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Xelpro
Esomeprazole
Xelpro
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.
Xelpro
Esomeprazole
Xelpro
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.
Xelpro MUPS
Esomeprazole (MUPS tablet)
Xelpro MUPS
Esomeprazole (MUPS tablet)
Indication detailsView
Esomeprazole MUPS tablet is indicated in:
- Gastro-esophageal Reflux Disease (GERD).
- Risk reduction in NSAID associated gastric ulcer.
- H. pylori eradication (Triple therapy).
- Zollinger-Ellison syndrome and idiopathic hypersecretion.
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.
DosageView
Erosive esophagitis-
Children 1-11 years:
- Adult (≥18 years): 40 mg once daily for 4 weeks.
- Children & adolescents (12-18 years): 40 mg once daily for 4 weeks.
- Adult (≥18 years): 20 mg once daily.
- Children & adolescents (12-18 years): 20 mg once daily.
- Adult (≥18 years): 20 mg once daily for 4-8 weeks.
- Adult (≥18 years): 20 mg twice daily for 7 days.
- Children & adolescents (12-18 years): 20 mg twice daily for 7 days.
- Adult (≥18 years): 40-80 mg twice daily.
Children 1-11 years:
- Erosive esophagitis: Weight <20 kg: 10 mg once daily for 8 weeks. Weight ≥20 kg: 10 mg or 20 mg once daily for 8 weeks
- Maintenance of healing of erosive esophagitis: 10 mg once daily
AdministrationView
Esomeprazole MUPS tablets should be swallowed whole with liquid. The tablets should not be chewed or crushed. If required, the tablets can also be dispersed in half a glass of non-carbonated water (mineral water is not suitable). No other liquids should be used. Stir until the tablets disintegrate and drink the liquid with the pellets immediately or within 30 minutes. Rinse the glass with half a glass of water and drink. The pellets must not be chewed or crushed.
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
Esomeprazole should be used carefully if the patient has severe liver dysfunction and severe renal impairment. Taking a proton pump inhibitor like Esomeprazole may slightly increase the risk of hip, wrist and spine fracture, particularly when it is taken over a period of more than one year.
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 anddiazepam, 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 anddiazepam, 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
The manufacturer advises caution. It is not known if Esomeprazole or its metabolites appear in human breast milk.
StorageView
Store in a cool & dry place below 25ºC, protect from light. Keep out of reach of children.
Xemi
Gemifloxacin
Xemi
Gemifloxacin
Indications
Pneumonia
Indication detailsView
Gemifloxacin is indicated for the treatment of the following bacterial infections in adults caused by sensitive organisms as follows-
- Acute bacterial exacerbation of chronic bronchitis: caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, or Moraxella catarrhalis.
- Community-acquired pneumonia (of mild to moderate severity): caused by Streptococcus pneumoniae (including multi-drug resistant strains), Haemophilus influenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, Chlamydia pneumoniae, or Klebsiella pneumoniae.
Therapeutic classView
4-Quinolone preparations
PharmacologyView
Gemifloxacin is a fluoroquinolone antibiotic. It is bactericidal with minimum bactericidal concentrations. Gemifloxacin acts by inhibiting DNA synthesis through inhibition of the bacterial type II topoisomerases, DNA gyrase, and/or topoisomerase IV (TOPO IV) which are both essential for bacterial growth.
Gemifloxacin is rapidly absorbed after oral administration. It is widely distributed throughout the body. Studies in healthy subjects showed that gemifloxacin is distributed rapidly into target tissues and body fluids such as the lung (epithelial lining fluid, alveolar macrophages, bronchial tissue) and nasal secretions.
Following oral administration of gemifloxacin, approximately 36% and 61% of the dose is excreted in the urine and feces, respectively, as unchanged drug and metabolites. AUC values were generally only slightly higher (approx. 10%) in women than in men. No dose adjustment is required based on gender
Gemifloxacin is rapidly absorbed after oral administration. It is widely distributed throughout the body. Studies in healthy subjects showed that gemifloxacin is distributed rapidly into target tissues and body fluids such as the lung (epithelial lining fluid, alveolar macrophages, bronchial tissue) and nasal secretions.
Following oral administration of gemifloxacin, approximately 36% and 61% of the dose is excreted in the urine and feces, respectively, as unchanged drug and metabolites. AUC values were generally only slightly higher (approx. 10%) in women than in men. No dose adjustment is required based on gender
DosageView
Acute bacterial exacerbation of chronic bronchitis: 320 mg once daily for 5 days.
Community-acquired pneumonia (Mild to moderate severity):
Community-acquired pneumonia (Mild to moderate severity):
- Due to known or suspected S. pneumoniae, H. influenzae, M. pneumoniae, or C. pneumoniae infection: One 320 mg tablet daily for 5 days.
- Due to known or suspected multi-drug resistant Streptococcus pneumoniae, K.pneumoniae, or M. catarrhalis infection: One 320 mg tablet daily for 7 days.
Side effectsView
The general adverse events include abdominal pain, diarrhea, headache, nausea, rash and vomiting. Some side effects have been infrequently reported such as fungal overgrowth in body, dizziness and insomnia, urticaria, pruritis and a maculopapular erythmatous skin rash.
ContraindicationsView
Known hypersensitivity to Gemifloxacin and other quinolones, Patients who have previously suffered tendon damage with fluoroquinolones. Gemifloxacin should not be used in children under 18 years of age.
PrecautionsView
For patients with severe impairment of renal function, alteration of the dosage regimen to 160 mg once daily is necessary. Adequate hydration of patients receiving Gemifloxacin should be maintained to prevent the formation of a highly concentrated urine and crystalluria. Gemifloxacin may cause dizziness; if this occurs, patients should not operate an automobile or machinery or engage in activities requiring mental alertness or co-ordination.
Tendinitis and tendon ruptures may occur in any age group during treatment with quinolones, including Gemifloxacin, but particularly in elderly patients or when corticosteroids are being co-administered. Gemifloxacin should be discontinued if tendinitis is suspected or at the first sign of pain or inflammation and the affected limb should be rested. In clinical studies with Gemifloxacin a small mean increase in QTc interval was observed. Gemifloxacin should be used with caution in patients predisposed to QTc interval prolongation or in patients taking other medications that are known to prolong the QTc interval. Gemifloxacin should be used with caution in patients with epilepsy.
Tendinitis and tendon ruptures may occur in any age group during treatment with quinolones, including Gemifloxacin, but particularly in elderly patients or when corticosteroids are being co-administered. Gemifloxacin should be discontinued if tendinitis is suspected or at the first sign of pain or inflammation and the affected limb should be rested. In clinical studies with Gemifloxacin a small mean increase in QTc interval was observed. Gemifloxacin should be used with caution in patients predisposed to QTc interval prolongation or in patients taking other medications that are known to prolong the QTc interval. Gemifloxacin should be used with caution in patients with epilepsy.
InteractionsView
Gemifloxacin absorption is significantly reduced when aluminium or magnesium containing antacids and iron salts are concomitantly administered. Gemifloxacin should be taken at least 2 hours before or 3 hours after these agents. Gemifloxacin should be taken at least 2 hours before sucralfate administration. No clinically significant interactions have been observed when Gemifloxacin was co-administered with omeprazole theophylline, digoxin, warfarin and oral contraceptives.
Pregnancy & lactationView
Gemifloxacin should not be used in pregnant or lactating women. The safety and efficacy of Gemifloxacin in pregnant or lactating women have not been established.
Pediatric usageView
Renal impairment: Dose adjustment in patients with mild/moderate renal impairment is not required. Some modification of dosage is recommended for patients with severe renal dysfunction. The following table provides dosage guidelines for use in patients with renal impairment:
Elderly patients: Dose adjustment is not required.
- Creatinine Clearance (>40 ml/min): See usual dosage
- Creatinine Clearance (<40 ml/min): 160 mg once daily
- Patients on haemodialysis or continuous ambulatory peritoneal dialysis therapy should receive 160 mg once daily.
Elderly patients: Dose adjustment is not required.
Overdose effectsView
No specific antidote is known. Dialysis does not remove Gemifloxacin sufficiently to be useful in overdose. In the event of acute oral overdosage, the stomach should be emptied by inducing vomiting or by gastric lavage; the patient should be carefully observed, treated symptomatically and adequate hydration should be maintained.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Xemimax
Cefepime Hydrochloride
Xemimax
Cefepime Hydrochloride
Indications
Urinary tract infection
Indication detailsView
Cefepime is indicated for the treatment of the following infections caused by susceptible strains of the microorganisms:
- Pneumonia (moderate to severe): caused by Streptococcus pneumoniae, including cases associated with concurrent bacteremia, Pseudomonas aeruginosa, Klebsiella pneumoniae, or Enterobacter species.
- Febrile Neutropenia: Cefepime as monotherapy is indicated for empiric treatment of febrile neutropenic patients. In patients at high risk for severe infection (including patients with a history of recent bone marrow transplantation, with hypotension at presentation, with an underlying hematologic malignancy, or with severe or prolonged neutropenia), antimicrobial monotherapy may not be appropriate. Insufficient data exist to support the efficacy of cefepime monotherapy in such patients.
- Uncomplicated and Complicated Urinary Tract Infections (including pyelonephritis): caused by Escherichia coli or Klebsiella pneumoniae, when the infection is severe, or caused by Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis, when the infection is mild to moderate, including cases associated with concurrent bacteremia with these microorganisms.
- Uncomplicated Skin and Skin Structure Infections: caused by Staphylococcus aureus (methicillin- susceptible strains only) or Streptococcus pyogenes.
- Complicated Intra-abdominal Infections (used in combination with metronidazole): caused by Escherichia coli, viridians group streptococci, Pseudomonas aeruginosa, Klebsiella pneumoniae, Enterobacter species, or Bacteroides fragilis.
Therapeutic classView
Fourth generation Cephalosporins
PharmacologyView
Cephalosporins are bactericidal and have the same mode of action as other beta-lactam antibiotics (such as penicillins). Cephalosporins disrupt the synthesis of the peptidoglycan layer of bacterial cell walls. The peptidoglycan layer is important for cell wall structural integrity, especially in Gram-positive organisms. The final transpeptidation step in the synthesis of the peptidoglycan is facilitated by transpeptidases known as penicillin binding proteins (PBPs).
DosageView
Cefepime should be administered intravenously over approximately 30 minutes.
*including cases associated with concurrent bacteremia.
**or until resolution of neutropenia. In patients whose fever resolves but who remain neutropenic for more than 7 days, the need for continued antimicrobial therapy should be re evaluated frequently.
*** IM route of administration is indicated only for mild to moderate, uncomplicated or complicated UTls due to E. coli when the IM route is considered to be a more appropriate route of drug administration.
- Moderate to Severe Pneumonia due to S. pneumoniae, *P. aeruginosa, K. pneumoniae, or Enterobacter species: 1-2 gm IV 12 hourly for 10 days.
- Empiric therapy for febrile neutropenic patients: 2 gm IV 8 hourly for 7** days.
- Mild to Moderate Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli, K. pneumoniae, or P. mirabilis*: 0.5-1 gm IV/IM*** 12 hourly for 7-10 days.
- Severe Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli or K. pneumoniae*: 2 gm IV 12 hourly for 10 days.
- Moderate to Severe Uncomplicated Skin and Skin Structure Infections due to S. aureus or S. pyogenes: 2 gm IV 12 hourly for 10 days.
- Complicated Intra-abdominal Infections (used in combination with metronidazole) caused by E. coli, viridans group streptococci, P. aeruginosa, K. pneumoniae, Enterobacter species, or B. fragilis: 2 gm IV 12 hourly for 7-10 days.
*including cases associated with concurrent bacteremia.
**or until resolution of neutropenia. In patients whose fever resolves but who remain neutropenic for more than 7 days, the need for continued antimicrobial therapy should be re evaluated frequently.
*** IM route of administration is indicated only for mild to moderate, uncomplicated or complicated UTls due to E. coli when the IM route is considered to be a more appropriate route of drug administration.
Side effectsView
Cefepime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.
ContraindicationsView
Cefepime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.
PrecautionsView
- Prescribing Cefepime in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
- As with other antimicrobials, prolonged use of Cefepime may result in overgrowth of non susceptible microorganisms. Repeated evaluation of the patient's condition is essential.
- Many cephalosporins, including cefepime, have been associated with a fall in prothrombin activity. Those at risk include patients with renal or hepatic impairment, or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy. Prothrombin time should be monitored in patients at risk.
- Cefepime should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.
- Arginine has been shown to alter glucose metabolism and elevate serum potassium transiently when administered at 33 times the amount provided by the maximum recommended human dose of Cefepime. The effect of lower doses is not presently known.
InteractionsView
Renal function should be monitored carefully if high doses of aminoglycosides are to be administered with Cefepime because of the increased potential of nephrotoxicity and ototoxicity of aminoglycoside antibiotics. Nephrotoxicity has been reported following concomitant administration of other cephalosporins with potent diuretics such as furosemide.
Pregnancy & lactationView
Pregnancy Category B. There are, however, no adequate and well-controlled studies of cefepime use 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. Cefepime is excreted in human breast milk in very low concentrations (0.5 pg/ml). Caution should be exercised when cefepime is administered to a nursing woman.
Pediatric usageView
Pediatric Use (2 months up to 16 years): The maximum dose for pediatric patients should not exceed the recommended adult dose. The usual recommended dosage in pediatric patients up to 40 kg in weight for uncomplicated and complicated urinary tract infections (including pyelonephritis), uncomplicated skin and skin structure infections, and pneumonia is 50 mg/kg/dose, administered every 12 hours (50 mg/kg/dose, every 8 hours for febrile neutropenic patients), for durations as given above.
Geriatric Use: Serious adverse events have occurred in geriatric patients with renal insufficiency given unadjusted doses of cefepime, including life-threatening or fatal occurrences of the following: encephalopathy, myoclonus, and seizures. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and renal function should be monitored.
Impaired Hepatic Function: No adjustment is necessary for patients with impaired hepatic function.
Impaired Renal Function: In patients with impaired renal function (creatinine clearance<60 ml/min), the dose of Cefepime should be adjusted to compensate for the slower rate of renal elimination.
Geriatric Use: Serious adverse events have occurred in geriatric patients with renal insufficiency given unadjusted doses of cefepime, including life-threatening or fatal occurrences of the following: encephalopathy, myoclonus, and seizures. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and renal function should be monitored.
Impaired Hepatic Function: No adjustment is necessary for patients with impaired hepatic function.
Impaired Renal Function: In patients with impaired renal function (creatinine clearance<60 ml/min), the dose of Cefepime should be adjusted to compensate for the slower rate of renal elimination.
