Find Medicines — Doctors In Bangladesh

Ema

Esomeprazole

Tablet (Enteric Coated) 20 mg Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Ema

Esomeprazole

Capsule (Delayed Release) 40 mg Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Ema

Esomeprazole

Tablet (Enteric Coated) 40 mg Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Ema

Esomeprazole

IV Injection 40 mg/vial Allopathic

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 (C_max) occur at approximately 1.5 hours (T_max). The C_maxincreases 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.

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.

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.

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.

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.

Emaprox

Naproxen Sodium + Esomeprazole Magnesium

Tablet (Delayed Release) 500 mg+20 mg Allopathic Drugs for Osteoarthritis

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.

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-

Adults: One tablet twice daily of either: 375 mg naproxen/20 mg of esomeprazole; or 500 mg naproxen/20 mg of esomeprazole

Juvenile Idiopathic Arthritis in Adolescent Patients 12 Years of Age & Older-

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).

With food & others: Administration of Naproxen & Esomeprazole together with high-fat food in healthy volunteers does not affect the extent of absorption of naproxen but significantly prolongs t_max by 10 hours and decreases peak plasma concentration (C_max) by about 12%

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.

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.

StorageView

Store at temperature of below 30°C, protect from light & moisture. Keep out of reach of children.

Emaprox

Naproxen Sodium + Esomeprazole Magnesium

Tablet (Delayed Release) 375 mg+20 mg Allopathic Drugs for Osteoarthritis

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.

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-

Adults: One tablet twice daily of either: 375 mg naproxen/20 mg of esomeprazole; or 500 mg naproxen/20 mg of esomeprazole

Juvenile Idiopathic Arthritis in Adolescent Patients 12 Years of Age & Older-

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).

With food & others: Administration of Naproxen & Esomeprazole together with high-fat food in healthy volunteers does not affect the extent of absorption of naproxen but significantly prolongs t_max by 10 hours and decreases peak plasma concentration (C_max) by about 12%

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.

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.

StorageView

Store at temperature of below 30°C, protect from light & moisture. Keep out of reach of children.

Emazid

Empagliflozin

Tablet 10 mg Allopathic Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors

Indications

Type 2 DM

Indication detailsView

Empagliflozin is indicated in:

As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
To reduce the risk of cardiovascular death in adult patients with type 2 diabetes mellitus and established cardiovascular disease.

Therapeutic classView

Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors

PharmacologyView

Empagliflozin is a sodium glucose co-transporter-2 (SGLT-2) inhibitor. SGLT2 co-transporters are responsible for reabsorption of glucose from the glomerular filtrate in the kidney. The glucuretic effect resulting from SGLT2 inhibition reduces renal absorption and lowers the renal threshold for glucose, resulting in increased glucose excretion. Additionally, it contributes to reduced hyperglycaemia, assists weight loss, and reduces blood pressure.

DosageView

The recommended dose of Empagliflozin is 10 mg once daily, taken in the morning, with or without food. In patients tolerating Empagliflozin, the dose may be increased to 25 mg once daily. In patients with volume depletion, correcting this condition prior to initiation of Empagliflozin is recommended.

Side effectsView

The most common adverse reactions associated with Empagliflozin are urinary tract infections and female genital mycotic infections. Others common side effects includes dehydration, hypotension, weakness, dizziness and increased thirstiness.

ContraindicationsView

Empagliflozin is contraindicated in patients with history of serious hypersensitivity reaction to Empagliflozin or any of its ingredients, severe renal impairment, end-stage renal disease, or dialysis.

PrecautionsView

Assessment of renal function is recommended prior to initiation of Empagliflozin and periodically thereafter. Empagliflozin should not initiated in patients with an eGFR less than 45 ml/min/1.73 m². No dose adjustment is needed in patients with an eGFR greater than or equal to 45 ml/min/1.73 m².

InteractionsView

Diuretics: Co-administration of Empagliflozin with diuretics resulted in increased urine volume.

Insulin or Insulin Secretagogues: Co-administration of Empagliflozin with insulin or insulin secretagogues increases the risk for hypoglycemia.

Positive Urine Glucose Test: Monitoring glycemic control with urine glucose tests is not recommended in patients taking SGLT2 inhibitors as SGLT2 inhibitors increase urinary glucose excretion and will lead to positive urine glucose tests. Use alternative methods to monitor glycemic control.

Interference with 1,5-anhydroglucitol (1,5-AG) Assay: Monitoring glycemic control with 1,5-AG assay is not recommended as measurements of 1,5-AG are unreliable in assessing glycemic control in patients taking SGLT2 inhibitors. Use alternative methods to monitor glycemic control.

Pregnancy & lactationView

There are no adequate and well-controlled studies of Empagliflozin in pregnant women. Empagliflozin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known if Empagliflozin is excreted in human milk. It is not recommended when breastfeeding.

Overdose effectsView

In the event of an overdose with Empagliflozin the usual supportive measures (e.g., remove unabsorbed material from the gastrointestinal tract, perform clinical monitoring, and institute supportive treatment) should be employed. Removal of Empagliflozin by hemodialysis has not been studied.

StorageView

Keep in a cool & dry place (below 30° C), protected from light & moisture. Keep out of the reach of children.

Emazid

Empagliflozin

Tablet 25 mg Allopathic Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors

Indications

Type 2 DM

Indication detailsView

Empagliflozin is indicated in:

As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
To reduce the risk of cardiovascular death in adult patients with type 2 diabetes mellitus and established cardiovascular disease.

Therapeutic classView

Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors

PharmacologyView

Empagliflozin is a sodium glucose co-transporter-2 (SGLT-2) inhibitor. SGLT2 co-transporters are responsible for reabsorption of glucose from the glomerular filtrate in the kidney. The glucuretic effect resulting from SGLT2 inhibition reduces renal absorption and lowers the renal threshold for glucose, resulting in increased glucose excretion. Additionally, it contributes to reduced hyperglycaemia, assists weight loss, and reduces blood pressure.

DosageView

The recommended dose of Empagliflozin is 10 mg once daily, taken in the morning, with or without food. In patients tolerating Empagliflozin, the dose may be increased to 25 mg once daily. In patients with volume depletion, correcting this condition prior to initiation of Empagliflozin is recommended.

Side effectsView

The most common adverse reactions associated with Empagliflozin are urinary tract infections and female genital mycotic infections. Others common side effects includes dehydration, hypotension, weakness, dizziness and increased thirstiness.

ContraindicationsView

Empagliflozin is contraindicated in patients with history of serious hypersensitivity reaction to Empagliflozin or any of its ingredients, severe renal impairment, end-stage renal disease, or dialysis.

PrecautionsView

Assessment of renal function is recommended prior to initiation of Empagliflozin and periodically thereafter. Empagliflozin should not initiated in patients with an eGFR less than 45 ml/min/1.73 m². No dose adjustment is needed in patients with an eGFR greater than or equal to 45 ml/min/1.73 m².

InteractionsView

Diuretics: Co-administration of Empagliflozin with diuretics resulted in increased urine volume.

Insulin or Insulin Secretagogues: Co-administration of Empagliflozin with insulin or insulin secretagogues increases the risk for hypoglycemia.

Positive Urine Glucose Test: Monitoring glycemic control with urine glucose tests is not recommended in patients taking SGLT2 inhibitors as SGLT2 inhibitors increase urinary glucose excretion and will lead to positive urine glucose tests. Use alternative methods to monitor glycemic control.

Interference with 1,5-anhydroglucitol (1,5-AG) Assay: Monitoring glycemic control with 1,5-AG assay is not recommended as measurements of 1,5-AG are unreliable in assessing glycemic control in patients taking SGLT2 inhibitors. Use alternative methods to monitor glycemic control.

Pregnancy & lactationView

There are no adequate and well-controlled studies of Empagliflozin in pregnant women. Empagliflozin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known if Empagliflozin is excreted in human milk. It is not recommended when breastfeeding.

Overdose effectsView

In the event of an overdose with Empagliflozin the usual supportive measures (e.g., remove unabsorbed material from the gastrointestinal tract, perform clinical monitoring, and institute supportive treatment) should be employed. Removal of Empagliflozin by hemodialysis has not been studied.

StorageView

Keep in a cool & dry place (below 30° C), protected from light & moisture. Keep out of the reach of children.

