of affinity for the ß1 receptor than any other beta-blocker available up to now. Selectively blocks ß1 adrenergic receptor in the heart and vascular smooth muscle and reduces heart rate and cardiac output resulting in decrease of arterial hypertension. Lipid metabolism can be adversely affected by ß-blockers, in patients with non-ß1 selective ß1-blocker, but Bisoprolol does not cause any change in the cholesterol fraction including the cardioprotective HDL-cholesterol, in long-term therapy.
DosageView
Adult: In the treatment of mild to moderate hypertension, Bisoprolol fumarate must be individualized to the needs of the patient. The usual starting dose is 5 mg once daily either added to a diuretic or alone. If the response to 5 mg is inadequate, the dose may be increased to 10 mg and then, if necessary, to 20 mg once daily. An appropriate interval for dose titration is 2 weeks. Increasing the dose beyond 20 mg once daily produces only a small incremental benefit.
Children: Safety and effectiveness in children have not been established.
Patients With Renal or Hepatic Impairment: In patients with hepatic impairment (hepatitis or cirrhosis) or renal dysfunction (creatinine clearance less than 40 mL/min) as in other patients, the initial daily dose should be 5 mg. Because of the possibility of accumulation, caution must be used in dose titration. Since limited data suggest that bisoprolol fumarate is not dialysable, drug replacement is not necessary in patients undergoing dialysis.
Geriatrics: In the elderly, it is not usually necessary to adjust the dose, unless there is also significant renal or hepatic dysfunction
Children: Safety and effectiveness in children have not been established.
Patients With Renal or Hepatic Impairment: In patients with hepatic impairment (hepatitis or cirrhosis) or renal dysfunction (creatinine clearance less than 40 mL/min) as in other patients, the initial daily dose should be 5 mg. Because of the possibility of accumulation, caution must be used in dose titration. Since limited data suggest that bisoprolol fumarate is not dialysable, drug replacement is not necessary in patients undergoing dialysis.
Geriatrics: In the elderly, it is not usually necessary to adjust the dose, unless there is also significant renal or hepatic dysfunction
Side effectsView
Bisoprolol, like any medication, may have some side effects. It is important that you keep your doctor informed of all side effects especially if you experience one of the following for several days. The most common side effects, whether or not caused by Bisoprolol, are: headache, fatigue, urinary tract infection, rhinitis or sinusitis (inflammation in the nose), diarrhea, dizziness, peripheral edema (swelling of the ankles), joint pain, cough, insomnia (trouble sleeping), nausea (feeling like vomiting), and sore throat. You must seek medical attention immediately if you experience an allergic reaction with symptoms of rash, itching, swelling, dizziness or trouble breathing.
Medicines affect different people in different ways. Just because side effects have occurred in other patients does not mean you will get them. Discuss how you feel on Bisoprolol with your doctor or pharmacist. Do not stop or restart Bisoprolol on your own.
Medicines affect different people in different ways. Just because side effects have occurred in other patients does not mean you will get them. Discuss how you feel on Bisoprolol with your doctor or pharmacist. Do not stop or restart Bisoprolol on your own.
ContraindicationsView
In patients with cardiogenic shock, overt heart failure, second or third degree A-V block, right ventricular failure secondary to pulmonary hypertension and sinus bradycardia.
PrecautionsView
Monitoring of renal, hepatic and hematopoietic function should be performed at regular intervals during long-term treatment with bisoprolol.
InteractionsView
Other β-blocking Agents: Bisoprolol fumarate should not be combined with other β-blocking agents.
Catecholamine-Depleting Drugs: Patients receiving catecholamine-depleting drugs, such as reserpine or guanethidine, should be monitored closely because the added β-adrenergic blocking action of bisoprolol fumarate may produce excessive reduction of sympathetic activity.
Centrally Active Antihypertensive Agents: β-blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. If the two drugs are coadministered, the β-blocker should be withdrawn several days before discontinuing clonidine. If replacing clonidine by β-blocker therapy, the introduction of β-blockers should be delayed for several days after clonidine administration has stopped (see also prescribing information for clonidine).
Antiarrhythmic Agents: Bisoprolol fumarate should be used with care when myocardial depressants or inhibitors of A-V conduction, such as certain calcium antagonists (particularly of the phenyl alkylamine (verapamil) and benzothiazepine (diltiazem) classes), or antiarrhythmic agents, such as disopyramide, are used concurrently.
Calcium Channel Blockers: Combined use of β-blockers and calcium channel blockers with negative inotropic effects can lead to prolongation of S-A and A-V conduction, particularly in patients with impaired ventricular function or conduction abnormalities. This may result in severe hypotension, bradycardia and cardiac failure.
Catecholamine-Depleting Drugs: Patients receiving catecholamine-depleting drugs, such as reserpine or guanethidine, should be monitored closely because the added β-adrenergic blocking action of bisoprolol fumarate may produce excessive reduction of sympathetic activity.
Centrally Active Antihypertensive Agents: β-blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. If the two drugs are coadministered, the β-blocker should be withdrawn several days before discontinuing clonidine. If replacing clonidine by β-blocker therapy, the introduction of β-blockers should be delayed for several days after clonidine administration has stopped (see also prescribing information for clonidine).
Antiarrhythmic Agents: Bisoprolol fumarate should be used with care when myocardial depressants or inhibitors of A-V conduction, such as certain calcium antagonists (particularly of the phenyl alkylamine (verapamil) and benzothiazepine (diltiazem) classes), or antiarrhythmic agents, such as disopyramide, are used concurrently.
Calcium Channel Blockers: Combined use of β-blockers and calcium channel blockers with negative inotropic effects can lead to prolongation of S-A and A-V conduction, particularly in patients with impaired ventricular function or conduction abnormalities. This may result in severe hypotension, bradycardia and cardiac failure.