Overdose effectsView
Patients who receive an overdose should be carefully observed and given supportive treatment. In the presence of renal insufficiency, hemodialysis, not peritoneal dialysis, is recommended to aid the removal of cefepime from the body. Accidental overdosing has occurred when large doses were given to patients with impaired renal function. Symptoms of overdose include encephalopathy (disturbance of consciousness including confusion, hallucinations, stupor, and coma), myoclonus, seizures, and neuromuscular excitability.
ReconstitutionView
For IV the resulting solution should be injected directly into the vein over a period of three to five minutes or injected into the tubing of an administration set while the patient is receiving a compatible IV fluid.
Intravenous: Cefepime is compatible with Sterile Water for Injection. It is also compatible at concentrations between 1 mg/ml and 40 mg/ml with the following IV infusion fluids: 0.9% Sodium Chloride Injection, 5% and 10% Dextrose Injection, M/6 Sodium Lactate Injection, 5% Dextrose and 0.9% Sodium Chloride Injection, Lactated Ringers and 5% Dextrose Injection.
Intramuscular: Cefepime is compatible with the following diluent such as: Sterile Water for Injection, 0.9% Sodium Chloride Injection, 5% Dextrose Injection, Sterile Bacteriostatic Water for Injection with Parabens or Benzyl Alcohol or 0.5% or 1% Lidocaine Hydrochloride.
500 mg (IV) vials for intravenous administration:
Intravenous: Cefepime is compatible with Sterile Water for Injection. It is also compatible at concentrations between 1 mg/ml and 40 mg/ml with the following IV infusion fluids: 0.9% Sodium Chloride Injection, 5% and 10% Dextrose Injection, M/6 Sodium Lactate Injection, 5% Dextrose and 0.9% Sodium Chloride Injection, Lactated Ringers and 5% Dextrose Injection.
Intramuscular: Cefepime is compatible with the following diluent such as: Sterile Water for Injection, 0.9% Sodium Chloride Injection, 5% Dextrose Injection, Sterile Bacteriostatic Water for Injection with Parabens or Benzyl Alcohol or 0.5% or 1% Lidocaine Hydrochloride.
500 mg (IV) vials for intravenous administration:
- Amount of WFI to be added: 5 ml
- Approximate available volume: 5.6 ml
- Amount of WFI to be added: 1.3 ml
- Approximate available volume: 1.8 ml
- Amount of WFI to be added: 10 ml
- Approximate available volume: 11.3 ml
- Amount of WFI to be added: 2.4 ml
- Approximate available volume: 3.6 ml
- Amount of WFI to be added: 10 ml
- Approximate available volume: 12.5 ml
StorageView
Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician.
Xemimax
Cefepime Hydrochloride
Xemimax
Cefepime Hydrochloride
Indications
Urinary tract infection
Indication detailsView
Cefepime is indicated for the treatment of the following infections caused by susceptible strains of the microorganisms:
- Pneumonia (moderate to severe): caused by Streptococcus pneumoniae, including cases associated with concurrent bacteremia, Pseudomonas aeruginosa, Klebsiella pneumoniae, or Enterobacter species.
- Febrile Neutropenia: Cefepime as monotherapy is indicated for empiric treatment of febrile neutropenic patients. In patients at high risk for severe infection (including patients with a history of recent bone marrow transplantation, with hypotension at presentation, with an underlying hematologic malignancy, or with severe or prolonged neutropenia), antimicrobial monotherapy may not be appropriate. Insufficient data exist to support the efficacy of cefepime monotherapy in such patients.
- Uncomplicated and Complicated Urinary Tract Infections (including pyelonephritis): caused by Escherichia coli or Klebsiella pneumoniae, when the infection is severe, or caused by Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis, when the infection is mild to moderate, including cases associated with concurrent bacteremia with these microorganisms.
- Uncomplicated Skin and Skin Structure Infections: caused by Staphylococcus aureus (methicillin- susceptible strains only) or Streptococcus pyogenes.
- Complicated Intra-abdominal Infections (used in combination with metronidazole): caused by Escherichia coli, viridians group streptococci, Pseudomonas aeruginosa, Klebsiella pneumoniae, Enterobacter species, or Bacteroides fragilis.
Therapeutic classView
Fourth generation Cephalosporins
PharmacologyView
Cephalosporins are bactericidal and have the same mode of action as other beta-lactam antibiotics (such as penicillins). Cephalosporins disrupt the synthesis of the peptidoglycan layer of bacterial cell walls. The peptidoglycan layer is important for cell wall structural integrity, especially in Gram-positive organisms. The final transpeptidation step in the synthesis of the peptidoglycan is facilitated by transpeptidases known as penicillin binding proteins (PBPs).
DosageView
Cefepime should be administered intravenously over approximately 30 minutes.
*including cases associated with concurrent bacteremia.
**or until resolution of neutropenia. In patients whose fever resolves but who remain neutropenic for more than 7 days, the need for continued antimicrobial therapy should be re evaluated frequently.
*** IM route of administration is indicated only for mild to moderate, uncomplicated or complicated UTls due to E. coli when the IM route is considered to be a more appropriate route of drug administration.
- Moderate to Severe Pneumonia due to S. pneumoniae, *P. aeruginosa, K. pneumoniae, or Enterobacter species: 1-2 gm IV 12 hourly for 10 days.
- Empiric therapy for febrile neutropenic patients: 2 gm IV 8 hourly for 7** days.
- Mild to Moderate Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli, K. pneumoniae, or P. mirabilis*: 0.5-1 gm IV/IM*** 12 hourly for 7-10 days.
- Severe Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli or K. pneumoniae*: 2 gm IV 12 hourly for 10 days.
- Moderate to Severe Uncomplicated Skin and Skin Structure Infections due to S. aureus or S. pyogenes: 2 gm IV 12 hourly for 10 days.
- Complicated Intra-abdominal Infections (used in combination with metronidazole) caused by E. coli, viridans group streptococci, P. aeruginosa, K. pneumoniae, Enterobacter species, or B. fragilis: 2 gm IV 12 hourly for 7-10 days.
*including cases associated with concurrent bacteremia.
**or until resolution of neutropenia. In patients whose fever resolves but who remain neutropenic for more than 7 days, the need for continued antimicrobial therapy should be re evaluated frequently.
*** IM route of administration is indicated only for mild to moderate, uncomplicated or complicated UTls due to E. coli when the IM route is considered to be a more appropriate route of drug administration.
Side effectsView
Cefepime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.
ContraindicationsView
Cefepime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.
PrecautionsView
- Prescribing Cefepime in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
- As with other antimicrobials, prolonged use of Cefepime may result in overgrowth of non susceptible microorganisms. Repeated evaluation of the patient's condition is essential.
- Many cephalosporins, including cefepime, have been associated with a fall in prothrombin activity. Those at risk include patients with renal or hepatic impairment, or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy. Prothrombin time should be monitored in patients at risk.
- Cefepime should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.
- Arginine has been shown to alter glucose metabolism and elevate serum potassium transiently when administered at 33 times the amount provided by the maximum recommended human dose of Cefepime. The effect of lower doses is not presently known.
InteractionsView
Renal function should be monitored carefully if high doses of aminoglycosides are to be administered with Cefepime because of the increased potential of nephrotoxicity and ototoxicity of aminoglycoside antibiotics. Nephrotoxicity has been reported following concomitant administration of other cephalosporins with potent diuretics such as furosemide.
Pregnancy & lactationView
Pregnancy Category B. There are, however, no adequate and well-controlled studies of cefepime use 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. Cefepime is excreted in human breast milk in very low concentrations (0.5 pg/ml). Caution should be exercised when cefepime is administered to a nursing woman.
Pediatric usageView
Pediatric Use (2 months up to 16 years): The maximum dose for pediatric patients should not exceed the recommended adult dose. The usual recommended dosage in pediatric patients up to 40 kg in weight for uncomplicated and complicated urinary tract infections (including pyelonephritis), uncomplicated skin and skin structure infections, and pneumonia is 50 mg/kg/dose, administered every 12 hours (50 mg/kg/dose, every 8 hours for febrile neutropenic patients), for durations as given above.
Geriatric Use: Serious adverse events have occurred in geriatric patients with renal insufficiency given unadjusted doses of cefepime, including life-threatening or fatal occurrences of the following: encephalopathy, myoclonus, and seizures. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and renal function should be monitored.
Impaired Hepatic Function: No adjustment is necessary for patients with impaired hepatic function.
Impaired Renal Function: In patients with impaired renal function (creatinine clearance<60 ml/min), the dose of Cefepime should be adjusted to compensate for the slower rate of renal elimination.
Geriatric Use: Serious adverse events have occurred in geriatric patients with renal insufficiency given unadjusted doses of cefepime, including life-threatening or fatal occurrences of the following: encephalopathy, myoclonus, and seizures. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and renal function should be monitored.
Impaired Hepatic Function: No adjustment is necessary for patients with impaired hepatic function.
Impaired Renal Function: In patients with impaired renal function (creatinine clearance<60 ml/min), the dose of Cefepime should be adjusted to compensate for the slower rate of renal elimination.
Overdose effectsView
Patients who receive an overdose should be carefully observed and given supportive treatment. In the presence of renal insufficiency, hemodialysis, not peritoneal dialysis, is recommended to aid the removal of cefepime from the body. Accidental overdosing has occurred when large doses were given to patients with impaired renal function. Symptoms of overdose include encephalopathy (disturbance of consciousness including confusion, hallucinations, stupor, and coma), myoclonus, seizures, and neuromuscular excitability.
ReconstitutionView
For IV the resulting solution should be injected directly into the vein over a period of three to five minutes or injected into the tubing of an administration set while the patient is receiving a compatible IV fluid.
Intravenous: Cefepime is compatible with Sterile Water for Injection. It is also compatible at concentrations between 1 mg/ml and 40 mg/ml with the following IV infusion fluids: 0.9% Sodium Chloride Injection, 5% and 10% Dextrose Injection, M/6 Sodium Lactate Injection, 5% Dextrose and 0.9% Sodium Chloride Injection, Lactated Ringers and 5% Dextrose Injection.
Intramuscular: Cefepime is compatible with the following diluent such as: Sterile Water for Injection, 0.9% Sodium Chloride Injection, 5% Dextrose Injection, Sterile Bacteriostatic Water for Injection with Parabens or Benzyl Alcohol or 0.5% or 1% Lidocaine Hydrochloride.
500 mg (IV) vials for intravenous administration:
Intravenous: Cefepime is compatible with Sterile Water for Injection. It is also compatible at concentrations between 1 mg/ml and 40 mg/ml with the following IV infusion fluids: 0.9% Sodium Chloride Injection, 5% and 10% Dextrose Injection, M/6 Sodium Lactate Injection, 5% Dextrose and 0.9% Sodium Chloride Injection, Lactated Ringers and 5% Dextrose Injection.
Intramuscular: Cefepime is compatible with the following diluent such as: Sterile Water for Injection, 0.9% Sodium Chloride Injection, 5% Dextrose Injection, Sterile Bacteriostatic Water for Injection with Parabens or Benzyl Alcohol or 0.5% or 1% Lidocaine Hydrochloride.
500 mg (IV) vials for intravenous administration:
- Amount of WFI to be added: 5 ml
- Approximate available volume: 5.6 ml
- Amount of WFI to be added: 1.3 ml
- Approximate available volume: 1.8 ml
- Amount of WFI to be added: 10 ml
- Approximate available volume: 11.3 ml
- Amount of WFI to be added: 2.4 ml
- Approximate available volume: 3.6 ml
- Amount of WFI to be added: 10 ml
- Approximate available volume: 12.5 ml
StorageView
Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician.
Xemocid
Amino Acid + D-Sorbitol + Electrolytes
Xemocid
Amino Acid + D-Sorbitol + Electrolytes
Indications
Protein supply for peritoneal nutrition
Indication detailsView
Amino acid is indicated as a source of amino acids for protein synthesis in patients needing intravenous nutrition. Amino acid is particularly suitable for patients with basal amino acid requirements. Amino acid is also indicated in faster recovery in surgery, burns, renal insufficiency, hepatic insufficiency and effective management of cancer.
Therapeutic classView
Parenteral nutritional preparations
PharmacologyView
This IV solution is a sterile aqueous solution of crystalline Amino Acid and D-Sorbitol with electrolytes, which are necessary as the nitrogen source for parenteral nutrition. Nitrogen provided in the form of essential and non-essential amino acids. This IV solution contains all 18 essential and non-essential amino acids needed for protein synthesis. The amino acid composition is such that positive nitrogen balance can be achieved in the postoperative period and during extended periods of intravenous nutrition. The solution is clear, colorless to pale yellow colored, having a p H lying in the range of 5.0 to 7.0.
DosageView
The nitrogen requirement for maintenance of body protein mass depends on the patient's condition (nutritional state and degree of metabolic stress).
In obese patients, the dose should be based on the estimated ideal weight. Depending upon patients requirements, 1000-2000 ml Amino acids IV may be infused intravenously per 24 hours. Amino acids IV should be infused slowly, at rates 1.4-2.8 ml (30-60 drops) per minute.
In children and infants: The rate of infusion is 28-35 ml/kg body weight per day is recommended, with a step-wise increase in the rate of administration during the frst week.
- No or minor metabolic stress and normal nutritional state: 0.10-0.15 g nitrogen/kg/day,
- Moderate metabolic stress with or without malnutrition: 0.15-0.20 g nitrogen/kg/day,
- Severe catabolism as in burns, sepsis and trauma: up to 0.20-0.25 g nitrogen/kg/day.
In obese patients, the dose should be based on the estimated ideal weight. Depending upon patients requirements, 1000-2000 ml Amino acids IV may be infused intravenously per 24 hours. Amino acids IV should be infused slowly, at rates 1.4-2.8 ml (30-60 drops) per minute.
In children and infants: The rate of infusion is 28-35 ml/kg body weight per day is recommended, with a step-wise increase in the rate of administration during the frst week.
Side effectsView
This preparation is usually well tolerated. Nausea occurs rarely. Vomiting, flushing and sweating have been observed during infusion of Amino acid at rates exceeding the recommended maximal rate. Transient increases liver test during intravenous nutrition have been reported. The reasons are at present unclear. Hypersensitivity reactions have been reported. As with all hypertonic infusion solutions, thrombophlebitis may occur when peripheral veins are used. The incidence may be reduced by the simultaneous infusion of 10% fat emulsion. If given to severely ill, premature infants, hyperphenylalaninemia may occur.
ContraindicationsView
This is contraindicated in patients with inborn errors of amino acids metabolism, severe liver dysfunction and in severe uremia when dialysis facilities are not available. Due to the content of glucose, Amino Acids IV infusion and 10% Glucose with Electrolytes is contraindicated in patients with hyperosmolar nonketotic diabetic coma.