Emazid L

Empagliflozin + Linagliptin

Tablet 25 mg+5 mg Allopathic

Indication detailsView

This is a combination of empagliflozin, a sodium-glucose co-transporter 2 (SGLT2) inhibitor and linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Empagliflozin is indicated to reduce the risk of cardiovascular death in adults with type 2 diabetes mellitus and established cardiovascular disease.

PharmacologyView

Empagliflozin: Sodium-glucose co-transporter 2 (SGLT2) is the predominant transporter responsible for the reabsorption of glucose from the glomerular filtrate back into the circulation. Empagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, empagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increasing urinary glucose excretion.

Linagliptin: Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output.

DosageView

Assess renal function before initiating and as clinically indicated. The recommended dose of this is 10 mg empagliflozin and 5 mg linagliptin once daily, taken in the morning, with or without food. Dose may be increased to 25 mg empagliflozin and 5 mg linagliptin once daily.

Pediatric Patients: The safety and effectiveness in pediatric patients have not been established.

Geriatric Patients: Higher incidence of adverse reactions related to volume depletion and reduced renal function.

Renal Impairment: Higher incidence of adverse reactions related to reduced renal function.

Side effectsView

The most common side effects are:

urinary tract infection
stuffy or runny nose and sore throat
upper respiratory tract infection

PrecautionsView

Pancreatitis: There have been reports of acute pancreatitis, including fatal pancreatitis. If pancreatitis is suspected, promptly discontinue this tablet.

Ketoacidosis: Assess patients who present with signs and symptoms of metabolic acidosis for ketoacidosis, regardless of blood glucose level. If suspected, discontinue this tablet, evaluate and treat promptly. Before initiating this tablet, consider risk factors for ketoacidosis. Patients on this tablet may require monitoring and temporary discontinuation of therapy in clinical situations known to predispose to ketoacidosis.

Volume Depletion: Before initiating this tablet, assess volume status and renal function in patients with impaired renal function, elderly patients, or patients on loop diuretics. Monitor for signs and symptoms during therapy.

Urosepsis and Pyelonephritis: Evaluate patients for signs and symptoms of urinary tract infections and treat promptly, if indicated.

Hypoglycemia: Consider lowering the dose of insulin secretagogue or insulin to reduce the risk of hypoglycemia when initiating this tablet.

Necrotizing Fasciitis of the Perineum (Fournier’s Gangrene): Serious, life-threatening cases have occurred in both females and males. Assess patients presenting with pain or tenderness, erythema, or swelling in the genital or perineal area, along with fever or malaise. If suspected, institute prompt treatment.

Genital Mycotic Infections: Monitor and treat as appropriate.

Hypersensitivity Reactions: Serious hypersensitivity reactions (e.g., anaphylaxis, angioedema, and exfoliative skin conditions) have occurred with empagliflozin and linagliptin. If hypersensitivity reactions occur, discontinue this tablet, treat promptly, and monitor until signs and symptoms resolve.

Arthralgia: Severe and disabling arthralgia has been reported in patients taking DPP-4 inhibitors. Consider as a possible cause for severe joint pain and discontinue drug if appropriate.

Bullous Pemphigoid: There have been reports of bullous pemphigoid requiring hospitalization. Tell patients to report the development of blisters or erosions. If bullous pemphigoid is suspected, discontinue this tablet.

Heart Failure: Heart failure has been observed with two other members of the DPP-4 inhibitor class. Consider risks and benefits of this tablet in patients who have known risk factors for heart failure. Monitor for signs and symptoms.

Pregnancy & lactationView

Advise females of the potential risk to a fetus, especially during the second and third trimesters. This is not recommended when breastfeeding.

StorageView

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Emazid L

Empagliflozin + Linagliptin

Tablet 10 mg+5 mg Allopathic

Indication detailsView

This is a combination of empagliflozin, a sodium-glucose co-transporter 2 (SGLT2) inhibitor and linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Empagliflozin is indicated to reduce the risk of cardiovascular death in adults with type 2 diabetes mellitus and established cardiovascular disease.

PharmacologyView

Empagliflozin: Sodium-glucose co-transporter 2 (SGLT2) is the predominant transporter responsible for the reabsorption of glucose from the glomerular filtrate back into the circulation. Empagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, empagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increasing urinary glucose excretion.

Linagliptin: Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output.

DosageView

Assess renal function before initiating and as clinically indicated. The recommended dose of this is 10 mg empagliflozin and 5 mg linagliptin once daily, taken in the morning, with or without food. Dose may be increased to 25 mg empagliflozin and 5 mg linagliptin once daily.

Pediatric Patients: The safety and effectiveness in pediatric patients have not been established.

Geriatric Patients: Higher incidence of adverse reactions related to volume depletion and reduced renal function.

Renal Impairment: Higher incidence of adverse reactions related to reduced renal function.

Side effectsView

The most common side effects are:

urinary tract infection
stuffy or runny nose and sore throat
upper respiratory tract infection

PrecautionsView

Pancreatitis: There have been reports of acute pancreatitis, including fatal pancreatitis. If pancreatitis is suspected, promptly discontinue this tablet.

Ketoacidosis: Assess patients who present with signs and symptoms of metabolic acidosis for ketoacidosis, regardless of blood glucose level. If suspected, discontinue this tablet, evaluate and treat promptly. Before initiating this tablet, consider risk factors for ketoacidosis. Patients on this tablet may require monitoring and temporary discontinuation of therapy in clinical situations known to predispose to ketoacidosis.

Volume Depletion: Before initiating this tablet, assess volume status and renal function in patients with impaired renal function, elderly patients, or patients on loop diuretics. Monitor for signs and symptoms during therapy.

Urosepsis and Pyelonephritis: Evaluate patients for signs and symptoms of urinary tract infections and treat promptly, if indicated.

Hypoglycemia: Consider lowering the dose of insulin secretagogue or insulin to reduce the risk of hypoglycemia when initiating this tablet.

Necrotizing Fasciitis of the Perineum (Fournier’s Gangrene): Serious, life-threatening cases have occurred in both females and males. Assess patients presenting with pain or tenderness, erythema, or swelling in the genital or perineal area, along with fever or malaise. If suspected, institute prompt treatment.

Genital Mycotic Infections: Monitor and treat as appropriate.

Hypersensitivity Reactions: Serious hypersensitivity reactions (e.g., anaphylaxis, angioedema, and exfoliative skin conditions) have occurred with empagliflozin and linagliptin. If hypersensitivity reactions occur, discontinue this tablet, treat promptly, and monitor until signs and symptoms resolve.

Arthralgia: Severe and disabling arthralgia has been reported in patients taking DPP-4 inhibitors. Consider as a possible cause for severe joint pain and discontinue drug if appropriate.

Bullous Pemphigoid: There have been reports of bullous pemphigoid requiring hospitalization. Tell patients to report the development of blisters or erosions. If bullous pemphigoid is suspected, discontinue this tablet.

Heart Failure: Heart failure has been observed with two other members of the DPP-4 inhibitor class. Consider risks and benefits of this tablet in patients who have known risk factors for heart failure. Monitor for signs and symptoms.

Pregnancy & lactationView

Advise females of the potential risk to a fetus, especially during the second and third trimesters. This is not recommended when breastfeeding.

StorageView

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Emazid M

Empagliflozin + Metformin Hydrochloride

Tablet 5 mg+500 mg Allopathic Combination Oral hypoglycemic preparations

Indications

Type 2 DM

Indication detailsView

This tablet is indicated for the treatment of adults with type 2 diabetes mellitus as an adjunct to diet and exercise:

In patients insufficiently controlled on their maximally tolerated dose of Metformin alone
In combination with other medicinal products for the treatment of diabetes, in patients insufficiently controlled with Metformin and these medicinal products
In patients already being treated with the combination of Empagliflozin and Metformin as separate tablets.

Therapeutic classView

Combination Oral hypoglycemic preparations

PharmacologyView

Empagliflozin is an inhibitor of Sodium-Glucose Co-Transporter 2 (SGLT2). SGLT2 is the predominant transporter, responsible for reabsorption of glucose from the kidney back into the circulation. By inhibiting SGLT2, Empagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose and thereby increases urinary glucose excretion.

Metformin Hydrochloride is a biguanide type oral antihyperglycemic drug, used in the management of type 2 diabetes. It lowers both basal and postprandial plasma glucose. It does not produce hypoglycemia. Metformin Hydrochloride decreases hepatic glucose production, decreases intestinal absorption of glucose and improves insulin sensitivity by an increase in peripheral glucose uptake and utilization.