Pregnancy & lactationView
Pregnancy: Bisoprolol fumarate was not teratogenic in rats at doses up to 150 mg/kg/day, which is 375 times the maximum recommended human daily dose. Bisoprolol fumarate was fetotoxic (increased late resorptions) at 50 mg/kg/day and maternotoxic (decreased food intake and body-weight gain) at 150 mg/kg/day. Bisoprolol fumarate was not teratogenic in rabbits at doses up to 12.5 mg/kg/day, which is 31 times the maximum recommended human daily dose, but was embryolethal (increased early resorptions) at 12.5 mg/kg/day. There are no studies in pregnant women. Bisoprolol fumarate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Small amounts of bisoprolol fumarate (<2% of the dose) have been detected in the milk of lactating rats. It is not known whether this drug is excreted in human milk. If use of bisoprolol fumarate is considered essential, then mothers should stop nursing.
Lactation: Small amounts of bisoprolol fumarate (<2% of the dose) have been detected in the milk of lactating rats. It is not known whether this drug is excreted in human milk. If use of bisoprolol fumarate is considered essential, then mothers should stop nursing.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.
Oracal
Calcium Carbonate
Oracal
Calcium Carbonate
Indication detailsView
250 mg or 500 mg tablet: This is used for the treatment or prevention of calcium depletion in patients in whom dietary measures are inadequate. Conditions that may be associated with calcium deficiency include hypoparathyroidism, achlorhydria, chronic diarrhea, vitamin D deficiency, steatorrhea, sprue, pregnancy and lactation, menopause, pancreatitis, renal failure, alkalosis, and hyperphosphataemia. Calcium Carbonate is being used increasingly often to treat hyperphosphataemia in chronic renal failure as well as those on continuous ambulatory peritoneal dialysis (CAPD) and haemodialysis. Many patients are unable to tolerate sufficient doses for complete phosphate control and require additional measures such as stringent dietary phosphate restriction or relatively small doses of aluminium hydroxide. Calcium Carbonate containing preparations can provide short-term relief of dyspeptic systems but are no longer recommended for long-term treatment of peptic ulceration.
1000 mg tablet: This is indicated for the management of conditions associated with hyperidity and for fast relief of acid indigestion, heartburn, sour stomach and upset stomach.
1000 mg tablet: This is indicated for the management of conditions associated with hyperidity and for fast relief of acid indigestion, heartburn, sour stomach and upset stomach.
Therapeutic classView
Minerals in bone formation, Specific mineral preparations
PharmacologyView
Calcium carbonate reacts with gastric acid to produce a salt and water. For calcium carbonate the postulated chemical reaction is: CaCO3+2HCl = CaCl2+H2O+CO2. Two grams of calcium carbonate will readily bring 100 ml of hydrochloric acid to a pH above 6. The increase in gastric pH diminishes the activity of pepsin in the gastric secretion. Up to 30% of the oral calcium load may be absorbed.
DosageView
250 mg or 500 mg tablet: Calcium Carbonate is always used orally and when used as an antacid the recommended doses for adults are equivalent to 540-2000 mg Calcium Carbonate per day, doses for children being half of those for adults. As a dietary supplement, such as for the prevention of osteoporosis, 1250-3750 mg Calcium Carbonate (500-1500 mg calcium) daily is recommended in general, but again this will need to be tailored to the individual patient depending on any specific disease such as Calcium deficiency, malabsorption or parathyroid function. In pregnancy and lactation the recommended daily dose of calcium is 1200-1500 mg. In chronic renal failure the doses used vary from 2.5-9.0 gm Calcium Carbonate per day and need to be adjusted according to the individual patient. To maximize effective phosphate binding in this context the Calcium Carbonate should be given with meals.
1000 mg tablet: 2000-3000 mg tablet when symptoms occur; may be repeated hourly if needed or as directed by the physician.
1000 mg tablet: 2000-3000 mg tablet when symptoms occur; may be repeated hourly if needed or as directed by the physician.
Side effectsView
Orally administered Calcium Carbonate may be irritating to the GI tract. It may also cause constipation. Hypercalcaemia is rarely produced by administration of calcium alone, but may occur when large doses are given to patients with chronic renal failure.
ContraindicationsView
- Hypercalcaemia and hyperparathyroidism
- Hypercalciuria and nephrolithiasis
- Zollinger-Ellison syndrome
- Concomitant digoxin therapy (requires careful monitoring of serum calcium level)
InteractionsView
Calcium Carbonate may enhance the cardiac effects of digoxin and other cardiac glycosides, if systemic hypercalcaemia occurs. Calcium Carbonate may interfere with the absorption of concomitantly administered tetracycline preparations and in chronic renal failure modification of vitamin D therapy may be required to avoid hypercalcaemia when Calcium Carbonate is used as the primary phosphate binder.
Pregnancy & lactationView
Calcium containing drugs have been widely used in pregnancy by way of oral calcium supplementation or antacid therapy. Calcium Carbonate can be used in lactating women too.
Pediatric usageView
Use in children: Calcium carbonate has been extensively studied in children and infants with chronic renal failure and is both safe and effective.
Use in elderly: In case of elderly patients with renal failure when calcium carbonate is taken constipation may be troublesome one for this group. For this reason, monitoring of serum calcium and phosphate is of course indicated for elderly patients.
Use in elderly: In case of elderly patients with renal failure when calcium carbonate is taken constipation may be troublesome one for this group. For this reason, monitoring of serum calcium and phosphate is of course indicated for elderly patients.
StorageView
Store in a cool, dry place in controlled room temperature.
