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Emend
Aprepitant
Emend
Aprepitant
Indications
Nausea and vomiting
Indication detailsView
Aprepitant is indicated for-
- Prevention of postoperative nausea and vomiting (PONV)
- Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Aprepitant is a selective high affinity antagonist of human substance P neurokinin 1 (NK1) receptors. When substance P attaches to these receptors, it causes nausea and vomiting. Aprepitant stops substance P from binding to the NK1 receptors. By blocking the receptors, Aprepitant can prevent nausea and vomiting, which often happens after chemotherapy or as a complication of surgery.
DosageView
Post Operative Nausea and Vomiting: The recommended oral dosage of Aprepitant is 40 mg within 3 hours prior to induction of anesthesia.
Chemotherapy-Induced Nausea and Vomiting:
** The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy-
** The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
Chemotherapy-Induced Nausea and Vomiting:
** The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy-
- Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): 24 mg 30 minutes before the start of chemotherapy.
- Day 2: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
- Day 3: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
- Day 4: Dexamethasone 8 mg orally
** The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
- Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): one 8 mg tablet 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later.
- Day 2: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day
- Day 3: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day.
AdministrationView
Aprepitant may be taken with or without food. No dosage adjustment is necessary for the elderly patients.
Side effectsView
Constipation, Hypotension, Pruritus, Pyrexia
ContraindicationsView
Aprepitant is contraindicated in patients who are hypersensitive to any component of the product. Aprepitant should not be used concurrently with Pimozide, Terfenadine, Astemizole & Cisapride.
InteractionsView
Aprepitant is a substrate, a weak-to-moderate (dose dependent) inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9. Precautions should be taken while coadministering Aprepitant with drugs that use CYP3A4 or CYP2C9, for example- Warfarin, Tolbutamide, Phenytoin, Ketoconazole, Itraconazole, Nefazodone, Troleandomycin, Clarithromycin, Ritonavir, Nelfinavir, Diltiazem, Rifampin, Carbamazepine etc.
Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or back-up methods of contraception should be used during treatment with Aprepitant and for 1 month following the last dose of Aprepitant.
Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or back-up methods of contraception should be used during treatment with Aprepitant and for 1 month following the last dose of Aprepitant.
Pregnancy & lactationView
Pregnancy Category B. This drug should be used during pregnancy only if clearly needed. It is not known whether this drug is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug based on patient’s importance.
Pediatric usageView
Patients with Renal Impairment: No dosage adjustment is necessary for patients with renal impairment or for patients with end-stage renal disease (ESRD) undergoing hemodialysis.
Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment.
Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment.
Overdose effectsView
No specific information is available on the treatment of overdosage with Aprepitant. Single doses up to 600 mg of Aprepitant were generally well tolerated in healthy subjects. Drowsiness and headache can be seen due to overdose. In the event of overdose, Aprepitant should be discontinued. General supportive treatment and monitoring should be provided. Because of the antiemetic activity of Aprepitant, medicine-induced emesis may not be effective. Aprepitant cannot be removed by hemodialysis.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Emend
Aprepitant
Emend
Aprepitant
Indications
Nausea and vomiting
Indication detailsView
Aprepitant is indicated for-
- Prevention of postoperative nausea and vomiting (PONV)
- Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Aprepitant is a selective high affinity antagonist of human substance P neurokinin 1 (NK1) receptors. When substance P attaches to these receptors, it causes nausea and vomiting. Aprepitant stops substance P from binding to the NK1 receptors. By blocking the receptors, Aprepitant can prevent nausea and vomiting, which often happens after chemotherapy or as a complication of surgery.
DosageView
Post Operative Nausea and Vomiting: The recommended oral dosage of Aprepitant is 40 mg within 3 hours prior to induction of anesthesia.
Chemotherapy-Induced Nausea and Vomiting:
** The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy-
** The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
Chemotherapy-Induced Nausea and Vomiting:
** The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy-
- Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): 24 mg 30 minutes before the start of chemotherapy.
- Day 2: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
- Day 3: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
- Day 4: Dexamethasone 8 mg orally
** The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
- Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): one 8 mg tablet 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later.
- Day 2: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day
- Day 3: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day.
AdministrationView
Aprepitant may be taken with or without food. No dosage adjustment is necessary for the elderly patients.
Side effectsView
Constipation, Hypotension, Pruritus, Pyrexia
ContraindicationsView
Aprepitant is contraindicated in patients who are hypersensitive to any component of the product. Aprepitant should not be used concurrently with Pimozide, Terfenadine, Astemizole & Cisapride.