DosageView

The dosage should be individualized based on effectiveness and tolerability. Take this combination twice daily with meals. Dose escalation should be gradual to reduce the gastrointestinal side effects due to Metformin Hydrochloride. Maximum recommended daily dose of Metformin Hydrochloride is 2000 mg and Empagliflozin is 25 mg.

Recommended individualized starting dose:

In patients on Metformin Hydrochloride, switch to this combination containing Empagliflozin 5 mg with a similar total daily dose of Metformin Hydrochloride.
In patients on Empagliflozin, switch to this combination containing Metformin Hydrochloride 500 mg with a similar total daily dose of Empagliflozin.
In patients already treated with Empagliflozin and Metformin Hydrochloride separately switch to this combination containing the same total daily doses of each component.
In patients with volume depletion not previously treated with Empagliflozin, correct this condition before initiating this combination.

Renal impaired patient: Assess renal function before initiating this combination. In patients with an eGFR below 45 mL/min/1.73 m² is contraindicated.

Pediatric patients under 18 years of age: Safety and effectiveness in pediatric patients under 18 years of age have not been established.

Side effectsView

Most common adverse reactions associated with Empagliflozin (5% or greater incidence) were urinary tract infection and female genital mycotic infections. Most common adverse reactions associated with Metformin (>5%) are diarrhea, nausea/vomiting, flatulence, abdominal discomfort, indigestion, asthenia, and headache. The following important adverse reactions are given below:

Very common: Hypoglycemia (when used with sulphonylurea or insulin), Gastrointestinal symptoms
Common: Vaginal moniliasis, vulvovaginitis, balanitis and other genital infection. Urinary tract infection (including pyelonephritis and urosepsis), thirst, taste disturbance, pruritus (generalised), rash, Increased urination, serum lipids increased
Uncommon: Volume depletion, urticaria, dysuria, blood creatinine increased/Glomerular filtration rate decreased, Haematocrit increased
Rare: Diabetic ketoacidosis.

ContraindicationsView

Hypersensitivity to Empagliflozin and Metformin
Any type of acute metabolic acidosis (such as lactic acidosis, diabetic ketoacidosis)
Diabetic pre-coma
Severe renal failure (GFR <30 ml/min)
Acute conditions with the potential to alter renal function such as: dehydration, severe infection, shock
Disease which may cause tissue hypoxia (especially acute disease, or worsening of chronic disease) such as: decompensated heart failure, respiratory failure, recent myocardial infarction, shock
Hepatic impairment, acute alcohol intoxication, alcoholism

PrecautionsView

Lactic Acidosis: Postmarketing cases of Metformin Hydrochloride-associated lactic acidosis. If lactic acidosis is suspected, general supportive measures should be instituted promptly in a hospital setting, along with immediate discontinuation of this combination.

Hypotension: Before initiating this combination assess and correct volume status in patients with renal impairment, the elderly, in patients with low systolic blood pressure, and in patients on diuretics. Monitor for signs and symptoms of hypotension after initiating therapy and increase monitoring in clinical situations where volume contraction is expected.

Ketoacidosis: Before initiating this combination assess patients who present with signs and symptoms of metabolic acidosis for ketoacidosis, regardless of blood glucose level. If suspected, discontinue this combination, evaluate and treat promptly.

Acute kidney injury & impairment in renal function: Consider temporarily discontinuing this combination in settings of reduced oral intake or fluid losses. If acute kidney injury occurs, discontinue this combination promptly and institute treatment.

Urosepsis, Pyelonephritis, Fournier’s gangrene & Genital mycotic infections: Treatment with SGLT2 inhibitors increases the risk for urinary tract infections. Evaluate patients for signs and symptoms of urinary tract infections and treat promptly, if indicated.

Hypoglycemia: Consider lowering the dose of insulin secretagogue or insulin to reduce the risk of hypoglycemia when initiating this combination.

Vitamin B12 Deficiency: Metformin Hydrochloride may lower vitamin B12 levels. Monitor hematologic parameters annually.

Increased LDL-C: Monitor and treat as appropriate.

Macrovascular Outcomes: There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with this combination.

InteractionsView

Diuretics: Co-administration of Empagliflozin with diuretics resulted in increased urine volume and frequency of voids, which might enhance the potential for volume depletion.

Insulin or Insulin Secretagogues: Co-administration of Empagliflozin with insulin or insulin secretagogues increases the risk for hypoglycemia.

Positive Urine Glucose Test: Monitoring glycemic control with urine glucose tests is not recommended in patients taking SGLT2 inhibitors. Use alternative methods to monitor glycemic control.

Drugs that Reduce Metformin Clearance: Drugs that reduce Metformin clearance (such as ranolazine, vandetanib, dolutegravir, and cimetidine) may increase the accumulation of Metformin.

Carbonic Anhydrase Inhibitors: Carbonic anhydrase inhibitors may increase risk of lactic acidosis.

Drugs Affecting Glycemic Control: Thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid produce hoperglycemia. When such drugs are administered to a patient receiving Empagliflozin and Metformin combination, the patient should be closely observed to maintain adequate glycemic control. When such drugs are withdrawn from a patient receiving Empagliflozin and Metformin combination, the patient should be observed closely for hypoglycemia.

Alcohol: Alcohol can potentiate the effect of Metformin on lactate metabolism. Warn patients against excessive alcohol intake.

Pregnancy & lactationView

Advise females of the potential risk to a fetus especially during the second and third trimesters. This is not recommended when breastfeeding.

Overdose effectsView

In controlled clinical studies single doses of up to 800 mg Empagliflozin (equivalent to 32-times the highest recommended daily dose) in healthy volunteers and multiple daily doses of up to 100 mg Empagliflozin (equivalent to 4-times the highest recommended daily dose) in patients with type 2 diabetes did not show any toxicity. Hypoglycaemia has not been seen with Metformin doses of up to 85 g, although lactic acidosis has occurred in such circumstances. Lactic acidosis is a medical emergency and must be treated in hospital. In the event of an overdose, treatment should be initiated as appropriate to the patient's clinical status. The most effective method to remove lactate and Metformin is haemodialysis. The removal of Empagliflozin by haemodialysis has not been studied

StorageView

Keep below 30°C temperature, protected from light & moisture. Keep out of the reach of children.

Embelin

Ambrisentan

Tablet 5 mg Allopathic Anti-hypertensive

Indications

Pulmonary arterial hypertension

Indication detailsView

Ambrisentan is indicated for the treatment of Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise ability and delay clinical worsening.

Therapeutic classView

Anti-hypertensive, Endothelin receptor antagonist

PharmacologyView

Endothelin-1 (ET-1) is a potent autocrine and paracrine peptide. Two receptor subtypes, ET_A and ET_B, mediate the effects of ET-1 in the vascular smooth muscle and endothelium. The primary actions of ETA are vasoconstriction and cell proliferation, while the predominant actions of ETB are vasodilation, antiproliferation, and ET-1 clearance. Ambrisentan is a high-affinity ETA receptor antagonist with a high selectivity for the ET_A versus ET_B receptor (>4000-fold). The clinical impact of high selectivity for ET_A is not known.

The pharmacokinetics of Ambrisentan (S-Ambrisentan) in healthy subjects are dose proportional. The absolute bioavailability of Ambrisentan is not known. Ambrisentan is absorbed with peak concentrations occurring approximately 2 hours after oral administration in healthy subjects and PAH patients. Food does not affect its bioavailability. In vitro studies indicate that Ambrisentan is a substrate of P-gp. Ambrisentan is highly bound to plasma proteins (99%). The elimination of Ambrisentan is predominantly by non-renal pathways, but the relative contributions of metabolism and biliary elimination have not been well characterized. In plasma, the AUC of 4-hydroxymethyl Ambrisentan accounts for approximately 4% relative to parent Ambrisentan AUC. Thein vivo inversion of S-Ambrisentan to R-Ambrisentan is negligible. The mean oral clearance of Ambrisentan is 38 mL/min and 19 mL/min in healthy subjects and in PAH patients, respectively. Although Ambrisentan has a 15-hour terminal half-life, the mean trough concentration of Ambrisentan at steady-state is about 15% of the mean peak concentration and the accumulation factor is about 1.2 after long-term daily dosing, indicating that the effective half-life of Ambrisentan is about 9 hours.

DosageView

Adult dose: Initial treatment is 5 mg once daily, and can be increased to 10 mg once daily if 5 mg is tolerated. Ambrisentan may be administered with or without food.