Oracal D
Calcium Carbonate [Elemental source] + Vitamin D3
Oracal D
Calcium Carbonate [Elemental source] + Vitamin D3
Indications
Rickets
Indication detailsView
This combination is used for treatment of osteoporosis, osteomalacia, rickets, tetany and in parathyroid disease. Calcium supplements are often used to ensure adequate dietary intake in conditions such as pregnancy & lactation, osteogenesis and tooth formation (adjunct with definite treatment) and therapy with anti-seizure medications. It is also used as routine supplement and phosphate binder in chronic renal failure.
Therapeutic classView
Specific mineral & vitamin combined preparations
PharmacologyView
This is the preparation of Calcium Carbonate and Vitamin D3 (Cholecalciferol). Calcium is necessary for many normal functions of our body, especially bone formation and maintenance. Vitamin D3 helps for the absorption & reabsorption of Calcium. Vitamin D3 also stimulates bone formation. Clinical studies showed that Calcium and Vitamin D3 all together helps in bone growth, and in prevention of osteoporosis & bone fracture.
DosageView
Calcium 500 mg and Vitamin D3 200 IU Tablet: 2 tablets daily or 1 tablet twice daily. It is best taken with or just after a meal to improve absorption.
Calcium 500 mg and Vitamin D3 400 IU Tablet: 1 tablet twice daily. It is best taken with or just after a meal to improve absorption.
Calcium 500 mg and Vitamin D3 400 IU Tablet: 1 tablet twice daily. It is best taken with or just after a meal to improve absorption.
Side effectsView
It is generally well tolerated. If there is experience like nausea, vomiting, stomach cramps, dry mouth, increased thirst, increased urination while taking, noticed to physicians. Constipation may occur.
ContraindicationsView
It is contraindicated in case of hypercalcaemia, hyperthyroidism, renal calculi & nephrolithiasis and Zollinger-Ellison Syndrome.
PrecautionsView
If there is any pre-existing heart disease or kidney disease, precautions should be taken.
InteractionsView
It has possible interaction with calcium, aluminium or magnesium containing antacids & other calcium supplements, calcitriol & other vitamin D3 supplements; digoxin, tetracycline, doxycycline, minocycline or oxytetracycline.
Pregnancy & lactationView
This combination should be used as directed by physician during pregnancy or while breast-feeding.
Overdose effectsView
Symptoms of overdosage may include nausea and vomiting, severe drowsiness, dry mouth, loss of appetite, metallic taste, stomach cramps, diarrhea, headache, constipation.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.
Oracal M
Calcium Carbonate + Vitamin D3 + Multimineral
Oracal M
Calcium Carbonate + Vitamin D3 + Multimineral
Indications
Vitamin deficiency
Indication detailsView
This preparation is indicated in-
- Prevention and treatment of osteoporosis
- To maintain strong bone growth
- For proper functioning of heart, muscle and nerves
- As nutritional supplement
- For bone development and regeneration of bone
- Pregnancy & lactation
- Deficiency state of Calcium, Vitamin D3, Magnesium, Zinc, Copper, Manganese & Boron
Therapeutic classView
Specific mineral & vitamin combined preparations
PharmacologyView
Nutrition is the most important to prevent osteoporosis and other bone related diseases. Calcium, Magnesium & Vitamin D3 are the macronutrients for bone. Without Vitamin D3 very little Calcium is absorbed. Like Calcium, Magnesium increases bone strength and rigidity. Recent epidemiological studies showed that some micronutrients like Copper, Manganese, Zinc & Boron play an important role in bone health. Deficiency of the micronutrients is noticed in patients with osteoporosis.
DosageView
2 tablets per day, preferably 1 tablet in the morning and 1 tablet in the evening.
Side effectsView
It is generally well tolerated. If there is experience like nausea, vomiting, stomach cramps, dry mouth, increased thirst, increased urination while taking, noticed to physicians. Side effects from micronutrient are rare.
ContraindicationsView
It is contraindicated in case of hypercalcaemia, hyperthyroidism, renal calculi & nephrolithiasis and Zollinger-Ellison Syndrome.
PrecautionsView
If there is any pre-existing heart disease or kidney disease, precautions should be taken.
InteractionsView
It has possible interaction with Calcium, Aluminium or Magnesium containing Antacids & other Calcium supplements, Calcitriol & other Vitamin D3 supplements; Digoxin, Tetracycline, Doxycycline, Minocycline or Oxytetracycline.
Pregnancy & lactationView
This combination should be used as directed by physician during pregnancy or while breast-feeding.
Overdose effectsView
Symptoms of overdosage may include nausea and vomiting, severe drowsiness, dry mouth, loss of appetite, metallic taste, stomach cramps, diarrhea, headache & constipation.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.
Oracyn-K
Phenoxymethyl Penicillin [Penicillin V]
Oracyn-K
Phenoxymethyl Penicillin [Penicillin V]
Indications
Vincent’s infection
Indication detailsView
For the treatment of mild to moderately severe bacterial infections, if these are due to penicillin susceptible pathogens and respond to therapy with oral penicillin, such as:
- infections of the ear, nose and throat regions, e.g., tonsillitis, pharyngitis, laryngitis, otitis media, sinusitis.
- infections of the lower respiratory tract, e.g., bronchitis and pneumonia, bronchopneumonia.
- infections due to beta-hemolytic streptococci of group A, e.g., scarlet fever, erysipelas, rheumatic fever.
- skin infections, e.g., pyodermia, furunculosis, phlegmon, erysipeloid, erythema migrans, insofar as the micro-organisms are penicillin-susceptible.
- lymphadenitis and lymphangitis of bacterial origin.
- infections of the buccal cavity, gums or jaws, e.g., inflammatory infiltrates, delayed dentition stages II and III, antral fistulae, secondary bacterial infection with Gram-positive pathogens following virus-induced gingivitis or stomatitis.