PrecautionsView
IV infusion of amino acids is accompanied by increased urinary excretion of the trace elements copper and in particular zinc, which should be taken into account in the dosing of trace elements, particularly during long-term IV nutrition. Hyperphenylalaninemia may occur in severely ill, premature infants. In these patients, monitoring of the phenylalanine level is recommended and the infusion rate adjusted as needed. Amino Acids IV infusion and 10% Glucose with Electrolytes should be used with caution in patients with diabetes mellitus, severe heart failure or with renal function in combination with fluid restrictions or oliguria/anuria of another origin. In patients with hyperglycemia, administration of exogenous insulin might be necessary. In severely malnourished patients refeeding carbohydrates can trigger thiamine (vitamin B1 ) deficiency syndrome. Those at high risk are patients with a history of alcohol abuse, anorexia nervosa, prolonged fasting or starvation and pregnant women with hyperemesis gravidarum. In this kind of patients, parenteral nutrition containing glucose should be given with caution and parenteral administration of thiamine should be considered before and during the administration of glucose. Monitoring of serum potassium and blood glucose is recommended if Amino Acids IV infusion and 10% Glucose with electrolytes is infused rapidly or in a large quantity. For patients with hypophosphatemia, an additional supply of phosphate is recommended.
InteractionsView
At the recommended dosage the amino acid have no pharmacological effects and is not expected to interact with other medicaments.
Pregnancy & lactationView
Successful and safe administration of amino acid solutions during pregnancy in the human has been reported. Animal reproduction studies have not been carried out with Amino acid.
Overdose effectsView
If Amino Acids IV infusion and 10% Glucose with Electrolytes is administered at a higher rate than recommended, there is an augmented risk for nausea, vomiting and sweating. When peripheral veins are used thrombophlebitis may occur. Osmotic diuresis with dehydration may occur if the dosage recommendations are exceeded. There is also a risk of symptoms related to hyperglycemia with Amino Acids IV infusion and 10% Glucose with Electrolytes. In case of symptoms due to overdose, the infusion should be slowed down or discontinued.
StorageView
Protect from light and store between 15°C to 25°C temperature. Avoid freezing. Keep out of reach of children.
Xemocid Gold
Amino Acid + Glucose + Electrolytes
Xemocid Gold
Amino Acid + Glucose + Electrolytes
Indications
Prevent nitrogen loss
Indication detailsView
This is indicated as a source of amino acids, glucose and electrolytes in adult and pediatric patients needing IV nutrition. This is particularly suitable for patients with basal amino acid requirements.
Therapeutic classView
Parenteral nutritional preparations
PharmacologyView
A crystalline amino acid solution provides crystalline amino acids to promote protein synthesis and wound healing, and to reduce the rate of endogenous protein catabolism. Amino Acids given by central venous infusion in combination with concentrated dextrose, electrolytes, vitamins, trace metals, and ancillary fat supplements, constitutes total parenteral nutrition (TPN). Amino Acids can also be administered by peripheral vein with dextrose and maintenance electrolytes.
DosageView
Adults: The nitrogen requirement for maintenance of body protein mass depends on the patient's condition (nutritional state and degree of metabolic stress). The requirements are 0.10-0.15g nitrogen/kg/day (no or minor metabolic stress and normal nutritional state), 0.15-0.20g nitrogen/kg/day (moderate metabolic stress with or without malnutrition) and up to 0.20-0.25g nitrogen/kg/day (severe catabolism as in burns, sepsis and trauma). The dosage range is 0.10-0.25 g nitrogen/kg/day corresponds to 11-27 ml/kg/day. In obese patients, the dose should be based on the estimated ideal weight. Depending upon the patient’s requirements, 1000-2000 ml may be infused intravenously per 24 hours. This should be infused slowly; at a rate not exceeding 500 ml in 3 hours corresponding to approximately at rates 1.4-2.8 ml (30-60 drops) per minute.
Infants and children: In infants & children, a maximal rate of infusion of 30 ml/kg body weight/day is recommended, with a step-wise increase in the rate of administration during the first week of treatment.
Infants and children: In infants & children, a maximal rate of infusion of 30 ml/kg body weight/day is recommended, with a step-wise increase in the rate of administration during the first week of treatment.
Side effectsView
This preparation is usually well tolerated. Nausea occurs rarely. Vomiting, flushing and sweating have been observed during infusion of the solution at rates exceeding the recommended maximal rate. Transient increases in liver test during intravenous nutrition have been reported. The reasons are at present unclear. The underlying disease and the components and their amount in the intravenous feeding regimens have been suggested. Hypersensitivity reactions have been reported. As with all hypertonic infusion solution, thrombophlebitis may occur when peripheral veins are used. The incidence may be reduced by the simultaneous infusion of 10% fat emulsion.
ContraindicationsView
This preparation is contraindicated in patients with inborn errors of amino acids metabolism, severe liver damage & severe uremia when dialysis facilities are not available. Due to the content of the glucose, this preparation is contraindicated in patients with hyperosmolar nonketotic diabetic coma. This preparation is also contraindicated in patients with known hypersensitivity to any of its ingredients.
PrecautionsView
Hyperphenylalaninemia has been noted in severely ill, premature infants. In these patients, monitoring of the phenylalanine level is recommended and the infusion rate to be adjusted as needed. This preparation should be used with caution in patients with diabetes mellitus, severe heart failure or with renal function in combination with fluid restriction or oliguria/anuria of other origin. In patient with hyperglycemia, administration of exogenous insulin might be necessary. Do not use if the solution is turbid or contains particles. Discard any unused portion.
InteractionsView
At the recommended dosage this solution has no pharmacological effect and is expected not to interact with other medicaments.
Pregnancy & lactationView
Successful and safe administration of amino acid solution during pregnancy in human has been reported. Animal reproduction studies have not been carried out with 7% amino acid IV infusion with 10% glucose & electrolytes.
StorageView
Protect from light and store between 15°C to 25°C temperature. Avoid freezing. Keep away from the reach of children.
Xenapro
Naproxen Sodium
Xenapro
Naproxen Sodium
Indications
Systemic lupus erythematosus (SLE)
Indication detailsView
Naproxen is indicated for the relief of sign and symptoms of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, juvenile arthritis, tendonitis, bursitis & acute gout. It is also indicated for the management of primary dysmenorrhea & pain.
Therapeutic classView
Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
PharmacologyView
Naproxen is a non steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic & antipyretic properties. It is rapidly absorbed from the gastrointestinal tract and achieves 95% bioavailability.
DosageView
Naproxen Tablet-
- Rheumatoid arthritis, osteoarthritis and ankylosing spondylitis: The usual dose is 500-1000 mg daily in two divided doses after meals.
- Management of pain, primary dysmenorrhea, acute tendonitis & bursitis: Recommended starting dose is 500 mg followed by 500 mg every 12 hours or 250 mg every 6-8 hours. The initial total daily dose should not exceed 1250 mg and thereafter, the total daily dose should not exceed 1000 mg.
- Acute gout: Recommended starting dose is 750 mg followed by 250 mg every 8 hours until the attack has subsided.
- For Juvenile rheumatoid arthritis: The usual dose for children over 2 years is 10 mg/kg/day given as two divided doses at 12-hours intervals. Therapy in children under 2 years of age is not recommended.
- Is to be applied 2-6 times a day as required and is not recommended for use in children.
Side effectsView
Most frequently reported side effects include following:
- Gastrointestinal: Heartburn, abdominal pain, nausea, diarrhea, dyspepsia.
- Central Nervous System: Headache, vertigo, drowsiness.
- Dermatological: Pruritus (itching), purpura.
- Cardiovascular: Edema, palpitation.
- Others: Visual disturbances, hearing disturbances.
ContraindicationsView
Naproxen is contraindicated in patients with known hypersensitivity to Naproxen. It should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. It is contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
InteractionsView
ACE inhibitors: diminish the antihypertensive effect of ACE inhibitors.
Antacids & Sucralfate: delay the absorption of Naproxen.
Aspirin: increase adverse effects.
Diuretics: reduce the natriuretic effect of Furosemide and Thiazides.
Methotrexate: enhance the toxicity of Methotrexate.
Warfarin: increase the risk of GI bleeding.
Selective Serotonin Reuptake Inhibitors (SSRI): increase the risk of GI bleeding.
Antacids & Sucralfate: delay the absorption of Naproxen.
Aspirin: increase adverse effects.
Diuretics: reduce the natriuretic effect of Furosemide and Thiazides.
Methotrexate: enhance the toxicity of Methotrexate.
Warfarin: increase the risk of GI bleeding.
Selective Serotonin Reuptake Inhibitors (SSRI): increase the risk of GI bleeding.
Pregnancy & lactationView
US FDA pregnancy category of Naproxen is C. So, Naproxen should be avoided in pregnancy & lactation unless the potential benefits to the other outweigh the possible risks to the fetus.
StorageView
Keep below 30°C temperature, protected from light & moisture. Keep out of the reach of children.
Xenapro Plus
Naproxen Sodium + Esomeprazole Magnesium
Xenapro Plus
Naproxen Sodium + Esomeprazole Magnesium
Indications
Systemic lupus erythematosus (SLE)
Indication detailsView
Naproxen & Esomeprazole is indicated for the relief of signs & symptoms of-
- Osteoarthritis
- Rheumatoid arthritis
- Ankylosing spondylitis &
- To decrease the risk of developing gastric ulcers in patients at risk of developing NSAID-associated gastric ulcers.
Therapeutic classView
Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
PharmacologyView
This consists of an immediate release Esomeprazole Magnesium layer & an enteric-coated Naproxen core. As a result, Esomeprazole is released first into the stomach, prior to the dissolution of Naproxen in the small intestine.
Naproxen is a NSAID with analgesic & antipyretic properties. The mechanism of action of Naproxen is to inhibit the prostaglandin synthesis. Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/k+ -ATPase in the gastric parietal cell by acting specifically on the proton pump, Esomeprazole blocks the final step in acid production, thus reducing gastric acidity.
Naproxen is a NSAID with analgesic & antipyretic properties. The mechanism of action of Naproxen is to inhibit the prostaglandin synthesis. Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/k+ -ATPase in the gastric parietal cell by acting specifically on the proton pump, Esomeprazole blocks the final step in acid production, thus reducing gastric acidity.
DosageView
Carefully consider the potential benefits & risks of this tablet & other treatment options before deciding to use this tablet. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals. If a dose of Esomeprazole lower than a total daily dose of 40 mg is more appropriate, a different treatment should be considered.
Rheumatoid Arthritis, Osteoarthritis and Ankylosing Spondylitis-
Rheumatoid Arthritis, Osteoarthritis and Ankylosing Spondylitis-
- Adults: One tablet twice daily of either: 375 mg naproxen/20 mg of esomeprazole; or 500 mg naproxen/20 mg of esomeprazole
- Weight greater than 50 kg: 375 mg naproxen/20 mg of esomeprazole; or 500 mg naproxen/20 mg of esomeprazole
- Weight 38 kg to less than 50 kg: One tablet twice daily of 375 mg naproxen/20 mg of esomeprazole.
AdministrationView
Do not split, chew, crush or dissolve the tablet. This tablet is to be taken at least 30 minutes before meals.
Side effectsView
In general, this preparation is well tolerated. The most common adverse reactions in clinical trials (>5%): erosive gastritis, dyspepsia, gastritis, diarrhea, gastric ulcer, upper abdominal pain, nausea etc.
ContraindicationsView
- Known hypersensitivity to any component of this tablet or substituted benzimidazoles.
- History of asthmay urticaria or other allergic-type reactions after taking aspirin or other NSAIDs.
- Use during the peri-operative period in the setting of coronary artery bypass graft (CABG) surgery.
PrecautionsView
Patients with known CV disease/risk factors may be at greater risk. This tablet should be used with caution in patients with fluid retention or heart failure.
InteractionsView
With medicine:
- Concomitant use of NSAIDs may reduce the antihypertensive effect of ACE inhibitors, diuretics & beta-blockers
- Concomitant use of this tablet and warfarin may result in an increased risk of a bleeding complication.
- Esomeprazole inhibits gastric acid secretion & may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (eg. Ketoconazole, iron salts and digoxin).
Pregnancy & lactationView
Pregnancy category C. In late pregnancy, it should be avoided because it may cause premature closure of the ductus arteriosus. This tablet should not be used in nursing mothers due to the Naproxen component.
Pediatric usageView
Elderly patients: Studies indicate that although the total plasma concentration of naproxen is unchanged, the unbound plasma fraction of naproxen is increased in the elderly. Use caution when high doses are required & some adjustment of dosage may be required in elderly patients. As with other drugs used in the elderly use the lowest effective dose.
Patients with Moderate to Severe Renal impairment: Naproxen-containing products are not recommended for use in patients with moderate to severe or severe renal impairment (creatinine clearance <30 ml/min).
Hepatic insufficiency: Monitor patients with mild to moderate hepatic impairment closely & consider a possible dose reduction based on the Naproxen component of this tablet. This is not recommended in patients with severe hepatic impairment because Esomeprazole dosage should not exceed 20 mg daily in these patients.
Patients with Moderate to Severe Renal impairment: Naproxen-containing products are not recommended for use in patients with moderate to severe or severe renal impairment (creatinine clearance <30 ml/min).
Hepatic insufficiency: Monitor patients with mild to moderate hepatic impairment closely & consider a possible dose reduction based on the Naproxen component of this tablet. This is not recommended in patients with severe hepatic impairment because Esomeprazole dosage should not exceed 20 mg daily in these patients.
Overdose effectsView
There is no clinical data on overdosage with this tablet.
Overdose of Naproxen: Significant naproxen overdosage may be characterized by lethargy, drowsiness, epigastric pain, abdominal discomfort, heartburn, indigestion, nausea, transient alteration in liver function, hypoprothrombinemia, renal dysfunction, metabolic acidosis, apnea, vomiting etc.
Overdose of Esomeprazole: The major signs of acute toxicity were reduced motor activity, changes in respiratory frequency, tremor and intermittent clonic convulsions etc.
Overdose of Naproxen: Significant naproxen overdosage may be characterized by lethargy, drowsiness, epigastric pain, abdominal discomfort, heartburn, indigestion, nausea, transient alteration in liver function, hypoprothrombinemia, renal dysfunction, metabolic acidosis, apnea, vomiting etc.
Overdose of Esomeprazole: The major signs of acute toxicity were reduced motor activity, changes in respiratory frequency, tremor and intermittent clonic convulsions etc.
StorageView
Store at temperature of below 30°C, protect from light & moisture. Keep out of reach of children.