Pediatric patients: The safety and effectiveness of Ambrisentan in pediatric patients have not been established.

Side effectsView

Decreases in hemoglobin concentration and hematocrit have followed administration of other endothelin receptor antagonists and were observed in clinical studies with Ambrisentan

ContraindicationsView

Ambrisentan may cause fetal harm when administered to a pregnant woman. Ambrisentan is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus. Pregnancy must be excluded before the initiation of treatment with Ambrisentan and prevented during treatment and for one month after stopping treatment. Ambrisentan is contraindicated in patients with Idiopathic Pulmonary Fibrosis (IPF) including IPF patients with pulmonary hypertension (WHO Group 3).

PrecautionsView

Fluid Retention: Peripheral edema is a known class effect of endothelin receptor antagonists, and is also a clinical consequence of PAH and worsening PAH.

Pulmonary Veno-occlusive Disease: If patients develop acute pulmonary edema during initiation of therapy with vasodilating agents such as Ambrisentan, the possibility of pulmonary veno-occlusive disease should be considered, and if con_rmed. Ambrisentan should be discontinued.

Hematological Changes: Decreases in hemoglobin concentration and hematocrit have followed administration of other endothelin receptor antagonists and were observed in clinical studies with Ambrisentan.

Hepatic impairment: Ambrisentan is not recommended in patients with moderate or severe hepatic impairment.

InteractionsView

Multiple dose co-administration of Ambrisentan and Cyclosporine resulted in an approximately 2-fold increase in Ambrisentan exposure in healthy volunteers; therefore, limit the dose of Ambrisentan to 5 mg once daily when co-administered with Cyclosporine.

Pregnancy & lactationView

Pregnancy Category X. It is not known whether Ambrisentan is excreted in human milk. Breastfeeding while receiving Ambrisentan is not recommended.

StorageView

Store in a cool and dry place, below 30°C. Protect from light and moisture.

Emcil

Pivmecillinam

Tablet 200 mg Allopathic Mecillinams

Indications

Shigellosis

Indication detailsView

Pivmecillinam is indicated for treatment of infections caused by mecillinam-sensitive organisms, e.g. acute cystitis, complicated urinary tract infections, salmonellosis, shigellosis, enteropathic E. coli diarrhoea, gram-negative septicaemia, billiary infections.

Therapeutic classView

Mecillinams

PharmacologyView

Pivmecillinam belongs to a new class of penicillin-the amdinopenicillin. Pivmecillinam is a prodrug formulation of mecillinam which allows the drug to be administered by mouth. The prodrug form lacks antibacterial activity, but the active drug is liberated by enzymatic hydrolysis during absorption in the gastrointestinal tract.

Pivmecillinam is bactericidal. It acts by interfering with bacterial cell wall synthesis, but the site of action differs from that of other penicilins. Pivmecillinam is very active against Enterobacteriaceae. It is active against E. coli, Klebsiella, Proteus, Enterobacter, Salmonella, Shigella and Yersinia. Pivmecillinam has poor activity against Gram- positive organisms. It has poor activity against Pseudomonas aeruginosa and has practically no activity against Enterococcus faecalis.

DosageView

Adults:

The usual dose: 1-2 tablets 3 times daily according to severity of the infection.
In acute uncomplicated cystitis: initially 400 mg then 200 mg every 8 hours for 3 days.
In chronic or recurrent bacteriurea: 400 mg 6-8 hours.
For the treatment of salmonellosis (including enteric fever): 1.2-2.4 gm daily for 14 days. To eliminate salmonella carriage, therapy may be prolonged for 2-4 weeks. In complicated urinary tract infection the usual treatment time is 1-2 weeks.
For prophylactic treatment of recurrent urinary tract infections: 1 tablet every evening is recommended.

Children:

Weighing less than 20 kg should be given 20-60 mg/kg divided into 3-4 daily doses. Those weighing more than 20 kg should receive normal adult dose.
In shigellosis: 20 mg/kg 4 times a day for 5 days.
For UTI: 20-40 mg/kg/day in 3-4 divided doses
For salmonellosis: 30-60 mg/kg/day in 3-4 divided doses

AdministrationView

The tablet should be taken with at least 50-100 ml fluid. As the bioavailability is practically unaffected by simultaneous food intake, This tablets are best taken with or immediately after a meal.

Side effectsView

Pivmecillinam is generally well tolerated, even by patients with reduced kidney function. Upper gastrointestinal disturbances such as nausea, vomiting and diarrhoea or indigestion may occur when a dose has been given on an empty stomach. Skin rashes have been reported in some cases, but the characteristic ampicillin-rash has never been observed, nor has there been any evidence of hepato-, nephro-, or ototoxicity. The occurrence of anaphylaxis, though not yet reported, cannot be entirely excluded.

ContraindicationsView

There have been no reports on allergy to Pivmecillinam among patients with a known history of hypersensitivity to penicillins and cephalosporins. Nevertheless, it seems reasonable to exclude such patients from treatment with Pivmecillinam until further experience has been gained.

PrecautionsView

As with other antibiotics, which are excreted mainly by the kidneys, raised blood levels of mecillinam may occur if repeated doses are given with impaired renal function.

Pregnancy & lactationView

Mecillinam concentrations approximately 1/3 of the serum levels have been found in the umbilical cord, and low but detectable amounts in the amniotic fluid. So, use of pivmecillinam in pregnancy should be avoided. Mecillinam is not excreted into the milk of lactating mother

Pediatric usageView

Based on information available to date for patients with impaired renal function, the initial dose can remain unchanged as can the interval between doses. However, the amount administered as the maintenance dose should be changed according to the following criteria:

CrCl 30 ml/min or greater: full dosage
CrCl 10-30 ml/min: 50% dosage
CrCl <10 ml/min: 25% dosage

Use of Pivmecillinam in infants under 3 months of age should be avoided.

Overdose effectsView

There is no experience with over dosage of pivmecillinam. However, excessive doses are likely to cause nausea, vomiting and gastritis. Treatment should be restricted to symptomatic and supportive measures. If necessary haemodialysis will reduce the blood level.

StorageView

Store at a cool and dry place, protect from light and moisture.

Emcon

Levonorgestrel

Tablet 0.75 mg Allopathic Emergency Contraceptive Pill

Indications

Oral contraceptives

Indication detailsView

Emergency contraception is a rescue method that is aimed to prevent fertilization in case of unprotected intercourse.

This contraception must be used as soon as possible, preferably within 12 hours and no later than 72 hours (3 days) after the unprotected sexual intercourse, particularly;

if you have had sexual intercourse whereas either yourself or your partner did not use a contraceptive method;
if you have forgotten to take consecutive 3 contraceptive pills;
if your partner's condom has broken, slipped, or been improperly removed, or if he has forgotten to use it;
if you fear that your intrauterine device has been expelled;
if your vaginal diaphragm or your contraceptive cap has moved or if you have removed it too early;
if you are afraid that the method of coitus interruptus has failed or if you have had sexual intercourse during the period when you are supposed to be fertile while using the rhythm method;
in the event of rape.

Therapeutic classView

Emergency Contraceptive Pill, Oral Contraceptive preparations

PharmacologyView

Oral contraceptives containing levonorgestrel suppress gonadotropins, inhibiting ovulation. Specifically, levonorgestrel binds to progesterone and androgen receptors and slows the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus. This process results in the suppression of the normal physiological luteinizing hormone (LH) surge that precedes ovulation. It inhibits the rupture of follicles and viable egg release from the ovaries. Levonorgestrel has been proven to be more effective when administered before ovulation.

DosageView

1.5 mg Tablet: The treatment necessitates the intake of one tablet. The Levonorgestrel tablet must be taken as soon as possible, preferably within 12 hours, after the unprotected intercourse, and no longer than within 72 hours (3 days) after the intercourse. Levonorgestrel can be taken at any moment during the menstrual cycle.

0.75 mg Tablet: The first Levonorgestrel tablet must be taken within 72 hours of the intercourse and the second tablet should be taken after 12 hours of the intake of the first tablet. Levonorgestrel must be taken within 48 hours of unprotected intercourse and in no way after 72 hours because the effectiveness of the medicine starts reducing after 48 hours of intercourse. Levonorgestrel can be taken at any moment during the menstrual cycle.

After using emergency contraception, it is recommended to use a local contraceptive mean (condom, spermicide, and cervical cap) until the next menstrual period resumes. The use of Levonorgestrel does not contraindicate the continuation of regular hormonal contraception. If you have used this medicine while you were using oral contraception (contraceptive pill), you should carry on taking the usual tablets until the end of the treatment. In case no menstrual period occurs in the next pill-free period following the use of Levonorgestrel a pregnancy test should be performed to rule out a pregnancy.