Therapeutic classView
Benzylpenicillin & Phenoxymethyl penicillin
PharmacologyView
Phenoxymethyl penicillin or penicillin V is acid-stable and is absorbed from the upper part of the small intestine. Of different forms of Phenoxymethyl penicillin, the potassium salt of Phenoxymethyl penicillin is best absorbed. This may be given with meals but maximum absorption is achieved when drug is administered orally at least 1 hour before or 2 hours after the meal. Phenoxymethyl penicillin offers a very convenient means of treating Grampositive infections. Phenoxymethyl penicillin has the distinct advantage over penicillin G in resistance to inactivation by gastric acid.
DosageView
The dosage of Phenoxymethyl penicillin should be determined according to the sensitivity of the causative micro-organism and the severity of the infection, and adjusted to the clinical response of the patient.
Adults: 250-500 mg 6 hourly
Children (above 1 year):
Adults: 250-500 mg 6 hourly
Children (above 1 year):
- 125-250 mg 6 hourly
- 125 mg/5 ml powder for suspension: 1-2 teaspoonful (5-10 ml) 6 hourly
- 250 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly
- 62.5-125 mg 6 hourly.
- 125 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly, or as prescribed by the physician.
AdministrationView
Phenoxymethyl Penicillin is best taken on an empty stomach, preferably one hour before meals. The tablets are swallowed without chewing with sufficient amounts of liquid. Before each use of this syrup, the bottle has to be shaken vigorously.
Side effectsView
Occasionally, hypersensitivity reactions involving the skin (e.g. urticaria, morbilliform or scarlatiniform rashes, pruritus), eosinophilia or more serious allergic reactions, e.g. drug fever, vasculitis, serum sickness or interstitial nephritis, may develop. Anaphylactic or anaphylactoid reactions accompanied by, e.g- angioneurotic oedema, oedema of the larynx, bronchial spasm and shock may occur.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
ContraindicationsView
Phenoxymethyl Penicillin must not be administered in patients with hypersensitivity to penicillins or any of the excipients of this. Phenoxymethyl Penicillin must not be used to treat patients with severe gastrointestinal disorders accompanied by vomiting and diarrhea.
PrecautionsView
The possibility of cross-allergy between cephalosporins and penicillins must be considered. When treating patients with heart diseases or serious electrolyte disturbances of other origin, the potassium content of Phenoxymethyl Penicillin may have to be considered. Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
InteractionsView
Food: Concurrent intake of food leads to a reduction in the rate of absorption. Therefore, Phenoxymethyl penicillin is best taken on an empty stomach, preferably one hour before meals, in order to reach the highest possible rate of absorption.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Pregnancy & lactationView
Phenoxymethylpenicillin crosses the placenta. Given the appropriate indication, this may be used at any time throughout pregnancy. Phenoxymethylpenicillin passes into the breast milk in small amounts. This may be used during lactation; however, diarrhoea and yeast colonization of mucous membranes may occur in the infant.
Overdose effectsView
The toxicity of phenoxymethylpenicillin is low, and it has a broad therapeutic range. When a multiple therapeutic dose is taken orally once only, phenoxymethylpenicillin has no acute toxicity. There is a risk of encephalopathy in cases of administration of beta-lactam antibiotics, particularly in case of overdose or renal impairment. Special measures in the event of overdosage, other than discontinuation of the medication, are not required. Elimination of phenoxymethylpenicillin can be accomplished through haemodialysis.
StorageView
Store in a cool and dry place, protect from light.
Oracyn-K
Phenoxymethyl Penicillin [Penicillin V]
Oracyn-K
Phenoxymethyl Penicillin [Penicillin V]
Indications
Vincent’s infection
Indication detailsView
For the treatment of mild to moderately severe bacterial infections, if these are due to penicillin susceptible pathogens and respond to therapy with oral penicillin, such as:
- infections of the ear, nose and throat regions, e.g., tonsillitis, pharyngitis, laryngitis, otitis media, sinusitis.
- infections of the lower respiratory tract, e.g., bronchitis and pneumonia, bronchopneumonia.
- infections due to beta-hemolytic streptococci of group A, e.g., scarlet fever, erysipelas, rheumatic fever.
- skin infections, e.g., pyodermia, furunculosis, phlegmon, erysipeloid, erythema migrans, insofar as the micro-organisms are penicillin-susceptible.
- lymphadenitis and lymphangitis of bacterial origin.
- infections of the buccal cavity, gums or jaws, e.g., inflammatory infiltrates, delayed dentition stages II and III, antral fistulae, secondary bacterial infection with Gram-positive pathogens following virus-induced gingivitis or stomatitis.
Therapeutic classView
Benzylpenicillin & Phenoxymethyl penicillin
PharmacologyView
Phenoxymethyl penicillin or penicillin V is acid-stable and is absorbed from the upper part of the small intestine. Of different forms of Phenoxymethyl penicillin, the potassium salt of Phenoxymethyl penicillin is best absorbed. This may be given with meals but maximum absorption is achieved when drug is administered orally at least 1 hour before or 2 hours after the meal. Phenoxymethyl penicillin offers a very convenient means of treating Grampositive infections. Phenoxymethyl penicillin has the distinct advantage over penicillin G in resistance to inactivation by gastric acid.
DosageView
The dosage of Phenoxymethyl penicillin should be determined according to the sensitivity of the causative micro-organism and the severity of the infection, and adjusted to the clinical response of the patient.
Adults: 250-500 mg 6 hourly
Children (above 1 year):
Adults: 250-500 mg 6 hourly
Children (above 1 year):
- 125-250 mg 6 hourly
- 125 mg/5 ml powder for suspension: 1-2 teaspoonful (5-10 ml) 6 hourly
- 250 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly
- 62.5-125 mg 6 hourly.