Xenapro Plus
Naproxen Sodium + Esomeprazole Magnesium
Xenapro Plus
Naproxen Sodium + Esomeprazole Magnesium
Indications
Systemic lupus erythematosus (SLE)
Indication detailsView
Naproxen & Esomeprazole is indicated for the relief of signs & symptoms of-
- Osteoarthritis
- Rheumatoid arthritis
- Ankylosing spondylitis &
- To decrease the risk of developing gastric ulcers in patients at risk of developing NSAID-associated gastric ulcers.
Therapeutic classView
Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
PharmacologyView
This consists of an immediate release Esomeprazole Magnesium layer & an enteric-coated Naproxen core. As a result, Esomeprazole is released first into the stomach, prior to the dissolution of Naproxen in the small intestine.
Naproxen is a NSAID with analgesic & antipyretic properties. The mechanism of action of Naproxen is to inhibit the prostaglandin synthesis. Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/k+ -ATPase in the gastric parietal cell by acting specifically on the proton pump, Esomeprazole blocks the final step in acid production, thus reducing gastric acidity.
Naproxen is a NSAID with analgesic & antipyretic properties. The mechanism of action of Naproxen is to inhibit the prostaglandin synthesis. Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/k+ -ATPase in the gastric parietal cell by acting specifically on the proton pump, Esomeprazole blocks the final step in acid production, thus reducing gastric acidity.
DosageView
Carefully consider the potential benefits & risks of this tablet & other treatment options before deciding to use this tablet. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals. If a dose of Esomeprazole lower than a total daily dose of 40 mg is more appropriate, a different treatment should be considered.
Rheumatoid Arthritis, Osteoarthritis and Ankylosing Spondylitis-
Rheumatoid Arthritis, Osteoarthritis and Ankylosing Spondylitis-
- Adults: One tablet twice daily of either: 375 mg naproxen/20 mg of esomeprazole; or 500 mg naproxen/20 mg of esomeprazole
- Weight greater than 50 kg: 375 mg naproxen/20 mg of esomeprazole; or 500 mg naproxen/20 mg of esomeprazole
- Weight 38 kg to less than 50 kg: One tablet twice daily of 375 mg naproxen/20 mg of esomeprazole.
AdministrationView
Do not split, chew, crush or dissolve the tablet. This tablet is to be taken at least 30 minutes before meals.
Side effectsView
In general, this preparation is well tolerated. The most common adverse reactions in clinical trials (>5%): erosive gastritis, dyspepsia, gastritis, diarrhea, gastric ulcer, upper abdominal pain, nausea etc.
ContraindicationsView
- Known hypersensitivity to any component of this tablet or substituted benzimidazoles.
- History of asthmay urticaria or other allergic-type reactions after taking aspirin or other NSAIDs.
- Use during the peri-operative period in the setting of coronary artery bypass graft (CABG) surgery.
PrecautionsView
Patients with known CV disease/risk factors may be at greater risk. This tablet should be used with caution in patients with fluid retention or heart failure.
InteractionsView
With medicine:
- Concomitant use of NSAIDs may reduce the antihypertensive effect of ACE inhibitors, diuretics & beta-blockers
- Concomitant use of this tablet and warfarin may result in an increased risk of a bleeding complication.
- Esomeprazole inhibits gastric acid secretion & may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (eg. Ketoconazole, iron salts and digoxin).
Pregnancy & lactationView
Pregnancy category C. In late pregnancy, it should be avoided because it may cause premature closure of the ductus arteriosus. This tablet should not be used in nursing mothers due to the Naproxen component.
Pediatric usageView
Elderly patients: Studies indicate that although the total plasma concentration of naproxen is unchanged, the unbound plasma fraction of naproxen is increased in the elderly. Use caution when high doses are required & some adjustment of dosage may be required in elderly patients. As with other drugs used in the elderly use the lowest effective dose.
Patients with Moderate to Severe Renal impairment: Naproxen-containing products are not recommended for use in patients with moderate to severe or severe renal impairment (creatinine clearance <30 ml/min).
Hepatic insufficiency: Monitor patients with mild to moderate hepatic impairment closely & consider a possible dose reduction based on the Naproxen component of this tablet. This is not recommended in patients with severe hepatic impairment because Esomeprazole dosage should not exceed 20 mg daily in these patients.
Patients with Moderate to Severe Renal impairment: Naproxen-containing products are not recommended for use in patients with moderate to severe or severe renal impairment (creatinine clearance <30 ml/min).
Hepatic insufficiency: Monitor patients with mild to moderate hepatic impairment closely & consider a possible dose reduction based on the Naproxen component of this tablet. This is not recommended in patients with severe hepatic impairment because Esomeprazole dosage should not exceed 20 mg daily in these patients.
Overdose effectsView
There is no clinical data on overdosage with this tablet.
Overdose of Naproxen: Significant naproxen overdosage may be characterized by lethargy, drowsiness, epigastric pain, abdominal discomfort, heartburn, indigestion, nausea, transient alteration in liver function, hypoprothrombinemia, renal dysfunction, metabolic acidosis, apnea, vomiting etc.
Overdose of Esomeprazole: The major signs of acute toxicity were reduced motor activity, changes in respiratory frequency, tremor and intermittent clonic convulsions etc.
Overdose of Naproxen: Significant naproxen overdosage may be characterized by lethargy, drowsiness, epigastric pain, abdominal discomfort, heartburn, indigestion, nausea, transient alteration in liver function, hypoprothrombinemia, renal dysfunction, metabolic acidosis, apnea, vomiting etc.
Overdose of Esomeprazole: The major signs of acute toxicity were reduced motor activity, changes in respiratory frequency, tremor and intermittent clonic convulsions etc.
StorageView
Store at temperature of below 30°C, protect from light & moisture. Keep out of reach of children.
Xenim
Cefepime Hydrochloride
Xenim
Cefepime Hydrochloride
Indications
Urinary tract infection
Indication detailsView
Cefepime is indicated for the treatment of the following infections caused by susceptible strains of the microorganisms:
- Pneumonia (moderate to severe): caused by Streptococcus pneumoniae, including cases associated with concurrent bacteremia, Pseudomonas aeruginosa, Klebsiella pneumoniae, or Enterobacter species.
- Febrile Neutropenia: Cefepime as monotherapy is indicated for empiric treatment of febrile neutropenic patients. In patients at high risk for severe infection (including patients with a history of recent bone marrow transplantation, with hypotension at presentation, with an underlying hematologic malignancy, or with severe or prolonged neutropenia), antimicrobial monotherapy may not be appropriate. Insufficient data exist to support the efficacy of cefepime monotherapy in such patients.
- Uncomplicated and Complicated Urinary Tract Infections (including pyelonephritis): caused by Escherichia coli or Klebsiella pneumoniae, when the infection is severe, or caused by Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis, when the infection is mild to moderate, including cases associated with concurrent bacteremia with these microorganisms.
- Uncomplicated Skin and Skin Structure Infections: caused by Staphylococcus aureus (methicillin- susceptible strains only) or Streptococcus pyogenes.
- Complicated Intra-abdominal Infections (used in combination with metronidazole): caused by Escherichia coli, viridians group streptococci, Pseudomonas aeruginosa, Klebsiella pneumoniae, Enterobacter species, or Bacteroides fragilis.
Therapeutic classView
Fourth generation Cephalosporins
PharmacologyView
Cephalosporins are bactericidal and have the same mode of action as other beta-lactam antibiotics (such as penicillins). Cephalosporins disrupt the synthesis of the peptidoglycan layer of bacterial cell walls. The peptidoglycan layer is important for cell wall structural integrity, especially in Gram-positive organisms. The final transpeptidation step in the synthesis of the peptidoglycan is facilitated by transpeptidases known as penicillin binding proteins (PBPs).
DosageView
Cefepime should be administered intravenously over approximately 30 minutes.
*including cases associated with concurrent bacteremia.
**or until resolution of neutropenia. In patients whose fever resolves but who remain neutropenic for more than 7 days, the need for continued antimicrobial therapy should be re evaluated frequently.
*** IM route of administration is indicated only for mild to moderate, uncomplicated or complicated UTls due to E. coli when the IM route is considered to be a more appropriate route of drug administration.
- Moderate to Severe Pneumonia due to S. pneumoniae, *P. aeruginosa, K. pneumoniae, or Enterobacter species: 1-2 gm IV 12 hourly for 10 days.
- Empiric therapy for febrile neutropenic patients: 2 gm IV 8 hourly for 7** days.
- Mild to Moderate Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli, K. pneumoniae, or P. mirabilis*: 0.5-1 gm IV/IM*** 12 hourly for 7-10 days.
- Severe Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli or K. pneumoniae*: 2 gm IV 12 hourly for 10 days.
- Moderate to Severe Uncomplicated Skin and Skin Structure Infections due to S. aureus or S. pyogenes: 2 gm IV 12 hourly for 10 days.
- Complicated Intra-abdominal Infections (used in combination with metronidazole) caused by E. coli, viridans group streptococci, P. aeruginosa, K. pneumoniae, Enterobacter species, or B. fragilis: 2 gm IV 12 hourly for 7-10 days.
*including cases associated with concurrent bacteremia.
**or until resolution of neutropenia. In patients whose fever resolves but who remain neutropenic for more than 7 days, the need for continued antimicrobial therapy should be re evaluated frequently.
*** IM route of administration is indicated only for mild to moderate, uncomplicated or complicated UTls due to E. coli when the IM route is considered to be a more appropriate route of drug administration.
Side effectsView
Cefepime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.
ContraindicationsView
Cefepime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.
PrecautionsView
- Prescribing Cefepime in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
- As with other antimicrobials, prolonged use of Cefepime may result in overgrowth of non susceptible microorganisms. Repeated evaluation of the patient's condition is essential.
- Many cephalosporins, including cefepime, have been associated with a fall in prothrombin activity. Those at risk include patients with renal or hepatic impairment, or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy. Prothrombin time should be monitored in patients at risk.
- Cefepime should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.
- Arginine has been shown to alter glucose metabolism and elevate serum potassium transiently when administered at 33 times the amount provided by the maximum recommended human dose of Cefepime. The effect of lower doses is not presently known.
InteractionsView
Renal function should be monitored carefully if high doses of aminoglycosides are to be administered with Cefepime because of the increased potential of nephrotoxicity and ototoxicity of aminoglycoside antibiotics. Nephrotoxicity has been reported following concomitant administration of other cephalosporins with potent diuretics such as furosemide.
Pregnancy & lactationView
Pregnancy Category B. There are, however, no adequate and well-controlled studies of cefepime use 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. Cefepime is excreted in human breast milk in very low concentrations (0.5 pg/ml). Caution should be exercised when cefepime is administered to a nursing woman.
Pediatric usageView
Pediatric Use (2 months up to 16 years): The maximum dose for pediatric patients should not exceed the recommended adult dose. The usual recommended dosage in pediatric patients up to 40 kg in weight for uncomplicated and complicated urinary tract infections (including pyelonephritis), uncomplicated skin and skin structure infections, and pneumonia is 50 mg/kg/dose, administered every 12 hours (50 mg/kg/dose, every 8 hours for febrile neutropenic patients), for durations as given above.
Geriatric Use: Serious adverse events have occurred in geriatric patients with renal insufficiency given unadjusted doses of cefepime, including life-threatening or fatal occurrences of the following: encephalopathy, myoclonus, and seizures. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and renal function should be monitored.
Impaired Hepatic Function: No adjustment is necessary for patients with impaired hepatic function.
Impaired Renal Function: In patients with impaired renal function (creatinine clearance<60 ml/min), the dose of Cefepime should be adjusted to compensate for the slower rate of renal elimination.
Geriatric Use: Serious adverse events have occurred in geriatric patients with renal insufficiency given unadjusted doses of cefepime, including life-threatening or fatal occurrences of the following: encephalopathy, myoclonus, and seizures. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and renal function should be monitored.
Impaired Hepatic Function: No adjustment is necessary for patients with impaired hepatic function.
Impaired Renal Function: In patients with impaired renal function (creatinine clearance<60 ml/min), the dose of Cefepime should be adjusted to compensate for the slower rate of renal elimination.
Overdose effectsView
Patients who receive an overdose should be carefully observed and given supportive treatment. In the presence of renal insufficiency, hemodialysis, not peritoneal dialysis, is recommended to aid the removal of cefepime from the body. Accidental overdosing has occurred when large doses were given to patients with impaired renal function. Symptoms of overdose include encephalopathy (disturbance of consciousness including confusion, hallucinations, stupor, and coma), myoclonus, seizures, and neuromuscular excitability.
ReconstitutionView
For IV the resulting solution should be injected directly into the vein over a period of three to five minutes or injected into the tubing of an administration set while the patient is receiving a compatible IV fluid.
Intravenous: Cefepime is compatible with Sterile Water for Injection. It is also compatible at concentrations between 1 mg/ml and 40 mg/ml with the following IV infusion fluids: 0.9% Sodium Chloride Injection, 5% and 10% Dextrose Injection, M/6 Sodium Lactate Injection, 5% Dextrose and 0.9% Sodium Chloride Injection, Lactated Ringers and 5% Dextrose Injection.
Intramuscular: Cefepime is compatible with the following diluent such as: Sterile Water for Injection, 0.9% Sodium Chloride Injection, 5% Dextrose Injection, Sterile Bacteriostatic Water for Injection with Parabens or Benzyl Alcohol or 0.5% or 1% Lidocaine Hydrochloride.
500 mg (IV) vials for intravenous administration:
Intravenous: Cefepime is compatible with Sterile Water for Injection. It is also compatible at concentrations between 1 mg/ml and 40 mg/ml with the following IV infusion fluids: 0.9% Sodium Chloride Injection, 5% and 10% Dextrose Injection, M/6 Sodium Lactate Injection, 5% Dextrose and 0.9% Sodium Chloride Injection, Lactated Ringers and 5% Dextrose Injection.
Intramuscular: Cefepime is compatible with the following diluent such as: Sterile Water for Injection, 0.9% Sodium Chloride Injection, 5% Dextrose Injection, Sterile Bacteriostatic Water for Injection with Parabens or Benzyl Alcohol or 0.5% or 1% Lidocaine Hydrochloride.
500 mg (IV) vials for intravenous administration:
- Amount of WFI to be added: 5 ml
- Approximate available volume: 5.6 ml
- Amount of WFI to be added: 1.3 ml
- Approximate available volume: 1.8 ml
- Amount of WFI to be added: 10 ml
- Approximate available volume: 11.3 ml
- Amount of WFI to be added: 2.4 ml
- Approximate available volume: 3.6 ml
- Amount of WFI to be added: 10 ml
- Approximate available volume: 12.5 ml
StorageView
Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician.