AdministrationView

Oral use. The tablet should be taken with a glass of water.

Side effectsView

Undesirable effects which have been observed are:

Nausea and vomiting
Dizziness, fatigue, headache
Abdominal pain
A feeling of breast tenderness
Bleeding can occur after taking this medicine

Inform the doctor of any unwanted effect which is not mentioned here.

ContraindicationsView

If you have hypersensitivity to levonorgestrel or any of the excipients of Levonorgestrel.

PrecautionsView

Emergency contraception must be used exceptionally, since:

It does not allow to prevent a pregnancy in every instance:
The associated hormonal overdosing is not advisable in the case of regular intake.
It cannot replace regular contraception.

After taking Levonorgestrel, the menstrual period usually occurs at the expected date nevertheless, it can occur earlier or later by a few days. After taking this medicine, it is therefore mandatory to check the absence of pregnancy by performing a pregnancy test in case of abnormal bleeding at the date of excepted menses or in case of menstrual delay of more than 5 days.

The use of emergency contraception does not replace the necessary precautions against sexually transmitted diseases and the measures to be taken in case of risk of transmission.

Taking this medicine is not recommended if you have had an ectopic pregnancy or if you have had salpingitis or if you have a severe digestive disease that impairs the absorption of medications.

If vomiting would occur within three hours after taking this medicine, it is recommended to take immediately another Levonorgestrel tablet.

InteractionsView

Interactions with other medicines and other forms of interaction: Simultaneous administration of certain anticonvulsant agents (phenobarbitone, phenytoin, primidone, carbamazepine), also other medications such as rifampicin, and griseofulvin can reduce or suppress the effectiveness of this emergency contraception.

Pregnancy & lactationView

This medicine is not indicated in case of pre-existing pregnancy and cannot interrupt it. In case of failure of this contraceptive mean persisting pregnancy, epidemiological studies indicate no adverse effects of progestogen on the malformation of a fetus. Lactation is possible. However, since levonorgestrel is secreted into breast milk, it is suggested that you breastfeed immediately before taking each Levonorgestrel tablet and that you skip the nursing following each Levonorgestrel administration.

Overdose effectsView

No acute toxicity has been demonstrated with this medicine in the case of intake of several doses. The efficacy of this medicine is not guaranteed if the dose has been omitted.

StorageView

Do not exceed the expiry date printed on the outer packaging. Keep the tablet in the outer carton. Keep the medicine away from children. Store in cool dry conditions (below 30° C).

Emcon 1

Levonorgestrel

Tablet 1.5 mg Allopathic Emergency Contraceptive Pill

Indications

Oral contraceptives

Indication detailsView

Emergency contraception is a rescue method that is aimed to prevent fertilization in case of unprotected intercourse.

This contraception must be used as soon as possible, preferably within 12 hours and no later than 72 hours (3 days) after the unprotected sexual intercourse, particularly;

if you have had sexual intercourse whereas either yourself or your partner did not use a contraceptive method;
if you have forgotten to take consecutive 3 contraceptive pills;
if your partner's condom has broken, slipped, or been improperly removed, or if he has forgotten to use it;
if you fear that your intrauterine device has been expelled;
if your vaginal diaphragm or your contraceptive cap has moved or if you have removed it too early;
if you are afraid that the method of coitus interruptus has failed or if you have had sexual intercourse during the period when you are supposed to be fertile while using the rhythm method;
in the event of rape.

Therapeutic classView

Emergency Contraceptive Pill, Oral Contraceptive preparations

PharmacologyView

Oral contraceptives containing levonorgestrel suppress gonadotropins, inhibiting ovulation. Specifically, levonorgestrel binds to progesterone and androgen receptors and slows the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus. This process results in the suppression of the normal physiological luteinizing hormone (LH) surge that precedes ovulation. It inhibits the rupture of follicles and viable egg release from the ovaries. Levonorgestrel has been proven to be more effective when administered before ovulation.

DosageView

1.5 mg Tablet: The treatment necessitates the intake of one tablet. The Levonorgestrel tablet must be taken as soon as possible, preferably within 12 hours, after the unprotected intercourse, and no longer than within 72 hours (3 days) after the intercourse. Levonorgestrel can be taken at any moment during the menstrual cycle.

0.75 mg Tablet: The first Levonorgestrel tablet must be taken within 72 hours of the intercourse and the second tablet should be taken after 12 hours of the intake of the first tablet. Levonorgestrel must be taken within 48 hours of unprotected intercourse and in no way after 72 hours because the effectiveness of the medicine starts reducing after 48 hours of intercourse. Levonorgestrel can be taken at any moment during the menstrual cycle.

After using emergency contraception, it is recommended to use a local contraceptive mean (condom, spermicide, and cervical cap) until the next menstrual period resumes. The use of Levonorgestrel does not contraindicate the continuation of regular hormonal contraception. If you have used this medicine while you were using oral contraception (contraceptive pill), you should carry on taking the usual tablets until the end of the treatment. In case no menstrual period occurs in the next pill-free period following the use of Levonorgestrel a pregnancy test should be performed to rule out a pregnancy.

AdministrationView

Oral use. The tablet should be taken with a glass of water.

Side effectsView

Undesirable effects which have been observed are:

Nausea and vomiting
Dizziness, fatigue, headache
Abdominal pain
A feeling of breast tenderness
Bleeding can occur after taking this medicine

Inform the doctor of any unwanted effect which is not mentioned here.

ContraindicationsView

If you have hypersensitivity to levonorgestrel or any of the excipients of Levonorgestrel.

PrecautionsView

Emergency contraception must be used exceptionally, since:

It does not allow to prevent a pregnancy in every instance:
The associated hormonal overdosing is not advisable in the case of regular intake.
It cannot replace regular contraception.

After taking Levonorgestrel, the menstrual period usually occurs at the expected date nevertheless, it can occur earlier or later by a few days. After taking this medicine, it is therefore mandatory to check the absence of pregnancy by performing a pregnancy test in case of abnormal bleeding at the date of excepted menses or in case of menstrual delay of more than 5 days.

The use of emergency contraception does not replace the necessary precautions against sexually transmitted diseases and the measures to be taken in case of risk of transmission.

Taking this medicine is not recommended if you have had an ectopic pregnancy or if you have had salpingitis or if you have a severe digestive disease that impairs the absorption of medications.

If vomiting would occur within three hours after taking this medicine, it is recommended to take immediately another Levonorgestrel tablet.

InteractionsView

Interactions with other medicines and other forms of interaction: Simultaneous administration of certain anticonvulsant agents (phenobarbitone, phenytoin, primidone, carbamazepine), also other medications such as rifampicin, and griseofulvin can reduce or suppress the effectiveness of this emergency contraception.

Pregnancy & lactationView

This medicine is not indicated in case of pre-existing pregnancy and cannot interrupt it. In case of failure of this contraceptive mean persisting pregnancy, epidemiological studies indicate no adverse effects of progestogen on the malformation of a fetus. Lactation is possible. However, since levonorgestrel is secreted into breast milk, it is suggested that you breastfeed immediately before taking each Levonorgestrel tablet and that you skip the nursing following each Levonorgestrel administration.

Overdose effectsView

No acute toxicity has been demonstrated with this medicine in the case of intake of several doses. The efficacy of this medicine is not guaranteed if the dose has been omitted.

StorageView

Do not exceed the expiry date printed on the outer packaging. Keep the tablet in the outer carton. Keep the medicine away from children. Store in cool dry conditions (below 30° C).

Emect

Ivermectin (Tablet)

Tablet 6 mg Allopathic Anthelmintic

Indication detailsView

Strongyloidiasis of the intestinal tract: Ivermectin is indicated for the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite Strongyloides stercoralis. This indication is based on clinical studies of both comparative and open-label designs, in which 64-100% of infected patients were cured following a single 200-mcg/kg dose of ivermectin.

Onchocerciasis: Ivermectin is indicated for the treatment of onchocerciasis due to the nematode parasite Onchocerca volvulus. This indication is based on randomized, double-blind, placebo-controlled and comparative studies conducted in 1427 patients in onchocerciasis-endemic areas of West Africa. The comparative studies used diethylcarbamazine citrate (DEC-C).