- 125 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly, or as prescribed by the physician.
AdministrationView
Phenoxymethyl Penicillin is best taken on an empty stomach, preferably one hour before meals. The tablets are swallowed without chewing with sufficient amounts of liquid. Before each use of this syrup, the bottle has to be shaken vigorously.
Side effectsView
Occasionally, hypersensitivity reactions involving the skin (e.g. urticaria, morbilliform or scarlatiniform rashes, pruritus), eosinophilia or more serious allergic reactions, e.g. drug fever, vasculitis, serum sickness or interstitial nephritis, may develop. Anaphylactic or anaphylactoid reactions accompanied by, e.g- angioneurotic oedema, oedema of the larynx, bronchial spasm and shock may occur.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
ContraindicationsView
Phenoxymethyl Penicillin must not be administered in patients with hypersensitivity to penicillins or any of the excipients of this. Phenoxymethyl Penicillin must not be used to treat patients with severe gastrointestinal disorders accompanied by vomiting and diarrhea.
PrecautionsView
The possibility of cross-allergy between cephalosporins and penicillins must be considered. When treating patients with heart diseases or serious electrolyte disturbances of other origin, the potassium content of Phenoxymethyl Penicillin may have to be considered. Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
InteractionsView
Food: Concurrent intake of food leads to a reduction in the rate of absorption. Therefore, Phenoxymethyl penicillin is best taken on an empty stomach, preferably one hour before meals, in order to reach the highest possible rate of absorption.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Pregnancy & lactationView
Phenoxymethylpenicillin crosses the placenta. Given the appropriate indication, this may be used at any time throughout pregnancy. Phenoxymethylpenicillin passes into the breast milk in small amounts. This may be used during lactation; however, diarrhoea and yeast colonization of mucous membranes may occur in the infant.
Overdose effectsView
The toxicity of phenoxymethylpenicillin is low, and it has a broad therapeutic range. When a multiple therapeutic dose is taken orally once only, phenoxymethylpenicillin has no acute toxicity. There is a risk of encephalopathy in cases of administration of beta-lactam antibiotics, particularly in case of overdose or renal impairment. Special measures in the event of overdosage, other than discontinuation of the medication, are not required. Elimination of phenoxymethylpenicillin can be accomplished through haemodialysis.
StorageView
Store in a cool and dry place, protect from light.
Oracyn-K
Phenoxymethyl Penicillin [Penicillin V]
Oracyn-K
Phenoxymethyl Penicillin [Penicillin V]
Indications
Vincent’s infection
Indication detailsView
For the treatment of mild to moderately severe bacterial infections, if these are due to penicillin susceptible pathogens and respond to therapy with oral penicillin, such as:
- infections of the ear, nose and throat regions, e.g., tonsillitis, pharyngitis, laryngitis, otitis media, sinusitis.
- infections of the lower respiratory tract, e.g., bronchitis and pneumonia, bronchopneumonia.
- infections due to beta-hemolytic streptococci of group A, e.g., scarlet fever, erysipelas, rheumatic fever.
- skin infections, e.g., pyodermia, furunculosis, phlegmon, erysipeloid, erythema migrans, insofar as the micro-organisms are penicillin-susceptible.
- lymphadenitis and lymphangitis of bacterial origin.
- infections of the buccal cavity, gums or jaws, e.g., inflammatory infiltrates, delayed dentition stages II and III, antral fistulae, secondary bacterial infection with Gram-positive pathogens following virus-induced gingivitis or stomatitis.
Therapeutic classView
Benzylpenicillin & Phenoxymethyl penicillin
PharmacologyView
Phenoxymethyl penicillin or penicillin V is acid-stable and is absorbed from the upper part of the small intestine. Of different forms of Phenoxymethyl penicillin, the potassium salt of Phenoxymethyl penicillin is best absorbed. This may be given with meals but maximum absorption is achieved when drug is administered orally at least 1 hour before or 2 hours after the meal. Phenoxymethyl penicillin offers a very convenient means of treating Grampositive infections. Phenoxymethyl penicillin has the distinct advantage over penicillin G in resistance to inactivation by gastric acid.
DosageView
The dosage of Phenoxymethyl penicillin should be determined according to the sensitivity of the causative micro-organism and the severity of the infection, and adjusted to the clinical response of the patient.
Adults: 250-500 mg 6 hourly
Children (above 1 year):
Adults: 250-500 mg 6 hourly
Children (above 1 year):
- 125-250 mg 6 hourly
- 125 mg/5 ml powder for suspension: 1-2 teaspoonful (5-10 ml) 6 hourly
- 250 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly
- 62.5-125 mg 6 hourly.
- 125 mg/5 ml powder for suspension: ½-1 teaspoonful (2.5-5 ml) 6 hourly, or as prescribed by the physician.
AdministrationView
Phenoxymethyl Penicillin is best taken on an empty stomach, preferably one hour before meals. The tablets are swallowed without chewing with sufficient amounts of liquid. Before each use of this syrup, the bottle has to be shaken vigorously.
Side effectsView
Occasionally, hypersensitivity reactions involving the skin (e.g. urticaria, morbilliform or scarlatiniform rashes, pruritus), eosinophilia or more serious allergic reactions, e.g. drug fever, vasculitis, serum sickness or interstitial nephritis, may develop. Anaphylactic or anaphylactoid reactions accompanied by, e.g- angioneurotic oedema, oedema of the larynx, bronchial spasm and shock may occur.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
In the event of signs pointing to anaphylactic/anaphylactoid reactions, the treatment must be terminated immediately. In occasional instances, there may be skin rashes or inflammation of mucous membranes, especially in the region of the mouth (stomatitis); dryness of the mouth and disorders of taste may rarely occur.