Xenim
Cefepime Hydrochloride
Xenim
Cefepime Hydrochloride
Indications
Urinary tract infection
Indication detailsView
Cefepime is indicated for the treatment of the following infections caused by susceptible strains of the microorganisms:
- Pneumonia (moderate to severe): caused by Streptococcus pneumoniae, including cases associated with concurrent bacteremia, Pseudomonas aeruginosa, Klebsiella pneumoniae, or Enterobacter species.
- Febrile Neutropenia: Cefepime as monotherapy is indicated for empiric treatment of febrile neutropenic patients. In patients at high risk for severe infection (including patients with a history of recent bone marrow transplantation, with hypotension at presentation, with an underlying hematologic malignancy, or with severe or prolonged neutropenia), antimicrobial monotherapy may not be appropriate. Insufficient data exist to support the efficacy of cefepime monotherapy in such patients.
- Uncomplicated and Complicated Urinary Tract Infections (including pyelonephritis): caused by Escherichia coli or Klebsiella pneumoniae, when the infection is severe, or caused by Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis, when the infection is mild to moderate, including cases associated with concurrent bacteremia with these microorganisms.
- Uncomplicated Skin and Skin Structure Infections: caused by Staphylococcus aureus (methicillin- susceptible strains only) or Streptococcus pyogenes.
- Complicated Intra-abdominal Infections (used in combination with metronidazole): caused by Escherichia coli, viridians group streptococci, Pseudomonas aeruginosa, Klebsiella pneumoniae, Enterobacter species, or Bacteroides fragilis.
Therapeutic classView
Fourth generation Cephalosporins
PharmacologyView
Cephalosporins are bactericidal and have the same mode of action as other beta-lactam antibiotics (such as penicillins). Cephalosporins disrupt the synthesis of the peptidoglycan layer of bacterial cell walls. The peptidoglycan layer is important for cell wall structural integrity, especially in Gram-positive organisms. The final transpeptidation step in the synthesis of the peptidoglycan is facilitated by transpeptidases known as penicillin binding proteins (PBPs).
DosageView
Cefepime should be administered intravenously over approximately 30 minutes.
*including cases associated with concurrent bacteremia.
**or until resolution of neutropenia. In patients whose fever resolves but who remain neutropenic for more than 7 days, the need for continued antimicrobial therapy should be re evaluated frequently.
*** IM route of administration is indicated only for mild to moderate, uncomplicated or complicated UTls due to E. coli when the IM route is considered to be a more appropriate route of drug administration.
- Moderate to Severe Pneumonia due to S. pneumoniae, *P. aeruginosa, K. pneumoniae, or Enterobacter species: 1-2 gm IV 12 hourly for 10 days.
- Empiric therapy for febrile neutropenic patients: 2 gm IV 8 hourly for 7** days.
- Mild to Moderate Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli, K. pneumoniae, or P. mirabilis*: 0.5-1 gm IV/IM*** 12 hourly for 7-10 days.
- Severe Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis, due to E. coli or K. pneumoniae*: 2 gm IV 12 hourly for 10 days.
- Moderate to Severe Uncomplicated Skin and Skin Structure Infections due to S. aureus or S. pyogenes: 2 gm IV 12 hourly for 10 days.
- Complicated Intra-abdominal Infections (used in combination with metronidazole) caused by E. coli, viridans group streptococci, P. aeruginosa, K. pneumoniae, Enterobacter species, or B. fragilis: 2 gm IV 12 hourly for 7-10 days.
*including cases associated with concurrent bacteremia.
**or until resolution of neutropenia. In patients whose fever resolves but who remain neutropenic for more than 7 days, the need for continued antimicrobial therapy should be re evaluated frequently.
*** IM route of administration is indicated only for mild to moderate, uncomplicated or complicated UTls due to E. coli when the IM route is considered to be a more appropriate route of drug administration.
Side effectsView
Cefepime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.
ContraindicationsView
Cefepime is contraindicated in patients who have shown immediate hypersensitivity reactions to cefepime or the cephalosporin class of antibiotics, penicillin, or other betalactum antibiotics.
PrecautionsView
- Prescribing Cefepime in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
- As with other antimicrobials, prolonged use of Cefepime may result in overgrowth of non susceptible microorganisms. Repeated evaluation of the patient's condition is essential.
- Many cephalosporins, including cefepime, have been associated with a fall in prothrombin activity. Those at risk include patients with renal or hepatic impairment, or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy. Prothrombin time should be monitored in patients at risk.
- Cefepime should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.
- Arginine has been shown to alter glucose metabolism and elevate serum potassium transiently when administered at 33 times the amount provided by the maximum recommended human dose of Cefepime. The effect of lower doses is not presently known.
InteractionsView
Renal function should be monitored carefully if high doses of aminoglycosides are to be administered with Cefepime because of the increased potential of nephrotoxicity and ototoxicity of aminoglycoside antibiotics. Nephrotoxicity has been reported following concomitant administration of other cephalosporins with potent diuretics such as furosemide.
Pregnancy & lactationView
Pregnancy Category B. There are, however, no adequate and well-controlled studies of cefepime use 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. Cefepime is excreted in human breast milk in very low concentrations (0.5 pg/ml). Caution should be exercised when cefepime is administered to a nursing woman.
Pediatric usageView
Pediatric Use (2 months up to 16 years): The maximum dose for pediatric patients should not exceed the recommended adult dose. The usual recommended dosage in pediatric patients up to 40 kg in weight for uncomplicated and complicated urinary tract infections (including pyelonephritis), uncomplicated skin and skin structure infections, and pneumonia is 50 mg/kg/dose, administered every 12 hours (50 mg/kg/dose, every 8 hours for febrile neutropenic patients), for durations as given above.
Geriatric Use: Serious adverse events have occurred in geriatric patients with renal insufficiency given unadjusted doses of cefepime, including life-threatening or fatal occurrences of the following: encephalopathy, myoclonus, and seizures. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and renal function should be monitored.
Impaired Hepatic Function: No adjustment is necessary for patients with impaired hepatic function.
Impaired Renal Function: In patients with impaired renal function (creatinine clearance<60 ml/min), the dose of Cefepime should be adjusted to compensate for the slower rate of renal elimination.
Geriatric Use: Serious adverse events have occurred in geriatric patients with renal insufficiency given unadjusted doses of cefepime, including life-threatening or fatal occurrences of the following: encephalopathy, myoclonus, and seizures. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and renal function should be monitored.
Impaired Hepatic Function: No adjustment is necessary for patients with impaired hepatic function.
Impaired Renal Function: In patients with impaired renal function (creatinine clearance<60 ml/min), the dose of Cefepime should be adjusted to compensate for the slower rate of renal elimination.
Overdose effectsView
Patients who receive an overdose should be carefully observed and given supportive treatment. In the presence of renal insufficiency, hemodialysis, not peritoneal dialysis, is recommended to aid the removal of cefepime from the body. Accidental overdosing has occurred when large doses were given to patients with impaired renal function. Symptoms of overdose include encephalopathy (disturbance of consciousness including confusion, hallucinations, stupor, and coma), myoclonus, seizures, and neuromuscular excitability.
ReconstitutionView
For IV the resulting solution should be injected directly into the vein over a period of three to five minutes or injected into the tubing of an administration set while the patient is receiving a compatible IV fluid.
Intravenous: Cefepime is compatible with Sterile Water for Injection. It is also compatible at concentrations between 1 mg/ml and 40 mg/ml with the following IV infusion fluids: 0.9% Sodium Chloride Injection, 5% and 10% Dextrose Injection, M/6 Sodium Lactate Injection, 5% Dextrose and 0.9% Sodium Chloride Injection, Lactated Ringers and 5% Dextrose Injection.
Intramuscular: Cefepime is compatible with the following diluent such as: Sterile Water for Injection, 0.9% Sodium Chloride Injection, 5% Dextrose Injection, Sterile Bacteriostatic Water for Injection with Parabens or Benzyl Alcohol or 0.5% or 1% Lidocaine Hydrochloride.
500 mg (IV) vials for intravenous administration:
Intravenous: Cefepime is compatible with Sterile Water for Injection. It is also compatible at concentrations between 1 mg/ml and 40 mg/ml with the following IV infusion fluids: 0.9% Sodium Chloride Injection, 5% and 10% Dextrose Injection, M/6 Sodium Lactate Injection, 5% Dextrose and 0.9% Sodium Chloride Injection, Lactated Ringers and 5% Dextrose Injection.
Intramuscular: Cefepime is compatible with the following diluent such as: Sterile Water for Injection, 0.9% Sodium Chloride Injection, 5% Dextrose Injection, Sterile Bacteriostatic Water for Injection with Parabens or Benzyl Alcohol or 0.5% or 1% Lidocaine Hydrochloride.
500 mg (IV) vials for intravenous administration:
- Amount of WFI to be added: 5 ml
- Approximate available volume: 5.6 ml
- Amount of WFI to be added: 1.3 ml
- Approximate available volume: 1.8 ml
- Amount of WFI to be added: 10 ml
- Approximate available volume: 11.3 ml
- Amount of WFI to be added: 2.4 ml
- Approximate available volume: 3.6 ml
- Amount of WFI to be added: 10 ml
- Approximate available volume: 12.5 ml
StorageView
Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician.
Xenobese
Orlistat
Xenobese
Orlistat
Indications
Obesity
Indication detailsView
Adults: Orlistat is indicated in conjunction with a mildly hypocaloric diet for the treatment of obese patients with a body mass index (BMI)>30 kg/m2 and overweight patients (BMI >28 kg/m2 ) with associated risk factors such as type II diabetes, hyperlipidemia and hypertension. Treatment with Orlistat should be discontinued after 12 weeks in patients who have not lost at least 5% of their body weight as measured at the start of drug therapy.
Adolescents (12 years & older): Obese adolescents should be treated with Orlistat only if an adequate reduction of body weight cannot be achieved by means of diet & increased physical activity. Treatment with orlistat should be considered in particular if complications of obesity are present.
Adolescents (12 years & older): Obese adolescents should be treated with Orlistat only if an adequate reduction of body weight cannot be achieved by means of diet & increased physical activity. Treatment with orlistat should be considered in particular if complications of obesity are present.
Therapeutic classView
Appetite suppressant drugs/Anti-obesity drugs
PharmacologyView
Orlistat is a potent, specific and long-acting lipase inhibitor. It exerts its therapeutic activity in the lumen of the stomach and upper small intestine by forming a covalent bond with the active serine site of gastric and pancreatic lipases. The inactivated enzyme is thus rendered unable to hydrolyze dietary fats in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides can not be absorbed, a caloric deficit arises which has a positive effect on weight control. Systemic absorption of orlistat is therefore not needed for the activity. At the recommended therapeutic dose of 120 mg three times a day, orlistat inhibit dietary fat absorption by approximately 30%.
DosageView
The recommended dose of Orlistat is one 120 mg capsule to be taken immediately before, during or up to one hour after each main meal. If a meal is missed or contains no fat the dose of Orlistat should be omitted. Doses of Orlistat above 120 mg three times daily have not been shown to provide additional benefits. The effect of Orlistat results in an increase in fecal fat 24-48 hours after dosing. Upon discontinuation of therapy, fecal fat content usually returns to pretreatment levels within 48-72 hours.
The safety & efficacy of Orlistat were investigated in clinical studies lasting up to 4 years. The recommended dose of Orlistat for adolescents is as same as adults.
Special dosage instruction: The tolerability and efficacy of Orlistat have not been studied in elderly patients, or patients with hepatic and/ or renal impairments.
The safety & efficacy of Orlistat were investigated in clinical studies lasting up to 4 years. The recommended dose of Orlistat for adolescents is as same as adults.
Special dosage instruction: The tolerability and efficacy of Orlistat have not been studied in elderly patients, or patients with hepatic and/ or renal impairments.
Side effectsView
Common: Undesirable effects of Orlistat are largely gastrointestinal in nature. Common gastrointestinal side effects are oily spotting from the rectum, flatulence, fecal urgency, oily or fatty stool, abdominal discomfort etc.
Rare: Influenza, anxiety. headache, fatigue etc may rarely occur in some patients. Rare cases of hypersensitivity have been reported. Main clinical symptoms are pruritus, exanthema, urticaria, angioedema and anaphylaxis.
Rare: Influenza, anxiety. headache, fatigue etc may rarely occur in some patients. Rare cases of hypersensitivity have been reported. Main clinical symptoms are pruritus, exanthema, urticaria, angioedema and anaphylaxis.
ContraindicationsView
Orlistat is contraindicated in patients with chronic malabsorption syndrome, in patients with cholestasis and in patients who are hypersensitive to orlistat or to any of the other ingredients of the capsules.
PrecautionsView
Organic causes of obesity (e.g. hypothyroidism) should be excluded before prescribing Orlistat. Orlistat and cyclosporine should not be coadministered. Cyclosporine should be taken at least 2 hours before or after Orlistat in patients taking both drugs. Cyclosporine level should be measured and frequently monitored.
In clinical trial, the decrease in body weight with Orlistat therapy was less in type II diabetic patients than in non-diabetic patients. Antidiabetic drug treatment should be closely monitored during Orlistat therapy. Because of the improvement in glycemic control, the dose of oral antidiabetics or of insulin may need to be adjusted.
Patients should be advised to adhere to the dietary recommendations. The probability of occurrence of gastrointestinal side effects may increase when Orlistat is taken with a fatty meal. The daily intake of fat should be distributed between three main meals. Patients should be strongly encouraged to take a multivitamin supplement that contains fat soluble vitamins to ensure adequate nutrition because orlistat has been shown to reduce the absorption of some fat soluble vitamins & beta-carotene. In addition, the levels of vitamin D & beta carotene may be low in obese patients compared with non-obese patients.
In clinical trial, the decrease in body weight with Orlistat therapy was less in type II diabetic patients than in non-diabetic patients. Antidiabetic drug treatment should be closely monitored during Orlistat therapy. Because of the improvement in glycemic control, the dose of oral antidiabetics or of insulin may need to be adjusted.
Patients should be advised to adhere to the dietary recommendations. The probability of occurrence of gastrointestinal side effects may increase when Orlistat is taken with a fatty meal. The daily intake of fat should be distributed between three main meals. Patients should be strongly encouraged to take a multivitamin supplement that contains fat soluble vitamins to ensure adequate nutrition because orlistat has been shown to reduce the absorption of some fat soluble vitamins & beta-carotene. In addition, the levels of vitamin D & beta carotene may be low in obese patients compared with non-obese patients.