Therapeutic classView

Anthelmintic

PharmacologyView

Ivermectin selectively binds and with high affinity to glutamate-gated chloride ion channels, which occur in invertebrate nerve and muscle cells leading to an increase in the permeability of cell membranes to chloride ions with hyperpolarization of the nerve or muscle cell and, ultimately, death of the parasite.

DosageView

For Treatment (If COVIO Positive): 2 Tablets of Ivermectin 6 mg once daily for 5 days. (2+0+0 for 5 days).
For Prophylaxis: Single-dose as mentioned below to be taken on Day 1 & same dose on Day 7.

Body Weight 15-24 kg: 1 Tablet of Ivermectin 3 mg
Body Weight 25-35 kg: 1 Tablet of Ivermectin 6 mg
Body Weight 36-50 kg: 1 Tablet of Ivermectin 6 mg + 1 Tablet of Ivermectin 3 mg
Body Weight 51-65 kg: 2 Tablets of Ivermectin 6 mg
Body Weight 66-79 kg: 2 Tablets of Ivermectin 6 mg + 1 Tablet of Ivermectin 3 mg
Body Weight >80 kg: 3 Tablets of Ivermectin 6 mg

Strongyloidiasis: The recommended dosage of Ivermectin for the treatment of strongyloidiasis is a single oral dose designed to provide approximately 200 mcg/kg of body weight. Patients should take tablets on an empty stomach with water. In general, additional doses are not necessary. However, follow-up stool examinations should be performed to verify eradication of infection.

Dosage Guidelines for Ivermectin for Strongyloidiasis:

Body Weight (kg) 15-24: Dose 3 mg/kg
Body Weight (kg) 25-35: Dose 6 mg/kg
Body Weight (kg) 36-50: Dose 9 mg/kg
Body Weight (kg) 51-65: Dose 12 mg/kg
Body Weight (kg) 66-79: Dose 15 mg/kg
Body Weight (kg) >80: Dose 200 mcg/kg

Onchocerciasis: The recommended dosage of Ivermectin is a single oral dose designed to provide approximately 150 mcg of Ivermectin per kg of body weight on an empty stomach with water, the most commonly used dose interval is 12 months. For the treatment of individual patients, retreatment may be considered at intervals as short as 3 months.

Dosage Guidelines for Ivermectin for Onchocerciasis:

Body Weight (kg) 15-25: Dose 3 mg/kg
Body Weight (kg) 26-44: Dose 6 mg/kg
Body Weight (kg) 45-64: Dose 9 mg/kg
Body Weight (kg) 65-84: Dose 12 mg/kg
Body Weight (kg) >85: Dose 150 mcg/kg

Side effectsView

Strongyloidiasis: In four clinical studies involving a total of 109 patients given either one or two doses of 170 to 200 mcg/kg of Ivermectin, the following adverse reactions were reported as possibly, probably, or definitely related to Ivermectin.

Body as a whole: asthenia/fatigue (0.9%), abdominal pain (0.9%)
Gastrointestinal: anorexia (0.9%), constipation (0.9%), diarrhea (1.8%), nausea (1.8%), vomiting (0.9%) Nervous System/Psychiatric: dizziness (2.8%), somnolence (0.9%), vertigo (0.9%), tremor (0.9%)
Skin: pruritus (2.8%), rash (0.9%), and urticaria (0.9%).

Onchocerciasis: arthralgia/synovitis (19.3%), axillary lymph node enlargement and tenderness (11.0% and 4.4%, respectively), cervical lymph node enlargement and tenderness (5.3% and 1.2%, respectively), inguinal lymph node enlargement and tenderness (12.6% and 13.9%, respectively), other lymph node enlargement and tenderness (3.0% and 1.9%, respectively), pruritus (27.5%), skin involvement including edema, papular and pustular or frank urticarial rash (22.7%), and fever (22.6%), abnormal sensation in the eyes, eyelid edema, anterior uveitis, conjunctivitis, limbitis, keratitis, and chorioretinitis or choroiditis. These have rarely been severe or associated with loss of vision and have generally resolved without corticosteroid treatment. The following adverse reactions have been reported since the drug was registered overseas: hypotension (mainly orthostatic hypotension), worsening of bronchial asthma, toxic epidermal necrolysis, and Stevens-Johnson syndrome.

ContraindicationsView

It is contraindicated in patients who are hypersensitive to any component of this product.

PrecautionsView

Historical data have shown that microfilaricidal drugs, such as diethylcarbamazine citrate (DEC-C), might cause cutaneous and/or systemic reactions of varying severity (the Mazzotti reaction) and ophthalmological reactions in patients with onchocerciasis. These reactions are probably due to allergic and inflammatory responses to the death of microfilariae. Patients treated with Ivermectin for onchocerciasis may experience these reactions in addition to clinical adverse reactions possibly, probably, or definitely related to the drug itself. The treatment of severe Mazzotti reactions has not been subjected to controlled clinical trials. Oral hydration, recumbency, intravenous normal saline, and/or parenteral corticosteroids have been used to treat postural hypotension. Antihistamines and/or aspirin have been used for most mild to moderate cases. After treatment with microfilaricidal drugs, patients with hyperreactive onchodermatitis (sowda) may be more likely than others to experience severe adverse reactions, especially edema and aggravation of onchodermatitis. Rarely, patients with onchocerciasis who are also heavily infected with Loa loa may develop a serious or even fatal encephalopathy either spontaneously or following treatment with an effective microfilaricide. In these patients, the following adverse experiences have also been reported: back pain, conjunctival hemorrhage, dyspnea, urinary and/or fecal incontinence, difficulty in standing/walking, mental status changes, confusion, lethargy, stupor, or coma.

InteractionsView

Post-marketing reports of increased INR (International Normalized Ratio) have been rarely reported when ivermectin was co-administered with warfarin.

Pregnancy & lactationView

Pregnancy Category C. Ivermectin does not appear to be selectively fetotoxic to the developing fetus. There are, however, no adequate and well-controlled studies in pregnant women. Ivermectin should not be used during pregnancy since safety in pregnancy has not been established.

Nursing Mothers: Ivermectin is excreted in human milk in low concentrations. Treatment of mothers who intend to breast feed should only be undertaken when the risk of delayed treatment to the mother outweighs the possible risk to the newborn

Pediatric usageView

Pediatric Use: Safety and effectiveness in pediatric patients weighing less than 15 kg have not been established.

Geriatric Use: Clinical studies of Ivermectin did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.

StorageView

Keep in a dry place, below 30°C. Protect from light. Keep out of the reach of children.

Emectil

Chlorpromazine Hydrochloride

Syrup 25 mg/5 ml Allopathic Anti-emetic drugs

Indications

Vomiting

Indication detailsView

Chlorpromazine is indicated in the following conditions:

Schizophrenia and other psychoses (especially paranoid), mania and hypomania.
In anxiety psychomotor agitation excitement, violent or dangerously impulsive behaviour. Chlorpromazine is used as an adjunct in the short-term management of these conditions.
Intractable hiccup.
Nausea and vomiting of terminal illness (where other medicines have failed or are not available).
Childhood schizophrenia and autism.

Therapeutic classView

Anti-emetic drugs, Phenothiazine drugs, Phenothiazine related drugs

PharmacologyView

Chlorpromazine is a neuroleptic that acts by blocking the postsynaptic dopamine receptor in the mesolimbic dopaminergic system and inhibits the release of hypothalamic and hypophyseal hormones. It has antiemetic, serotonin-blocking, and weak antihistaminic properties and slight ganglion-blocking activity.

DosageView

Schizophrenia, Psychoses, Anxiety and Agitation

Oral-

Adult: Initially 25 mg three times daily or 75 mg at bedtime increasing by daily amounts of 25 mg to an effective maintenance dose. This is usually in the range 75 to 300 mg daily, but some patients may require up to 1 g daily.
Children: Under 1 Year: Do not use unless need is life saving. 1-5 Years: 0.5 mg/kg bodyweight every 4 - 6 hours to a maximum recommended dose of 40 mg daily. 6-12 Years: A third to half the adult dose, to a maximum recommended dose of 75 mg daily.
Elderly: Start with a third to a half the usual adult dose with a more gradual increase in dosage.

Intramuscular-

Adult: For acute relief of symptoms 25 - 50 mg every 6-8 hours.
Children: Under 1 Year: Do not use unless need is life saving. 1-5 Years: 0.5 mg/kg bodyweight every 6 - 8 hours. Dosage is not advised to exceed 40 mg daily. 6-12 Years: 0.5 mg/kg bodyweight every 6-8 hours. Not to exceed 75 mg daily.
Elderly: Doses in the lower range for adults should be sufficient to control symptoms, i.e. 25 mg, 8 hourly.