The occurrence of severe bullous skin reactions- usually involving the mucosae- has been reported in isolated cases (Stevens-Johnson syndrome, Lyell's syndrome). Gastrointestinal disturbances with, e.g., nausea, vomiting, abdominal pain, loose stools, or diarrhoea may develop.
Diarrhoea may sometimes be a symptom of enterocolitis which may, in some cases, be haemorrhagic. A particular form of enterocolitis that can occur with antibiotics is pseudomembranous colitis (in most cases due to Clostridium diffcile). This must be considered in patients in whom severe, persistent diarrhoea occurs during treatment or in the initial weeks thereafter. Even if pseudomembranous colitis is only suspected, administration of Phenoxymethyl penicillin must be halted immediately. This type of colitis requires immediate and appropriate treatment by a physician. Drugs that inhibit intestinal peristalsis must not be taken in such cases. In isolated cases, particularly after high doses and prolonged administration, changes in blood picture such as reduction in the number of white blood cells (e.g.,leucopenia, granulocytopenia, agranulocytosis), erythrocytes (e.g., due to haemolytic anaemia), thrombocytes, or pancytopenia and myelosuppression may occur. During treatment for spirochaetal infections, Herxheimer's reaction characterized by the occurrence or worsening of general symptoms such as fever, chills, headache, and joint pains may develop. In isolated cases, drug-induced aseptic meningitis may occur.
In extremely rare cases, transient discolouration of the teeth may be seen during treatment with Phenoxymethyl penicillin. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro organisms.
Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
ContraindicationsView
Phenoxymethyl Penicillin must not be administered in patients with hypersensitivity to penicillins or any of the excipients of this. Phenoxymethyl Penicillin must not be used to treat patients with severe gastrointestinal disorders accompanied by vomiting and diarrhea.
PrecautionsView
The possibility of cross-allergy between cephalosporins and penicillins must be considered. When treating patients with heart diseases or serious electrolyte disturbances of other origin, the potassium content of Phenoxymethyl Penicillin may have to be considered. Beta-lactams predispose the patient to encephalopathy risk (which may include convulsions, confusion, impairment of consciousness, movement disorders), particularly in case of overdose or renal impairment.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient's condition must therefore be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken. In patients with diabetes mellitus, the sugar content of Phenoxymethyl Penicillin syrup must be taken into consideration.
There is no indication of impaired ability to drive, or to operate machinery. Beta-lactams predispose the patient to encephalopathy risk. In the case of adverse reactions such as encephalopathy (which may include convulsions, confusion, impairment of consciousness, movement disorders), the patient should not operate machines or drive a vehicle.
InteractionsView
Food: Concurrent intake of food leads to a reduction in the rate of absorption. Therefore, Phenoxymethyl penicillin is best taken on an empty stomach, preferably one hour before meals, in order to reach the highest possible rate of absorption.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Drug interactions: Concomitant administration of penicillins may lead to increased levels of methotrexate in serum and potentiate its toxic effects. Monitoring of methotrexate serum levels is therefore necessary.
If diarrhoea occurs as a consequence of treatment with Phenoxymethyl penicillin, the absorption of other orally administered drugs may be disturbed and their effcacy may consequently be impaired. If penicillins are combined with bacteriostatic chemotherapeutics or antibiotics (e.g., tetracyclines, chloramphenicol), the activity of penicillins may be attenuated or abolished. Concurrent administration of probenecid inhibits the renal excretion of penicillins. Concurrent use of indomethacin, phenylbutazone, salicylates or sulfinpyrazone may cause elevated and prolonged serum levels of phenoxymethylpenicillin.
Administration of penicillins may cause a transient reduction in plasma concentrations of oestrogens and gestagens. The effectiveness of oral contraceptives is therefore uncertain.
The absorption of Phenoxymethyl penicillin may be reduced where intestinal sterilization with aminoglycosides (e.g. neomycin) has just been performed or is still in progress. Combined use of penicillins and oral anticoagulants (e.g. warfarin) may prolong prothrombin time/INR.
Interference with laboratory and diagnostic tests: Non-enzymatic urine glucose determinations and tests for urobilinogen may give false-positive results.
Pregnancy & lactationView
Phenoxymethylpenicillin crosses the placenta. Given the appropriate indication, this may be used at any time throughout pregnancy. Phenoxymethylpenicillin passes into the breast milk in small amounts. This may be used during lactation; however, diarrhoea and yeast colonization of mucous membranes may occur in the infant.
Overdose effectsView
The toxicity of phenoxymethylpenicillin is low, and it has a broad therapeutic range. When a multiple therapeutic dose is taken orally once only, phenoxymethylpenicillin has no acute toxicity. There is a risk of encephalopathy in cases of administration of beta-lactam antibiotics, particularly in case of overdose or renal impairment. Special measures in the event of overdosage, other than discontinuation of the medication, are not required. Elimination of phenoxymethylpenicillin can be accomplished through haemodialysis.
StorageView
Store in a cool and dry place, protect from light.
Oradexon
Dexamethasone
Oradexon
Dexamethasone
Indication detailsView
Allergic states: Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment in asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, perennial or seasonal allergic rhinitis and serum sickness.
Collagen disease: Like lupus erythematosus, rheumatoid arthritis etc.
Dermatologic diseases: Bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus and severe erythema multiforme (Stevens-Johnson syndrome).
Endocrine disorders: Primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, hypercalcemia associated with cancer and nonsuppurative thyroiditis.
Gastrointestinal diseases: Regional enteritis and ulcerative colitis.
Hematologic disorders: Acquired (autoimmune) hemolytic anemia, congenital (erythroid) hypoplastic anemia (Diamond-Blackfan anemia), idiopathic thrombocytopenic purpura in adults and selected cases of secondary thrombocytopenia.
Neoplastic diseases: Leukemias and lymphomas.