InteractionsView
No interactions with commonly prescribed medications such as alcohol, digoxin, nifedipine, oral contraceptives, phenytoin, pravastatin, warfarin, or metformin, glibenclamide, fibrates, furosemide, captopril, or atenolol have been observed in studies.
Pregnancy & lactationView
Use in pregnancy & lactation: No clinical data are available on pregnancy exposed to Orlistat. As it is not known whether Orlistat is excreted in breast milk. Orlistat should not be used during breastfeeding.
Overdose effectsView
Single doses of 800 mg Orlistat and multiple doses of up to 400 mg three times a day for 15 days have been studied in normal weight and obese subjects without significant adverse findings.
StorageView
Store in cool & dry place below 30°C, protect from light & moisture. Keep out of reach of children.
Xenocort
Clobetasol Propionate (Topical Preparation)
Xenocort
Clobetasol Propionate (Topical Preparation)
Indications
Vitiligo
Indication detailsView
Clobetasol Propionate is indicated for adults, elderly and children over 1 year in following dermatoses.
- Psoriasis (excluding widespread plaque psoriasis)
- Recalcitrant dermatoses
- Lichen planus
- Discoid lupus erythematosus
- Other skin conditions which do not respond satisfactorily to less potent steroids
Therapeutic classView
Other Topical corticosteroids
PharmacologyView
Clobetasol Propionate is a very potent topical corticosteroid. It has anti-inflammatory, antipruritic and vasoconstrictive properties. It shows anti-inflammatory activity via multiple mechanisms to inhibit late phase allergic reactions. It decreases the density of mast cells, chemotaxis and activation of eosinophils. It also reduces cytokine production and inhibits the metabolism of arachidonic acid.
DosageView
Adults, elderly and children over 1 year: Apply a thin layer of Clobetasol Propionate Cream or Ointment to the affected skin areas twice daily and rub in gently and completely. Repeated short courses of Clobetasol Propionate may be used to control exacerbations. In more resistant lesions, especially where there is hyperkeratosis, the effect of Clobetasol can be enhanced, if necessary, by occluding the treatment area with polythene film. Overnight occlusion only is usually adequate to bring about a satisfactory response. Clobetasol Propionate is super-high potency topical corticosteroids; therefore, treatment should be limited to 2 consecutive weeks. The maximum weekly dose should not be exceeded 50 gm/week. In case of children, courses should be limited if possible to five days and reviewed weekly.
AdministrationView
Route of administration: Cutaneous. Creams are especially appropriate for moist or weeping surfaces. Ointments are especially appropriate for dry, lichenified or scaly lesions.
Side effectsView
The most reported side effects are burning and stinging sensation. Less frequent adverse reactions are itching, skin atrophy, cracking and fissuring of the skin. Cushing syndrome has been reported in infants and adults as a result of prolonged use of topical Clobetasol Propionate formulations.
ContraindicationsView
It is contraindicated in patient with hypersensitivity to any component of the preparation. It should not be used in rosacea, acne vulgaris, perioral dermatitis, perianal and genital pruritus, pruritus without inflammation, untreated cutaneous infections.
PrecautionsView
In case of using occlusive dressings, the skin should be cleansed before a fresh dressing is applied. Topical corticosteroids should be used with caution in psoriasis as rebound relapses, and development of local or systemic toxicity due to impaired barrier function of the skin may occur. If used on the face, treatment should be limited to 5 days. When Clobetasol Propionate used on eyelids, care should be taken to avoid the eyes as cataract and glaucoma might result from repeated exposure.
InteractionsView
Co-administered drugs that can inhibit CYP3A4 (eg ritonavir, itraconazole) have been shown to inhibit the metabolism of corticosteroids leading to increased systemic exposure.
Pregnancy & lactationView
There are limited data from the use of Clobetasol Propionate cream in pregnant women. Topical administration of corticosteroids to pregnant animals can cause abnormalities of foetal development. The relevance of this finding to humans has not been established. However, the administration of Clobetasol Propionate Cream during pregnancy and lactation should only be considered if the expected benefit to the mother outweighs the possible risks of treatment.
It is unknown whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Clobetasol Propionate Cream is administered to a nursing woman.
It is unknown whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Clobetasol Propionate Cream is administered to a nursing woman.
Pediatric usageView
In infants and children under 12 years of age, long-term continuous topical corticosteroid therapy should be avoided where possible, as adrenal suppression can occur. Children are more susceptible to the use of topical corticosteroids which develops atrophic changes.
Overdose effectsView
Acute overdosage is very unlikely to occur, however, in the case of chronic over-dosage or misuse the features of hypercortisolism may occur and in this situation topical steroid should be discontinued.
StorageView
Keep below 30°C temperature, protected from light and moisture. Do not freeze. Keep out of the reach of children.
Xenocort
Clobetasol Propionate (Topical Preparation)
Xenocort
Clobetasol Propionate (Topical Preparation)
Indications
Vitiligo
Indication detailsView
Clobetasol Propionate is indicated for adults, elderly and children over 1 year in following dermatoses.
- Psoriasis (excluding widespread plaque psoriasis)
- Recalcitrant dermatoses
- Lichen planus
- Discoid lupus erythematosus
- Other skin conditions which do not respond satisfactorily to less potent steroids
Therapeutic classView
Other Topical corticosteroids
PharmacologyView
Clobetasol Propionate is a very potent topical corticosteroid. It has anti-inflammatory, antipruritic and vasoconstrictive properties. It shows anti-inflammatory activity via multiple mechanisms to inhibit late phase allergic reactions. It decreases the density of mast cells, chemotaxis and activation of eosinophils. It also reduces cytokine production and inhibits the metabolism of arachidonic acid.
DosageView
Adults, elderly and children over 1 year: Apply a thin layer of Clobetasol Propionate Cream or Ointment to the affected skin areas twice daily and rub in gently and completely. Repeated short courses of Clobetasol Propionate may be used to control exacerbations. In more resistant lesions, especially where there is hyperkeratosis, the effect of Clobetasol can be enhanced, if necessary, by occluding the treatment area with polythene film. Overnight occlusion only is usually adequate to bring about a satisfactory response. Clobetasol Propionate is super-high potency topical corticosteroids; therefore, treatment should be limited to 2 consecutive weeks. The maximum weekly dose should not be exceeded 50 gm/week. In case of children, courses should be limited if possible to five days and reviewed weekly.
AdministrationView
Route of administration: Cutaneous. Creams are especially appropriate for moist or weeping surfaces. Ointments are especially appropriate for dry, lichenified or scaly lesions.
Side effectsView
The most reported side effects are burning and stinging sensation. Less frequent adverse reactions are itching, skin atrophy, cracking and fissuring of the skin. Cushing syndrome has been reported in infants and adults as a result of prolonged use of topical Clobetasol Propionate formulations.
ContraindicationsView
It is contraindicated in patient with hypersensitivity to any component of the preparation. It should not be used in rosacea, acne vulgaris, perioral dermatitis, perianal and genital pruritus, pruritus without inflammation, untreated cutaneous infections.
PrecautionsView
In case of using occlusive dressings, the skin should be cleansed before a fresh dressing is applied. Topical corticosteroids should be used with caution in psoriasis as rebound relapses, and development of local or systemic toxicity due to impaired barrier function of the skin may occur. If used on the face, treatment should be limited to 5 days. When Clobetasol Propionate used on eyelids, care should be taken to avoid the eyes as cataract and glaucoma might result from repeated exposure.
InteractionsView
Co-administered drugs that can inhibit CYP3A4 (eg ritonavir, itraconazole) have been shown to inhibit the metabolism of corticosteroids leading to increased systemic exposure.
Pregnancy & lactationView
There are limited data from the use of Clobetasol Propionate cream in pregnant women. Topical administration of corticosteroids to pregnant animals can cause abnormalities of foetal development. The relevance of this finding to humans has not been established. However, the administration of Clobetasol Propionate Cream during pregnancy and lactation should only be considered if the expected benefit to the mother outweighs the possible risks of treatment.
It is unknown whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Clobetasol Propionate Cream is administered to a nursing woman.
It is unknown whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Clobetasol Propionate Cream is administered to a nursing woman.
Pediatric usageView
In infants and children under 12 years of age, long-term continuous topical corticosteroid therapy should be avoided where possible, as adrenal suppression can occur. Children are more susceptible to the use of topical corticosteroids which develops atrophic changes.
Overdose effectsView
Acute overdosage is very unlikely to occur, however, in the case of chronic over-dosage or misuse the features of hypercortisolism may occur and in this situation topical steroid should be discontinued.
StorageView
Keep below 30°C temperature, protected from light and moisture. Do not freeze. Keep out of the reach of children.
Xenoderm
Clobetasol Propionate + Neomycin Sulphate + Nystatin
Xenoderm
Clobetasol Propionate + Neomycin Sulphate + Nystatin
Indications
Severe inflammatory skin disorders
Indication detailsView
This preparation is indicated in-
- Short courses treatment of recalcitrant eczemas.
- Neurodermatoses.
- Psoriasis (excluding widespread plaque psoriasis) where secondary bacterial infection or fungal infection is present, suspected or likely to occur.
- Other inflammatory conditions which do not respond satisfactorily to less active steroids.
Therapeutic classView
Clobetasol / Clobetasone & Combined Preparations
PharmacologyView
Clobetasol Propionate is a very potent corticosteroid. It is prescribed to treat severe inflammatory skin disorders such as eczema and psoriasis that have not responded to weaker corticosteroids. Neomycin Sulphate is an antibiotic of the aminoglycoside type and is used to treat infections with bacteria. Nystatin is an antifungal that kills fungi and yeasts by interfering with their cell membranes. The mechanism of the topical steroids like Clobetasol, in general, is unclear. However, Clobetasol Propionate is highly active corticosteroid with topical anti-inflammatory activity. The major effect of Clobetasol Propionate on skin is a nonspecific anti-inflammatory response, partially due to vasoconstriction and decrease in collagen synthesis. Neomycin binds to the ribosomal 30s and 50s sub-units of susceptible bacteria and inhibits protein synthesis. Neomycin also causes a misreading of the genetic codes of the mRNA template and this causes incorrect amino acids to be incorporated into the growing polypeptide chain. Nystatin acts by binding to sterols in the cell membrane of the fungus with a resultant change in membrane permeability allowing leakage of intracellular components.
DosageView
Adults: Apply sparingly to the affected area once or twice daily until improvement occurs. In very resistant lesion, especially where there is hyperkeratosis, the anti-inflammatory effect of this preparation can be enhanced (if necessary) by occluding the treatment area with polythene. Treatment should not be continued for more than 7 days without medical supervision. If a longer course is necessary, it is recommended that treatment should not be continued for more than 4 weeks without the patient's condition being reviewed.
Elderly: This preparation is suitable for use in elderly. Caution should be exercised in cases where a decrease in renal function exists and significant systemic absorption of Neomycin Sulphate may occur.
Children: This preparation is suitable for use in children (2 years and over) at the same dose as adults. A possibility of increased absorption exists in very young children, thus this cream/ointment is not recommended for use in neonates and infants (younger than 2 years).
Elderly: This preparation is suitable for use in elderly. Caution should be exercised in cases where a decrease in renal function exists and significant systemic absorption of Neomycin Sulphate may occur.
Children: This preparation is suitable for use in children (2 years and over) at the same dose as adults. A possibility of increased absorption exists in very young children, thus this cream/ointment is not recommended for use in neonates and infants (younger than 2 years).
Side effectsView
As with other topical corticosteroids, prolonged use of large amount or treatment of extensive areas can result in sufficient systemic absorption to produce the features of hypercortisolism. The effect is more likely to occur in infants and children and if occlusive dressings are used. Prolonged and intensive treatment with highly active corticosteroid preparations may cause local atrophic changes in the skin such as thinning, striae, and dilatation of the superficial blood vessels, particularly when occlusive dressings are used, or when skin folds are involved. There are reports of pigmentation changes and hypertrichosis with topical steroids.
ContraindicationsView
This medication is contraindicated in rosacea, acne vulgaris and perioral dermatitis, primary cutaneous viral infection (eg-Herpes simplex, chicken pox) and hypersensitivity to the preparation.
PrecautionsView
Long-term continuous topical therapy should be avoided where possible, particularly in infants and children, as adrenal suppression can occur readily even without occlusion. If applied to the eyelids, care is needed to ensure that the preparation does not enter the eye, as glaucoma might result. If this medication does enter the eye, the affected eye should be thoroughly washed with copious amount of water.
InteractionsView
Neomycin Sulphate can intensify and prolong the respiratory depressant effects of neuromuscular blocking agents following significant systemic absorption. However, if used in accordance with the recommendations, systemic exposure to Neomycin Sulphate is expected to be minimal and drug interactions are unlikely to be significant. No hazardous interactions have been reported with use of Clobetasol Propionate or Nystatin.
Pregnancy & lactationView
There is little information to demonstrate the possible effect of topically applied Neomycin in pregnancy and lactation. However, Neomycin present in the maternal blood can cross the placenta and may give rise to a theoretical risk of foetal toxicity, thus the use of the preparation is not recommended in pregnancy and lactation. The safety of Clobetasol Propionate has not been established in lactating mothers.
Overdose effectsView
Acute overdosage is very unlikely to occur. No overdose-related problem yet reported. However, in the case of chronic overdosage or misuse, the features of hypercortisolism may appear and in this situation, topical steroids should be discontinued gradually.
StorageView
Store below 25°C temperature. Do not freeze. Keep out of reach of children.
Xenoderm
Clobetasol Propionate + Neomycin Sulphate + Nystatin
Xenoderm
Clobetasol Propionate + Neomycin Sulphate + Nystatin
Indications
Severe inflammatory skin disorders
Indication detailsView
This preparation is indicated in-
- Short courses treatment of recalcitrant eczemas.
- Neurodermatoses.
- Psoriasis (excluding widespread plaque psoriasis) where secondary bacterial infection or fungal infection is present, suspected or likely to occur.
- Other inflammatory conditions which do not respond satisfactorily to less active steroids.
Therapeutic classView
Clobetasol / Clobetasone & Combined Preparations
PharmacologyView
Clobetasol Propionate is a very potent corticosteroid. It is prescribed to treat severe inflammatory skin disorders such as eczema and psoriasis that have not responded to weaker corticosteroids. Neomycin Sulphate is an antibiotic of the aminoglycoside type and is used to treat infections with bacteria. Nystatin is an antifungal that kills fungi and yeasts by interfering with their cell membranes. The mechanism of the topical steroids like Clobetasol, in general, is unclear. However, Clobetasol Propionate is highly active corticosteroid with topical anti-inflammatory activity. The major effect of Clobetasol Propionate on skin is a nonspecific anti-inflammatory response, partially due to vasoconstriction and decrease in collagen synthesis. Neomycin binds to the ribosomal 30s and 50s sub-units of susceptible bacteria and inhibits protein synthesis. Neomycin also causes a misreading of the genetic codes of the mRNA template and this causes incorrect amino acids to be incorporated into the growing polypeptide chain. Nystatin acts by binding to sterols in the cell membrane of the fungus with a resultant change in membrane permeability allowing leakage of intracellular components.