Intractable Hiccup (Adult)

Oral: 25-50 mg three or four times daily.
Intramuscular: 25-50 mg every 6-8 hours.
Intravenous Infusion: If other routes of administration are inappropriate, give 25-50 mg in 500-1000 ml sodium chloride by slow intravenous infusion every 6-8 hours.

Nausea and Vomiting of Terminal Illness

Oral-

Adults: 10-25 mg every 4-6 hours.
Children: Under 1 Year: Do not use unless need is life saving. 1-5 Years: 0.5 mg/kg every 4 - 6 hours. Maximum daily dosage should not exceed 40 mg. 6-12 Years: 0.5 mg/kg every 4 - 6 hours. Maximum daily dosage should not exceed 75 mg.
Elderly: Initially a third to half the adult dose. The physician should then use their clinical judgement to obtain control.

Intramuscular-

Adults: 25 mg initially, then 25 - 50 mg every 3 - 4 hours until vomiting stops, then drug to be taken orally.
Children: Under 1 Year: Do not use unless need is life saving. 1-5 Years: 0.5 mg/kg 6 - 8 hourly. It is advised that maximum daily dosage should not exceed 40 mg. 6-12 Years: 0.5 mg/kg every 6 - 8 hours. It is advised that maximum daily dosage should not exceed 75 mg.

AdministrationView

May be taken with or without food. May be taken with meals to reduce GI discomfort.

Side effectsView

The following adverse effects have been reported for chlorpromazine or phenothiazines in
general.

Cardiovascular: Postural hypotension, ECG Changes.
Dermatological
Contact dermatitis, photosensitivity, urticarial, maculopapular, petechial or oedematous reactions.
Endocrine: Elevated prolactin levels, impaired thermoregulation, hyperglycaemia, other hypothalamic effects.
Gastrointestinal: Dry mouth, constipation.
Immunological: Raised ANA titre, positive SLE cells.
Genitourinary: Urinary retention.
Haematological: Leucopenia, agranulocytosis, eosinophilia, hemolytic anaemia, aplastic anaemia, thrombocytopenic purpura and pancytopenia have been reported.

ContraindicationsView

Chlorpromazine should never be used in the following circumstances:

Circulatory collapse.
CNS depression, e.g. coma or drug intoxication.
Previous history of a hypersensitivity reaction (e.g. jaundice or blood dyscrasia) to phenothiazines, especially chlorpromazine itself, or to any of the excipients contained in the tablets or injection.
Bone marrow depression.
Phaeochromocytoma.
Hepatic failure or active hepatic disease.
Chlorpromazine Injection contains sodium metabisulfite and sodium sulfite and may cause allergic-type reactions including anaphylactic symptoms and asthmatic episodes in susceptible people.

PrecautionsView

Chlorpromazine generally should not be used in epilepsy, Parkinson’s disease, hypoparathyroidism, myasthenia gravis and prostatic hypertrophy.

InteractionsView

Interactions resulting in decreased chlorpromazine levels: Food, alcohol and benztropine can reduce the absorption of chlorpromazine. Antacids can slow the absorption of chlorpromazine. Lithium and chronic administration of barbiturates can lead to increased clearance of chlorpromazine.

Interactions resulting in increased chlorpromazine levels: Tricyclic antidepressants decrease the clearance of chlorpromazine and may lead to increased serum levels. Administration of chlorpromazine with CYP1A2 inhibitors, in particular strong (such as ciprofloxacin and fluvoxamine) or moderate (such as oral contraceptives and vemurafenib) inhibitors leads to an increase in chlorpromazine plasma concentrations. Therefore, patients may experience any chlorpromazine dose-dependent adverse drug reaction.

Pregnancy & lactationView

Pregnancy category C. Studies in animals by oral route have shown reproductive toxicity (dose-related embryo fetotoxicity: increased resorptions and dead foetuses). Increased incidence of malformations was observed in mice but only at doses inducing maternal mortality. There is inadequate animal data regarding reproductive toxicity with chlorpromazine by parenteral route. In humans, the teratogenic risk of chlorpromazine has not been evaluated. Different prospective epidemiological studies conducted with other phenothiazines have yielded contradictory results regarding teratogenic risk. Chlorpromazine has been found to be excreted in breast milk in variable amounts, therefore it is not recommended for nursing mothers unless the expected benefits outweigh any potential risk.

Pediatric usageView

Elderly: The elderly are relatively more susceptible to the adverse effects of chlorpromazine. The starting dose should be about half the usual adult dose and dosage increments should be gradual and reviewed regularly.

StorageView

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Emedon

Domperidone Maleate

Tablet 10 mg Allopathic Motility Stimulants

Indications

Vomiting

Indication detailsView

Dyspeptic symptom complex, often associated with delayed gastric emptying, gastroesophageal reflux and esophagitis:

Epigastric sense of fullness, feeling of abdominal distension, upper abdominal pain
Eructation, flatulence, early satiety
Nausea and vomiting
Heartburn with or without regurgitations of gastric contents in the mouth
Non-ulcer dyspepsia

Acute nausea and vomiting of the functional, organic, infectious, dietetic origin or induced by radiotherapy or drug therapy or induced in migraine.

Parkinson's disease: In dopamine-agonist induced nausea and vomiting.

Radiological studies: Speeding barium transit in follow-through radiological studies.

Therapeutic classView

Motility Stimulants, Motility stimulants/Dopamine antagonist, Prokinetic drugs

PharmacologyView

Domperidone is a dopamine antagonist that principally blocks the dopamine receptors located in the ChemoreceptorTrigger Zone (CTZ) and stomach. Its gastroprokinetic action is based on its blocking effect of dopamine receptors that have an influence on the motility of the gastrointestinal tract. Due to its weak penetration across the blood-brain barrier, Domperidone has almost no effect on the dopaminergic receptors in the brain, therefore, excluding psychotropic and neurologic side effects. Domperidone restores normal motility and tone of the upper gastrointestinal tract, facilitates gastric emptying, enhances antral and duodenal peristalsis and regulates contraction of the pylorus. Domperidone also increases esophageal peristalsis and lower esophageal sphincter pressure, and thus prevents regurgitation of gastric content.

DosageView

Domperidone should be taken 15-30 minutes before meals and, if necessary, before retiring.

The usual recommended oral dose of Domperidone is as follows:

Adults: 10-20 mg (1-2 tablet or 10-20 ml suspension), every 6-8 hours daily. The maximum dose of Domperidone is 80 mg daily.
Children: 2-4 ml suspension/10 kg body weight or 0.4-0.8 ml paediatric drops/10 kg body weight, every 6-8 hours daily.

In dyspeptic symptom:

Adults: 10-20 mg (1-2 tablet or 10-20 ml suspension), every 6-8 hours daily.
Children: 0.2-0.4 mg/kg (2-4 ml suspension/10 kg or 0.4-0.8 ml paediatric drops/10 kg) body weight, every 6-8 hours daily.

In acute and sub-acute conditions (mainly in acute nausea and vomiting):

Adults: 20 mg (2 tablets or 20 ml suspension), every 6-8 hours daily
Children: 0.2-0.4 mg/kg (2-4 ml suspension/10 kg or 0.4-0.8 ml paediatric drops/10 kg) body weight, every 6-8 hours daily. (In acute nausea and vomiting maximum period of treatment is 12 weeks).

By rectum in suppositories:

Adults (including elderly): 30-60 mg every 4-8 hours.
Children: The maximum daily dose rectally in children's is 30 mg for those weighting 10 to 25 kg. The dose may be divided throughout day if necessary.
The maximum period of treatment is 12 weeks.

Side effectsView

Domperidone may produce hyperprolactinemia (1.3%).This may result in galactorrhea, breast enlargement, and soreness and reduced libido. Dry mouth (1%), thirst, headache (1.2%), nervousness, drowsiness (0.4%), diarrhea (0.2%), skin rash and itching (0.1%) may occur during treatment with domperidone. Extra-pyramidal reactions are seen in 0.05% of patients in clinical studies.

ContraindicationsView

Domperidone is contraindicated to patients having known hypersensitivity to this drug and in the case of neonates. Domperidone should not be used whenever gastrointestinal stimulation might be dangerous i.e., gastrointestinal hemorrhage, mechanical obstruction or perforation. Also contraindicated in patients with prolactin releasing pituitary tumor (prolactinoma).