Nervous system: Acute exacerbations of multiple sclerosis, cerebral edema associated with primary or metastatic brain tumor, craniotomy or head injury.
Ophthalmic diseases: Temporal arteritis, uveitis, and ocular inflammatory conditions unresponsive to topical corticosteroids.
Renal diseases: To induce a diuresis or remission of proteinuria in idiopathic nephrotic syndrome or that due to lupus erythematosus.
Respiratory diseases: Berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis.
Rheumatic disorders: As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in acute gouty arthritis, acute rheumatic carditis, ankylosing spondylitis, psoriatic arthritis, rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy). For the treatment of dermatomyositis, polymyositis, and systemic lupus erythematosus.
Miscellaneous: Diagnostic testing of adrenocortical hyperfunction, trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used with appropriate antituberculous chemotherapy.
Collagen disease: Like lupus erythematosus, rheumatoid arthritis etc.
Dermatologic diseases: Bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus and severe erythema multiforme (Stevens-Johnson syndrome).
Endocrine disorders: Primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, hypercalcemia associated with cancer and nonsuppurative thyroiditis.
Gastrointestinal diseases: Regional enteritis and ulcerative colitis.
Hematologic disorders: Acquired (autoimmune) hemolytic anemia, congenital (erythroid) hypoplastic anemia (Diamond-Blackfan anemia), idiopathic thrombocytopenic purpura in adults and selected cases of secondary thrombocytopenia.
Neoplastic diseases: Leukemias and lymphomas.
Nervous system: Acute exacerbations of multiple sclerosis, cerebral edema associated with primary or metastatic brain tumor, craniotomy or head injury.
Ophthalmic diseases: Temporal arteritis, uveitis, and ocular inflammatory conditions unresponsive to topical corticosteroids.
Renal diseases: To induce a diuresis or remission of proteinuria in idiopathic nephrotic syndrome or that due to lupus erythematosus.
Respiratory diseases: Berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis.
Rheumatic disorders: As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in acute gouty arthritis, acute rheumatic carditis, ankylosing spondylitis, psoriatic arthritis, rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy). For the treatment of dermatomyositis, polymyositis, and systemic lupus erythematosus.
Miscellaneous: Diagnostic testing of adrenocortical hyperfunction, trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used with appropriate antituberculous chemotherapy.
PharmacologyView
Dexamethasone is a synthetic glucocorticoid which decreases inflammation by inhibiting the migration of leukocytes and reversal of increased capillary permeability. It suppresses normal immune response.
DosageView
In general, glucocorticoid dosage depends on the severity of the condition and the response of the patient. If no favourable response is noted within a couple of days, continuation of glucocorticoid therapy is undesirable. In chronic conditions requiring long-term therapy the lowest dosage that provides adequate, but not necessarily complete, relief should be used.
For tablet:
For tablet:
- In adult patients, daily oral dosages vary from 1 mg to 10 mg and in children from 0.03-0.20 mg/kg body weight,according to the individual response.
- In some patients higher dosages may be temporarily required,to control the disease. As soon as circumstances permit,dosage should be decreased.
- For a short dexamethasone suppression test 1 mg dexamethasone is given at 11 p.m. and plasmacortisol measured the next morning.
- Patients who do not show a decrease in cortisol can be exposed to a longer test: 0.5 mg dexamethasone is given at 6-hour intervals
- for 48 hours followed by 2 mg every 6 hours for a further 48 hours. 24-hour urine collections are made before, during and at the end of the test for the determination of 17 alpha-hydroxycorticoids.
- Dexamethasone can be given by intravenous (IV), intramuscular (IM) or local injection. Dexamethasone injections can also be diluted with an infusion fluid or be injected directly into the infusion line.
- Intravenous injections of massive doses should be given slowly, over a period of several minutes.
- Intramuscular administration should be given by deep intramuscular injection,to prevent atrophy of the subcutaneous adipose tissues.
- Intra-articular injections should be given under strictly aseptic conditions as glucocorticoids decrease the resistance to infection. When diluted with these infusion fluids, Dexamethasone will keep its potency for at least 24 hours (at room temperature and in daylight conditions). As infusion fluids, Sodium chloride 0.9%, Anhydrous glucose 5%, Invert sugar 10%, Sorbitol 5%, Ringer's solution, Hartman's solution (Ringer-lactate) etc.can be used.
- The dosage of Dexamethasone depends on the severity of the condition and the response of the patient.
- For systemic therapy in adults, daily doses of 0.05-0.20 mg/kg body weight are usually sufficient. For emergencies (e.g. anaphylaxis, acute severe asthma, cerebral edema) substantially higher doses are required. An initial dose of 10-20 mg IV is followed by 6 mg IV or IM every 6 hours,until a satisfactory result has been obtained. Thereafter the dosage has to be tapered off gradually.
- Intra-articularly: 2-4 mg in large and 0.8-1 mg in small joints
- Intrabursally: 2-4 mg;in tendon sheaths:0.4-1 mg
- The frequency of these injections may vary from every 3-5 days to every 2-3 weeks
Side effectsView
The following adverse reactions have been associated with prolonged systemic glucocorticoid therapy.
Endocrine and metabolic disturbances: Cushing-like syndrome, hirsutism, menstrual irregularities, premature epiphyseal closure, secondary adrenocortical and pituitary unresponsiveness, decreased glucose tolerance, negative nitrogen and calcium balance.
Fluid and electrolyte disturbances: Sodium and fluid retention, hypertension, potassium loss, hypokalaemic alkalosis.
Musculo-skeletal effects: Myopathy, abdominal distension, osteoporosis, aseptic necrosis of femoral and humeral heads.
Gastro-intestinal effects: Gastric and duodenal ulceration, perforation and haemorrhage.