DosageView
Adults: Apply sparingly to the affected area once or twice daily until improvement occurs. In very resistant lesion, especially where there is hyperkeratosis, the anti-inflammatory effect of this preparation can be enhanced (if necessary) by occluding the treatment area with polythene. Treatment should not be continued for more than 7 days without medical supervision. If a longer course is necessary, it is recommended that treatment should not be continued for more than 4 weeks without the patient's condition being reviewed.
Elderly: This preparation is suitable for use in elderly. Caution should be exercised in cases where a decrease in renal function exists and significant systemic absorption of Neomycin Sulphate may occur.
Children: This preparation is suitable for use in children (2 years and over) at the same dose as adults. A possibility of increased absorption exists in very young children, thus this cream/ointment is not recommended for use in neonates and infants (younger than 2 years).
Elderly: This preparation is suitable for use in elderly. Caution should be exercised in cases where a decrease in renal function exists and significant systemic absorption of Neomycin Sulphate may occur.
Children: This preparation is suitable for use in children (2 years and over) at the same dose as adults. A possibility of increased absorption exists in very young children, thus this cream/ointment is not recommended for use in neonates and infants (younger than 2 years).
Side effectsView
As with other topical corticosteroids, prolonged use of large amount or treatment of extensive areas can result in sufficient systemic absorption to produce the features of hypercortisolism. The effect is more likely to occur in infants and children and if occlusive dressings are used. Prolonged and intensive treatment with highly active corticosteroid preparations may cause local atrophic changes in the skin such as thinning, striae, and dilatation of the superficial blood vessels, particularly when occlusive dressings are used, or when skin folds are involved. There are reports of pigmentation changes and hypertrichosis with topical steroids.
ContraindicationsView
This medication is contraindicated in rosacea, acne vulgaris and perioral dermatitis, primary cutaneous viral infection (eg-Herpes simplex, chicken pox) and hypersensitivity to the preparation.
PrecautionsView
Long-term continuous topical therapy should be avoided where possible, particularly in infants and children, as adrenal suppression can occur readily even without occlusion. If applied to the eyelids, care is needed to ensure that the preparation does not enter the eye, as glaucoma might result. If this medication does enter the eye, the affected eye should be thoroughly washed with copious amount of water.
InteractionsView
Neomycin Sulphate can intensify and prolong the respiratory depressant effects of neuromuscular blocking agents following significant systemic absorption. However, if used in accordance with the recommendations, systemic exposure to Neomycin Sulphate is expected to be minimal and drug interactions are unlikely to be significant. No hazardous interactions have been reported with use of Clobetasol Propionate or Nystatin.
Pregnancy & lactationView
There is little information to demonstrate the possible effect of topically applied Neomycin in pregnancy and lactation. However, Neomycin present in the maternal blood can cross the placenta and may give rise to a theoretical risk of foetal toxicity, thus the use of the preparation is not recommended in pregnancy and lactation. The safety of Clobetasol Propionate has not been established in lactating mothers.
Overdose effectsView
Acute overdosage is very unlikely to occur. No overdose-related problem yet reported. However, in the case of chronic overdosage or misuse, the features of hypercortisolism may appear and in this situation, topical steroids should be discontinued gradually.
StorageView
Store below 25°C temperature. Do not freeze. Keep out of reach of children.
Xenofer
Iron Sucrose Injection [Elemental Iron]
Xenofer
Iron Sucrose Injection [Elemental Iron]
Indications
Peritoneal dialysis dependent-chronic kidney disease (PDD-CKD) patients receiving an erythropoietin
Indication detailsView
This is indicated for the treatment of Iron deficiency in the following indications:
- Where there is a clinical need for a rapid Iron supply
- In patients who can not tolerate oral Iron therapy or who are non-compliant
- In active inflammatory bowel disease where oral Iron preparations are ineffective
- Non-dialysis dependent-chronic kidney disease (NDD-CKD) patients receiving an erythropoietin
- Non-dialysis dependent-chronic kidney disease (NDD-CKD) patients not receiving an erythropoietin
- Hemodialysis dependent-chronic kidney disease (HDD-CKD) patients receiving an erythropoietin
- Peritoneal dialysis dependent-chronic kidney disease (PDD-CKD) patients receiving an erythropoietin
- It is also indicated in the treatment of Iron deficiency anaemia in patients undergoing surgical procedures, patients donating blood, postpartum patients.
Therapeutic classView
Parenteral Iron Preparations
PharmacologyView
The therapeutic class of Iron Sucrose is haematinic. Iron Sucrose Injection USP is a brown, sterile, aqueous, complex of Polynuclear Iron (III) Hydroxide in Sucrose for Intravenous use. The drug product contains approximately 30% Sucrose w/v (300 mg/ml) and has a pH of 10.5-11.1. Following intravenous administration, Iron Sucrose Injection is dissociated into Iron and Sucrose by the reticuloendothelial system, and Iron is transferred from the blood to a pool of Iron in the liver and bone marrow. Ferritin, an Iron storage protein, binds and sequesters Iron in a nontoxic form, from which Iron is easily available. Iron binds to plasma transferrin, which carries Iron within the plasma and the extracellular fluid to supply the tissues. The transferrin receptor, located in the cell, and the transferrin-receptor complex is returned to the cell membrane. Transferrin without Iron (apotransferrin) is then released to the plasma. The intracellular Iron becomes (mostly) haemoglobin in circulating red blood cells (RBCs). Transferrin synthesis is increased and ferritin production reduced in Iron deficiency. The converse is true when Iron is plentiful. Its elimination halflife is 6 h, total clearance is 1.2 L/h, non-steady state apparent volume of distribution is 10.0 L and steady state apparent volume of distribution is 7.9 L. In Iron Sucrose, its Iron component appears to distribute mainly in blood and to some extent in extravascular fluid. A significant amount of the administered Iron distributes in the liver, spleen and bone marrow and that the bone marrow is an Iron trapping compartment and not a reversible volume distribution. The sucrose component is eliminated mainly through urinary excretion.
DosageView
Adults and Elderly: 5-10 ml Iron Sucrose Injection (100-200 mg Iron) once to three times a week depending on the hemoglobin level.
Children: There is limited data on children under study conditions. If there is a clinical need, it is recommended not to exceed 0.15 ml Iron Sucrose Injection (3 mg Iron) per kg body weight once to three times per week depending on the haemoglobin level.
Children: There is limited data on children under study conditions. If there is a clinical need, it is recommended not to exceed 0.15 ml Iron Sucrose Injection (3 mg Iron) per kg body weight once to three times per week depending on the haemoglobin level.
AdministrationView
Intravenous injection: Iron Sucrose Injection can also be administered undiluted by slow intravenous injection at the (normal) recommended rate of 1 ml Iron Sucrose Injection (20 mg Iron) per minute [5 ml Iron Sucrose Injection (100 mg Iron) in 2 to 5 minutes]. A maximum of 10 ml Iron Sucrose Injection (200 mg Iron) can be injected per injection. Before administration of the therapeutic dose in a new patient, a test dose of 1 ml Iron Sucrose Injection (20 mg Iron) in adults and in children with a body weight greater than 14 kg and half the daily dose (1.5 mg Iron/kg) in children with a body weight less than 14 kg should be injected over 1 to 2 minutes. If no adverse reactions occur within a waiting period of 15 minutes, the remaining portion of the injection can be administered at recommended speed. After an injection the arm of the patient should be extended.
Infusion: Iron Sucrose Injection should preferably be administered by drip infusion (in order to reduce the risk of hypotensive episodes and paravenous injection) in a dilution of 1 ml Iron Sucrose Injection (20 mg Iron) in max. 20 ml 0.9% w/v Sodium Chloride [5 ml (100 mg Iron) in max. 100 ml 0.9% w/v NaCI etc. up to 25 ml (500 mg Iron) in max. 500 ml 0.9% w/v NaCI]. Dilution must take place immediately prior to infusion and the solution should be administered as follows: 100 mg Iron in at least 15 minutes; 200 mg Iron in at least 30 minutes; 400 mg Iron In at least 1.5 hours, and 500 mg Iron in at least 3.5 hours. Further of the maximum tolerated single dose of 7 mg Iron/kg body weight, an Infusion time of at least 3.5 hours has to be respected, independently of the total dose.
Before administration of the therapeutic dose in a new patient the first 20 mg Iron in adults and in children with a body weight greater than 14 kg and half the daily dose (1.5 mg lron/kg) in children with a body weight less than 14 kg should be infused over 15 minutes as a test dose. If no adverse reactions occur, the remaining portion of the infusion can be administered at recommended speed.
Infusion: Iron Sucrose Injection should preferably be administered by drip infusion (in order to reduce the risk of hypotensive episodes and paravenous injection) in a dilution of 1 ml Iron Sucrose Injection (20 mg Iron) in max. 20 ml 0.9% w/v Sodium Chloride [5 ml (100 mg Iron) in max. 100 ml 0.9% w/v NaCI etc. up to 25 ml (500 mg Iron) in max. 500 ml 0.9% w/v NaCI]. Dilution must take place immediately prior to infusion and the solution should be administered as follows: 100 mg Iron in at least 15 minutes; 200 mg Iron in at least 30 minutes; 400 mg Iron In at least 1.5 hours, and 500 mg Iron in at least 3.5 hours. Further of the maximum tolerated single dose of 7 mg Iron/kg body weight, an Infusion time of at least 3.5 hours has to be respected, independently of the total dose.
Before administration of the therapeutic dose in a new patient the first 20 mg Iron in adults and in children with a body weight greater than 14 kg and half the daily dose (1.5 mg lron/kg) in children with a body weight less than 14 kg should be infused over 15 minutes as a test dose. If no adverse reactions occur, the remaining portion of the infusion can be administered at recommended speed.
Side effectsView
- Adverse reactions, whether or not related to Iron Sucrose injection are as follows: hypotension, cramps/leg cramps, nausea, headache, vomiting, and diarrhea. Some of these symptoms may be seen in patients with chronic renal failure or on hemodialysis not receiving intravenous iron.
- Body as a Whole: headache, fever, pain, asthenia, unwell, malaise, accidental injury. Cardiovascular Disorders
- General: hypotension, chest pain, hypertension, hypervolemia.
- Gastrointestinal Disorders: nausea, vomiting, abdominal pain, elevated liver enzymes.
- Central and Peripheral Nervous System: dizziness.
- Musculoskeletal System: cramps/leg cramps, musculoskeletal pain.
- Respiratory System: dyspnea pneumonia, cough.
- Skin and appendages: pruritus, application site reaction.
- Hypersensitivity reactions: In safety studies, several patients experienced mild or moderate hypersensitivity reactions presenting with wheezing, dyspnea, hypotension, rashes, or pruritus. Anaphylactoid reactions including patients who experienced serious or life-threatening reactions (anaphylactic shock, loss of consciousness or collapse, bronchospasm with dyspnea, or convulsion) associated with Iron Sucrose administration can occur. So, patients should be given a small test dose initially.
ContraindicationsView
The use of Iron Sucrose is contraindicated in patients with evidence of Iron overload, in patients with known hypersensitivity to Iron Sucrose or any of its inactive components, and in patients with anaemia not caused by Iron deficiency. It is also contraindicated in patients with history of allergic disorders including asthma, eczema and anaphylaxis, liver disease and infections.
PrecautionsView
General: Because body Iron excretion is limited and excess tissue Iron can be hazardous, caution should be exercised to withhold Iron administration in the presence of evidence of tissue Iron overload. Patients receiving Iron Sucrose require periodic monitoring of hematologic and haematinic parameters (hemoglobin, hematocrit, serum ferritin and transferrin saturation). Iron therapy should be withheld in patients with evidence of Iron overload. Transferrin saturation values increase rapidly after IV administration of Iron Sucrose; thus, serum Iron values may be reliably obtained 48 hours after IV dosing.
Hypersensitivity Reactions: Serious hypersensitivity reactions have been rarely reported in patients receiving Iron Sucrose. Several cases of mild or moderate hypersensitivity reactions were observed in these studies.
Hypotension: Hypotension has been reported frequently in hemodialysis patients receiving intravenous Iron. Hypotension following administration of Iron Sucrose may be related to rate of administration and total dose administered. Caution should be taken to administer Iron Sucrose according to recommended guidelines.
Hypersensitivity Reactions: Serious hypersensitivity reactions have been rarely reported in patients receiving Iron Sucrose. Several cases of mild or moderate hypersensitivity reactions were observed in these studies.
Hypotension: Hypotension has been reported frequently in hemodialysis patients receiving intravenous Iron. Hypotension following administration of Iron Sucrose may be related to rate of administration and total dose administered. Caution should be taken to administer Iron Sucrose according to recommended guidelines.
InteractionsView
Drug-drug interactions involving Iron Sucrose have not been studied. Iron Sucrose Injection should not be administered concomitantly with oral iron preparations since the absorption of oral Iron is reduced. Even oral Iron therapy should not be given until 5 days after last injection.
Pregnancy & lactationView
Pregnancy Category-B. No adequate and well controlled studies in pregnant women. This drug should be used during pregnancy only if clearly needed. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Iron Sucrose is administered to a nursing woman.
Pediatric usageView
Pediatric Use: Safety and effectiveness of Iron Sucrose in pediatric patients have not been established.
Geriatric Use: No overall differences in safety were observed between the elder subjects and younger subjects, 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.
Injection into dialyser: Iron Sucrose Injection may be administered directly into the venous limb of the dialyser under the same conditions as for intravenous injection.
Hemodialysis Dependent-Chronic Kidney Disease Patients (HDD-CKD): Iron Sucrose Injection may be administered undiluted as a 100 mg slow intravenous injection over 2 to 5 minutes or as an infusion of 100 mg, diluted in a maximum of 100 ml of 0.9% NaCI over a period of at least 15 minutes per consecutive hemodialysis session for a total cumulative dose of 1,000 mg.
Non-Dialysis Dependent-Chronic Kidney Disease Patient (NDD-CKD): Iron Sucrose Injection is administered as a total cumulative dose 1000 mg over a 14 day period as a 200 mg slow IV injection undiluted over 2 to 5 minutes on 5 different occasions within the 14 day period.
Geriatric Use: No overall differences in safety were observed between the elder subjects and younger subjects, 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.