PrecautionsView

Domperidone should be used with absolute caution in the case of children because there may be an increased risk of extra-pyramidal reactions in young children because of an incompletely developed blood-brain barrier. Since domperidone is highly metabolized in liver, it should be used with caution in patient with hepatic impairment.

InteractionsView

Domperidone may reduce the risk of hypoprolactemic effect of bromocriptine. The action of Domperidone on Gl function may be antagonized by antimuscarinics and opoid analgesics. Care should be exercised when domperidone is administered in combination with MAO (monoamine oxidase) inhibitors.

Pregnancy & lactationView

The safety of domperidone has not been proven and it is therefore not recommended during pregnancy. Animal studies have not demonstrated the teratogenic effect in the fetus. Domperidone may precipitate galactorrhea and improve post-natal lactation. It is secreted in breast milk but in very small quantities insufficient to be considered harmful.

Overdose effectsView

There are no reported cases of overdose.

StorageView

Store below 30°C, Protected from light & moisture. Keep out of children's reach.

Emedox

Pyridoxine Hydrochloride + Doxylamine Succinate

Tablet (Extended Release) 20 mg+20 mg Allopathic Anti-emetic drugs

Indications

Pregnancy-associated nausea and vomiting

Indication detailsView

This is indicated for the treatment of nausea and vomiting of pregnancy in women who do not respond to conservative management.

Therapeutic classView

Anti-emetic drugs

PharmacologyView

Doxylamine Succinate is an antihistamine that blocks Histamine (H1) receptor. It can cross the blood brain barrier and has a high affinity for H1 receptors in the brain that blocks H1 receptors. It also decreases the action of histamine at the H1 receptor by inhibiting both vestibular system & Muscarinic receptor. It affects the vestibular system & decreases the stimulation of the vomiting center. Its muscarinic receptor inhibition may also play a role in antihistamine antiemetic activity. Pyridoxine Hydrochloride is a vitamin B6 analog. It is used to prevent nausea and vomiting due to its antiemetic properties.

DosageView

Initially, take one tablet orally at bedtime (Day 1). If this dose adequately controls symptoms the next day, continue taking one tablet daily at bedtime only. However, if symptoms persist on Day 2, increase the daily dose to one tablet in the morning and one tablet at bedtime. The maximum recommended dose is two tablets per day, one in the morning and one at bedtime. Take on an empty stomach with a glass of water. Swallow tablets whole. Do not crush, chew, or split this tablets. Take daily and not on an as needed basis.

Side effectsView

Somnolence or other accidents resulting from the effect of the combined use of Doxylamine Succinate & Pyridoxine Hydrochloride with CNS depressants.

ContraindicationsView

Doxylamine Succinate & Pyridoxine Hydrochloride is contraindicated in women with any of the following conditions:

Known hypersensitivity to Doxylamine Succinate, other ethanolamine derivative antihistamines, Pyridoxine Hydrochloride or any inactive ingredient in the formulation
Monoamine oxidase (MAO) inhibitors intensify and prolong the adverse central nervous system effects of Doxylamine Succinate & Pyridoxine Hydrochloride

PrecautionsView

Doxylamine Succinate & Pyridoxine Hydrochloride may cause somnolence due to the anticholinergic properties of Doxylamine Succinate, an antihistamine. Women should avoid engaging in activities, such as driving or operating heavy machinery, while using Doxylamine Succinate & Pyridoxine Hydrochloride. Doxylamine Succinate & Pyridoxine Hydrochloride use is not recommended if a woman is concurrently using central nervous system (CNS) depressants including alcohol.

Doxylamine Succinate & Pyridoxine Hydrochloride has anticholinergic properties and, therefore, should be used with caution in women with asthma, increased intraocular pressure, narrow angle glaucoma, stenosing peptic ulcer, pyloroduodenal obstruction or urinary bladder-neck obstruction.

InteractionsView

Use of Doxylamine Succinate & Pyridoxine Hydrochloride is contraindicated in women who are taking monoamine oxidase inhibitors (MAOIs), which prolong and intensify the adverse central nervous system effects (the anticholinergic effects) of antihistamines. Concurrent use of alcohol and other CNS depressants (such as hypnotic sedatives and tranquilizers) with Doxylamine Succinate & Pyridoxine Hydrochloride is not recommended.

Pregnancy & lactationView

Pregnancy category A. This is intended for the treatment of nausea and vomiting of pregnancy in women who do not respond to conservative management. Both Doxylamine Succinate & Pyridoxine Hydrochloride are excreted into breast milk. Therefore, caution should be exercised while breastfeeding.

Overdose effectsView

Doxylamine Succinate & Pyridoxine Hydrochloride is an extended-release or Delayed Release formulation; therefore, signs and symptoms of intoxication may not be apparent immediately. Signs and symptoms of overdose may include restlessness, dryness of mouth, dilated pupils, sleepiness, vertigo, mental confusion and tachycardia. At toxic doses, Doxylamine Succinate exhibits anticholinergic effects, including seizures, rhabdomyolysis, acute renal failure and death. If treatment is needed, it consists of gastric lavage or activated charcoal, whole bowel irrigation and symptomatic treatment.

StorageView

Store at below 30°C in a dry place protected from light. Keep out of reach of children.

Emego Plus

Meclizine + Pyridoxine

Tablet 25 mg+50 mg Allopathic Anti-emetic drugs

Indications

Pregnancy-associated nausea and vomiting

Indication detailsView

Prevention and treatment of nausea, vomiting, dizziness, motion sickness, radiation sickness and vertigo associated with diseases of the vestibular system (e.g. Meniere's syndrome, labyrinthitis and other vestibular disturbances).

Therapeutic classView

Anti-emetic drugs

PharmacologyView

Meclizine is a piperazine-derivative antihistamine that is used as an antiemetic. It has antiemetic, anticholinergic and antihistaminic properties. It reduces the sensitivity of the labyrinthine apparatus. The action may be mediated through nerve pathways to the vomiting center (VC) from the chemoreceptor trigger zone (CTZ), peripheral nerve pathways, the VC, or other CNS centers. Pyridoxine is vitamin B-6. It has been added to enhance the anti-emetic effects & as a dietary suppliment.

DosageView

Adult and Children 12 years of age & over:

Nausea and vomiting: 25-50 mg daily or as directed by a physician.
Motion sickness: Take an initial dose of 25-50 mg, 1 hour prior to travel. May repeat the dose every 24 hours for the duration of the journey.
Radiation sickness: 50 mg administered 2-12 hours prior to radiation treatment.
Vertigo: 25-100 mg daily in divided doses.
Prevention of nausea and vomiting associated with emergency contraceptive pill (ECP): 25-50 mg, 1 hour before first ECP dose; repeat if needed in 24 hours.

The safety and efficacy for use in children less than 12 years of age have not been established.

Side effectsView

Drowsiness, dry mouth and, on rare occasions, blurred vision have been reported.

ContraindicationsView

Meclizine Hydrochloride and Pyridoxine Hydrochloride is contraindicated in patients who are hypersensitive to these ingredients.

PrecautionsView

Patients should be warned that Meclizine Hydrochloride may impair their ability to perform hazardous activities requiring mental alertness or physical coordination (e.g., operating machinery, driving a motor vehicle). Patients should avoid alcoholic beverages while taking this drug. Due to its potential anticholinergic action, this drug should be used with caution in patients with asthma, glaucoma or enlargement of the prostate gland.

InteractionsView

The CNS depressant effects of Meclizine can be potentiated by concurrent use of Ethanol or other CNS depressant agents such as Benzodiazepines, Barbiturates, Tricyclic antidepressants, opiate agonists, skeletal muscle relaxants and antihistamines. Concurrent use of other anticholinergics can potentiate the anticholinergic effects of Meclizine. Meclizine can increase the absorption of digoxin by decreasing gastrointestinal motility.

Pregnancy & lactationView

Pregnancy Category B. Large-scale human studies have not demonstrated adverse fetal effects. It has been suggested that based on available data, Meclizine presents the lowest risk of teratogenicity and is the drug of first choice in treating nausea and vomiting during pregnancy. Safety for use in the nursing mother has not been established.

Overdose effectsView

Symptoms: Extreme excitability, seizures, drowsiness and hallucinations.
Treatment: Appropriate supportive and symptomatic treatment. Consider dialysis

StorageView

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.