Dermatological effects: Impaired wound healing, skin atrophy, striae, petechiae and ecchymoses, bruising, facial erythema, increased sweating, acne.
Central Nervous System effects: Psychic disturbances ranging from euphoria to frank psychotic manifestations,convulsions,in children pseudotumor cerebri (benign intracranial hypertension) with vomiting and papilloedema.
Ophthalmic effects: Glaucoma, increased intraocular pressure, posterior subcapsular cataracts.
Immunosuppressive effects: Increased susceptibility to infections, decreased responsiveness to vaccination and skin tests.
Endocrine and metabolic disturbances: Cushing-like syndrome, hirsutism, menstrual irregularities, premature epiphyseal closure, secondary adrenocortical and pituitary unresponsiveness, decreased glucose tolerance, negative nitrogen and calcium balance.
Fluid and electrolyte disturbances: Sodium and fluid retention, hypertension, potassium loss, hypokalaemic alkalosis.
Musculo-skeletal effects: Myopathy, abdominal distension, osteoporosis, aseptic necrosis of femoral and humeral heads.
Gastro-intestinal effects: Gastric and duodenal ulceration, perforation and haemorrhage.
Dermatological effects: Impaired wound healing, skin atrophy, striae, petechiae and ecchymoses, bruising, facial erythema, increased sweating, acne.
Central Nervous System effects: Psychic disturbances ranging from euphoria to frank psychotic manifestations,convulsions,in children pseudotumor cerebri (benign intracranial hypertension) with vomiting and papilloedema.
Ophthalmic effects: Glaucoma, increased intraocular pressure, posterior subcapsular cataracts.
Immunosuppressive effects: Increased susceptibility to infections, decreased responsiveness to vaccination and skin tests.
ContraindicationsView
- Gastric and duodenal ulcers.
- Systemic and ophthalmic fungal infections.
- Viral infections, e.g. varicella and herpes genitalis infections. Viral infections of the eye.
- Glaucoma.
- Hypersensitivity to corticosteroids
PrecautionsView
General: The lowest possible dose of corticosteroids should be used to control the condition under treatment.The reduction should be gradual.
Cardio-renal: These agents should be used with caution in patients with congestive heart failure,hypertension, or renal insufficiency.
Endocrine: Drug-induced secondary adrenocortical insufficiency may be minimized by gradual reduction of dosage.
Gastrointestinal: Steroids should be used with caution in active or latent peptic ulcers, diverticulitis, intestinal anastomoses, and nonspecific ulcerative colitis, since they may increase the risk of a perforation.
Musculoskeletal: Special consideration should be given to patients at increased risk of osteoporosis (e.g.,postmenopausal women) before initiating corticosteroid therapy.
Neuro-psychiatric: An acute myopathy has been observed with the use of high doses of corticosteroids, most often occurring in patients with myasthenia gravis or in patients receiving concomitant therapy with neuromuscular blocking drugs (e.g., pancuronium). Psychic derangements may appear ranging from euphoria, insomnia, mood swings, personality changes, and severe depression, to frank psychotic manifestations.
Cardio-renal: These agents should be used with caution in patients with congestive heart failure,hypertension, or renal insufficiency.
Endocrine: Drug-induced secondary adrenocortical insufficiency may be minimized by gradual reduction of dosage.
Gastrointestinal: Steroids should be used with caution in active or latent peptic ulcers, diverticulitis, intestinal anastomoses, and nonspecific ulcerative colitis, since they may increase the risk of a perforation.
Musculoskeletal: Special consideration should be given to patients at increased risk of osteoporosis (e.g.,postmenopausal women) before initiating corticosteroid therapy.
Neuro-psychiatric: An acute myopathy has been observed with the use of high doses of corticosteroids, most often occurring in patients with myasthenia gravis or in patients receiving concomitant therapy with neuromuscular blocking drugs (e.g., pancuronium). Psychic derangements may appear ranging from euphoria, insomnia, mood swings, personality changes, and severe depression, to frank psychotic manifestations.
InteractionsView
- Diuretics and/or cardiac glycosides, since potassium loss may be enhanced.This is a particular risk in patients using cardiac glycosides; since hypokalaemia increases the toxicity of these drugs.
- Antidiabetics, since glucocorticoids may impair glucose tolerance, thereby increasing the need for antidiabetic drugs.
- Non-steroidal anti-inflammatory drugs, since the incidence and/or severity of gastro-intestinal ulceration may increase.
- Oral anti-coagulants since glucocorticoids may alter the need for these drugs.
- Glucocorticoids may be less effective when used concomitantly with liver enzyme inducing drugs,such as rifampicin, ephedrine, barbiturates, phenytoin and primidone.
- If patients undergoing long-term therapy with glucocorticoids are concomitantly given salicylates, any reduction in glucocorticoid dosage should be made with caution, since salicylate intoxication has been reported in such cases.
- Antacids;especially those containing magnesium trisilicate,have been reported to impair the gastro-intestinal absorption of glucocorticoids. Therefore, doses of one agent should be spaced as far as possible from the other.
Pregnancy & lactationView
Pregnancy Category C.There are no adequate and well-controlled studies in pregnant women. Corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Glucocorticoids appear in breast milk.Mothers taking high dosages of corticosteroids should be advised not to breast-feed
Pediatric usageView
In order to minimize the potential growth effects of corticosteroids, pediatric patients should be titrated to the lowest effective dose.
Overdose effectsView
Overdosage is unlikely, however, treatment of overdosage is by supportive and symptomatic therapy
StorageView
Tablet: Store in a cool & dry place, protected from light & moisture.
Injection: Store below 30° C, protected from light.Do not freeze. Keep medicines out of the reach of children
Injection: Store below 30° C, protected from light.Do not freeze. Keep medicines out of the reach of children