Injection into dialyser: Iron Sucrose Injection may be administered directly into the venous limb of the dialyser under the same conditions as for intravenous injection.
Hemodialysis Dependent-Chronic Kidney Disease Patients (HDD-CKD): Iron Sucrose Injection may be administered undiluted as a 100 mg slow intravenous injection over 2 to 5 minutes or as an infusion of 100 mg, diluted in a maximum of 100 ml of 0.9% NaCI over a period of at least 15 minutes per consecutive hemodialysis session for a total cumulative dose of 1,000 mg.
Non-Dialysis Dependent-Chronic Kidney Disease Patient (NDD-CKD): Iron Sucrose Injection is administered as a total cumulative dose 1000 mg over a 14 day period as a 200 mg slow IV injection undiluted over 2 to 5 minutes on 5 different occasions within the 14 day period.
Overdose effectsView
Dosages of Iron Sucrose Injection in excess of Iron needs may lead to accumulation of Iron in storage sites leading to hemosiderosis. Periodic monitoring of Iron parameters such as serum ferritin and transferrin saturation may assist in recognizing Iron accumulation. Iron Sucrose should not be administered to patients with Iron overload and should be discontinued when serum ferritin levels equal or exceed established guidelines. Particular caution should be exercised to avoid Iron overload where anaemia unresponsive to treatment has been incorrectly diagnosed as Iron deficiency anaemia. Symptoms associated with overdosage or infusing Iron Sucrose too rapidly included hypotension, headache, vomiting, nausea, dizziness, joint aches, paresthesia, abdominal and muscle pain, edema. and cardiovascular collapse. Most symptoms have been successfully treated with IV fluids, hydrocortisone, and/or antihistamines. Infusing the solution as recommended or at a slower rate may also alleviate symptoms.
StorageView
Store in a cool (15°C- 30°C) & dry place, protected from light. Keep out of the reach of children. Do not freeze.
Xenofer
Iron Sucrose Injection [Elemental Iron]
Xenofer
Iron Sucrose Injection [Elemental Iron]
Indications
Peritoneal dialysis dependent-chronic kidney disease (PDD-CKD) patients receiving an erythropoietin
Indication detailsView
This is indicated for the treatment of Iron deficiency in the following indications:
- Where there is a clinical need for a rapid Iron supply
- In patients who can not tolerate oral Iron therapy or who are non-compliant
- In active inflammatory bowel disease where oral Iron preparations are ineffective
- Non-dialysis dependent-chronic kidney disease (NDD-CKD) patients receiving an erythropoietin
- Non-dialysis dependent-chronic kidney disease (NDD-CKD) patients not receiving an erythropoietin
- Hemodialysis dependent-chronic kidney disease (HDD-CKD) patients receiving an erythropoietin
- Peritoneal dialysis dependent-chronic kidney disease (PDD-CKD) patients receiving an erythropoietin
- It is also indicated in the treatment of Iron deficiency anaemia in patients undergoing surgical procedures, patients donating blood, postpartum patients.
Therapeutic classView
Parenteral Iron Preparations
PharmacologyView
The therapeutic class of Iron Sucrose is haematinic. Iron Sucrose Injection USP is a brown, sterile, aqueous, complex of Polynuclear Iron (III) Hydroxide in Sucrose for Intravenous use. The drug product contains approximately 30% Sucrose w/v (300 mg/ml) and has a pH of 10.5-11.1. Following intravenous administration, Iron Sucrose Injection is dissociated into Iron and Sucrose by the reticuloendothelial system, and Iron is transferred from the blood to a pool of Iron in the liver and bone marrow. Ferritin, an Iron storage protein, binds and sequesters Iron in a nontoxic form, from which Iron is easily available. Iron binds to plasma transferrin, which carries Iron within the plasma and the extracellular fluid to supply the tissues. The transferrin receptor, located in the cell, and the transferrin-receptor complex is returned to the cell membrane. Transferrin without Iron (apotransferrin) is then released to the plasma. The intracellular Iron becomes (mostly) haemoglobin in circulating red blood cells (RBCs). Transferrin synthesis is increased and ferritin production reduced in Iron deficiency. The converse is true when Iron is plentiful. Its elimination halflife is 6 h, total clearance is 1.2 L/h, non-steady state apparent volume of distribution is 10.0 L and steady state apparent volume of distribution is 7.9 L. In Iron Sucrose, its Iron component appears to distribute mainly in blood and to some extent in extravascular fluid. A significant amount of the administered Iron distributes in the liver, spleen and bone marrow and that the bone marrow is an Iron trapping compartment and not a reversible volume distribution. The sucrose component is eliminated mainly through urinary excretion.
DosageView
Adults and Elderly: 5-10 ml Iron Sucrose Injection (100-200 mg Iron) once to three times a week depending on the hemoglobin level.
Children: There is limited data on children under study conditions. If there is a clinical need, it is recommended not to exceed 0.15 ml Iron Sucrose Injection (3 mg Iron) per kg body weight once to three times per week depending on the haemoglobin level.
Children: There is limited data on children under study conditions. If there is a clinical need, it is recommended not to exceed 0.15 ml Iron Sucrose Injection (3 mg Iron) per kg body weight once to three times per week depending on the haemoglobin level.
AdministrationView
Intravenous injection: Iron Sucrose Injection can also be administered undiluted by slow intravenous injection at the (normal) recommended rate of 1 ml Iron Sucrose Injection (20 mg Iron) per minute [5 ml Iron Sucrose Injection (100 mg Iron) in 2 to 5 minutes]. A maximum of 10 ml Iron Sucrose Injection (200 mg Iron) can be injected per injection. Before administration of the therapeutic dose in a new patient, a test dose of 1 ml Iron Sucrose Injection (20 mg Iron) in adults and in children with a body weight greater than 14 kg and half the daily dose (1.5 mg Iron/kg) in children with a body weight less than 14 kg should be injected over 1 to 2 minutes. If no adverse reactions occur within a waiting period of 15 minutes, the remaining portion of the injection can be administered at recommended speed. After an injection the arm of the patient should be extended.
Infusion: Iron Sucrose Injection should preferably be administered by drip infusion (in order to reduce the risk of hypotensive episodes and paravenous injection) in a dilution of 1 ml Iron Sucrose Injection (20 mg Iron) in max. 20 ml 0.9% w/v Sodium Chloride [5 ml (100 mg Iron) in max. 100 ml 0.9% w/v NaCI etc. up to 25 ml (500 mg Iron) in max. 500 ml 0.9% w/v NaCI]. Dilution must take place immediately prior to infusion and the solution should be administered as follows: 100 mg Iron in at least 15 minutes; 200 mg Iron in at least 30 minutes; 400 mg Iron In at least 1.5 hours, and 500 mg Iron in at least 3.5 hours. Further of the maximum tolerated single dose of 7 mg Iron/kg body weight, an Infusion time of at least 3.5 hours has to be respected, independently of the total dose.
Before administration of the therapeutic dose in a new patient the first 20 mg Iron in adults and in children with a body weight greater than 14 kg and half the daily dose (1.5 mg lron/kg) in children with a body weight less than 14 kg should be infused over 15 minutes as a test dose. If no adverse reactions occur, the remaining portion of the infusion can be administered at recommended speed.
Infusion: Iron Sucrose Injection should preferably be administered by drip infusion (in order to reduce the risk of hypotensive episodes and paravenous injection) in a dilution of 1 ml Iron Sucrose Injection (20 mg Iron) in max. 20 ml 0.9% w/v Sodium Chloride [5 ml (100 mg Iron) in max. 100 ml 0.9% w/v NaCI etc. up to 25 ml (500 mg Iron) in max. 500 ml 0.9% w/v NaCI]. Dilution must take place immediately prior to infusion and the solution should be administered as follows: 100 mg Iron in at least 15 minutes; 200 mg Iron in at least 30 minutes; 400 mg Iron In at least 1.5 hours, and 500 mg Iron in at least 3.5 hours. Further of the maximum tolerated single dose of 7 mg Iron/kg body weight, an Infusion time of at least 3.5 hours has to be respected, independently of the total dose.
Before administration of the therapeutic dose in a new patient the first 20 mg Iron in adults and in children with a body weight greater than 14 kg and half the daily dose (1.5 mg lron/kg) in children with a body weight less than 14 kg should be infused over 15 minutes as a test dose. If no adverse reactions occur, the remaining portion of the infusion can be administered at recommended speed.
Side effectsView
- Adverse reactions, whether or not related to Iron Sucrose injection are as follows: hypotension, cramps/leg cramps, nausea, headache, vomiting, and diarrhea. Some of these symptoms may be seen in patients with chronic renal failure or on hemodialysis not receiving intravenous iron.
- Body as a Whole: headache, fever, pain, asthenia, unwell, malaise, accidental injury. Cardiovascular Disorders
- General: hypotension, chest pain, hypertension, hypervolemia.
- Gastrointestinal Disorders: nausea, vomiting, abdominal pain, elevated liver enzymes.
- Central and Peripheral Nervous System: dizziness.
- Musculoskeletal System: cramps/leg cramps, musculoskeletal pain.
- Respiratory System: dyspnea pneumonia, cough.
- Skin and appendages: pruritus, application site reaction.
- Hypersensitivity reactions: In safety studies, several patients experienced mild or moderate hypersensitivity reactions presenting with wheezing, dyspnea, hypotension, rashes, or pruritus. Anaphylactoid reactions including patients who experienced serious or life-threatening reactions (anaphylactic shock, loss of consciousness or collapse, bronchospasm with dyspnea, or convulsion) associated with Iron Sucrose administration can occur. So, patients should be given a small test dose initially.
ContraindicationsView
The use of Iron Sucrose is contraindicated in patients with evidence of Iron overload, in patients with known hypersensitivity to Iron Sucrose or any of its inactive components, and in patients with anaemia not caused by Iron deficiency. It is also contraindicated in patients with history of allergic disorders including asthma, eczema and anaphylaxis, liver disease and infections.
PrecautionsView
General: Because body Iron excretion is limited and excess tissue Iron can be hazardous, caution should be exercised to withhold Iron administration in the presence of evidence of tissue Iron overload. Patients receiving Iron Sucrose require periodic monitoring of hematologic and haematinic parameters (hemoglobin, hematocrit, serum ferritin and transferrin saturation). Iron therapy should be withheld in patients with evidence of Iron overload. Transferrin saturation values increase rapidly after IV administration of Iron Sucrose; thus, serum Iron values may be reliably obtained 48 hours after IV dosing.
Hypersensitivity Reactions: Serious hypersensitivity reactions have been rarely reported in patients receiving Iron Sucrose. Several cases of mild or moderate hypersensitivity reactions were observed in these studies.
Hypotension: Hypotension has been reported frequently in hemodialysis patients receiving intravenous Iron. Hypotension following administration of Iron Sucrose may be related to rate of administration and total dose administered. Caution should be taken to administer Iron Sucrose according to recommended guidelines.
Hypersensitivity Reactions: Serious hypersensitivity reactions have been rarely reported in patients receiving Iron Sucrose. Several cases of mild or moderate hypersensitivity reactions were observed in these studies.
Hypotension: Hypotension has been reported frequently in hemodialysis patients receiving intravenous Iron. Hypotension following administration of Iron Sucrose may be related to rate of administration and total dose administered. Caution should be taken to administer Iron Sucrose according to recommended guidelines.
InteractionsView
Drug-drug interactions involving Iron Sucrose have not been studied. Iron Sucrose Injection should not be administered concomitantly with oral iron preparations since the absorption of oral Iron is reduced. Even oral Iron therapy should not be given until 5 days after last injection.
Pregnancy & lactationView
Pregnancy Category-B. No adequate and well controlled studies in pregnant women. This drug should be used during pregnancy only if clearly needed. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Iron Sucrose is administered to a nursing woman.
Pediatric usageView
Pediatric Use: Safety and effectiveness of Iron Sucrose in pediatric patients have not been established.
Geriatric Use: No overall differences in safety were observed between the elder subjects and younger subjects, 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.
Injection into dialyser: Iron Sucrose Injection may be administered directly into the venous limb of the dialyser under the same conditions as for intravenous injection.
Hemodialysis Dependent-Chronic Kidney Disease Patients (HDD-CKD): Iron Sucrose Injection may be administered undiluted as a 100 mg slow intravenous injection over 2 to 5 minutes or as an infusion of 100 mg, diluted in a maximum of 100 ml of 0.9% NaCI over a period of at least 15 minutes per consecutive hemodialysis session for a total cumulative dose of 1,000 mg.
Non-Dialysis Dependent-Chronic Kidney Disease Patient (NDD-CKD): Iron Sucrose Injection is administered as a total cumulative dose 1000 mg over a 14 day period as a 200 mg slow IV injection undiluted over 2 to 5 minutes on 5 different occasions within the 14 day period.
Geriatric Use: No overall differences in safety were observed between the elder subjects and younger subjects, 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.
Injection into dialyser: Iron Sucrose Injection may be administered directly into the venous limb of the dialyser under the same conditions as for intravenous injection.
Hemodialysis Dependent-Chronic Kidney Disease Patients (HDD-CKD): Iron Sucrose Injection may be administered undiluted as a 100 mg slow intravenous injection over 2 to 5 minutes or as an infusion of 100 mg, diluted in a maximum of 100 ml of 0.9% NaCI over a period of at least 15 minutes per consecutive hemodialysis session for a total cumulative dose of 1,000 mg.
Non-Dialysis Dependent-Chronic Kidney Disease Patient (NDD-CKD): Iron Sucrose Injection is administered as a total cumulative dose 1000 mg over a 14 day period as a 200 mg slow IV injection undiluted over 2 to 5 minutes on 5 different occasions within the 14 day period.
Overdose effectsView
Dosages of Iron Sucrose Injection in excess of Iron needs may lead to accumulation of Iron in storage sites leading to hemosiderosis. Periodic monitoring of Iron parameters such as serum ferritin and transferrin saturation may assist in recognizing Iron accumulation. Iron Sucrose should not be administered to patients with Iron overload and should be discontinued when serum ferritin levels equal or exceed established guidelines. Particular caution should be exercised to avoid Iron overload where anaemia unresponsive to treatment has been incorrectly diagnosed as Iron deficiency anaemia. Symptoms associated with overdosage or infusing Iron Sucrose too rapidly included hypotension, headache, vomiting, nausea, dizziness, joint aches, paresthesia, abdominal and muscle pain, edema. and cardiovascular collapse. Most symptoms have been successfully treated with IV fluids, hydrocortisone, and/or antihistamines. Infusing the solution as recommended or at a slower rate may also alleviate symptoms.
StorageView
Store in a cool (15°C- 30°C) & dry place, protected from light. Keep out of the reach of children. Do not freeze.