InteractionsView
Aprepitant is a substrate, a weak-to-moderate (dose dependent) inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9. Precautions should be taken while coadministering Aprepitant with drugs that use CYP3A4 or CYP2C9, for example- Warfarin, Tolbutamide, Phenytoin, Ketoconazole, Itraconazole, Nefazodone, Troleandomycin, Clarithromycin, Ritonavir, Nelfinavir, Diltiazem, Rifampin, Carbamazepine etc.
Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or back-up methods of contraception should be used during treatment with Aprepitant and for 1 month following the last dose of Aprepitant.
Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or back-up methods of contraception should be used during treatment with Aprepitant and for 1 month following the last dose of Aprepitant.
Pregnancy & lactationView
Pregnancy Category B. This drug should be used during pregnancy only if clearly needed. It is not known whether this drug is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug based on patient’s importance.
Pediatric usageView
Patients with Renal Impairment: No dosage adjustment is necessary for patients with renal impairment or for patients with end-stage renal disease (ESRD) undergoing hemodialysis.
Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment.
Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment.
Overdose effectsView
No specific information is available on the treatment of overdosage with Aprepitant. Single doses up to 600 mg of Aprepitant were generally well tolerated in healthy subjects. Drowsiness and headache can be seen due to overdose. In the event of overdose, Aprepitant should be discontinued. General supportive treatment and monitoring should be provided. Because of the antiemetic activity of Aprepitant, medicine-induced emesis may not be effective. Aprepitant cannot be removed by hemodialysis.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Emenil Plus
Meclizine + Pyridoxine
Emenil Plus
Meclizine + Pyridoxine
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.
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
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.
Emep
Esomeprazole
Emep
Esomeprazole
Indication detailsView
Esomeprazole is indicated:
- To relieve from chronic heartburn symptoms and other symptoms associated with GERD
- For the healing of erosive esophagitis
- For maintenance of healing of erosive esophagitis
- In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
- Zollinger-Ellison Syndrome
- Acid related Dyspepsia
- Duodenal & Gastric ulcer
PharmacologyView
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
DosageView
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don't heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.
Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.
AdministrationView
Esomeprazole tablet or capsule: should be swallowed whole and taken one hour before a meal.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Side effectsView
The most frequently occurring adverse events reported with Esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.
ContraindicationsView
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.
PrecautionsView
General: Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
InteractionsView
Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Esomeprazole does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.
Pediatric usageView
Paediatric Use: Safety and effectiveness in paediatric patients have not been established.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Overdose effectsView
A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Esomeprazole. No specific antidote for Esomeprazole is known. Since Esomeprazole is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.
ReconstitutionView
Infusion: Reconstitute one sterile single-dose vial of Esomeprazole IV Injection with 5 ml of the solvent (WFI) provided and further diluting the resulting solution within 0.9% Sodium Chloride solution or 5% Dextrose solution to make a final volume of 50 ml. The resultant infusion should be given intravenously over a period of 10-30 minutes. Chemical and physical in-use stability has been demonstrated for 12 hours after reconstitution with 0.9% Sodium Chloride solution or for 6 hours after reconstitution with 5% Dextrose solution. From a microbial point of view, the product should be used immediately. Any unused portion should be discarded.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.
Emep
Esomeprazole
Emep
Esomeprazole
Indication detailsView
Esomeprazole is indicated:
- To relieve from chronic heartburn symptoms and other symptoms associated with GERD
- For the healing of erosive esophagitis
- For maintenance of healing of erosive esophagitis
- In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
- Zollinger-Ellison Syndrome
- Acid related Dyspepsia
- Duodenal & Gastric ulcer
PharmacologyView
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
DosageView
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don't heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.
Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.
AdministrationView
Esomeprazole tablet or capsule: should be swallowed whole and taken one hour before a meal.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Side effectsView
The most frequently occurring adverse events reported with Esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.
ContraindicationsView
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.
PrecautionsView
General: Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
InteractionsView
Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Esomeprazole does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.
Pediatric usageView
Paediatric Use: Safety and effectiveness in paediatric patients have not been established.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Overdose effectsView
A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Esomeprazole. No specific antidote for Esomeprazole is known. Since Esomeprazole is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.
ReconstitutionView
Infusion: Reconstitute one sterile single-dose vial of Esomeprazole IV Injection with 5 ml of the solvent (WFI) provided and further diluting the resulting solution within 0.9% Sodium Chloride solution or 5% Dextrose solution to make a final volume of 50 ml. The resultant infusion should be given intravenously over a period of 10-30 minutes. Chemical and physical in-use stability has been demonstrated for 12 hours after reconstitution with 0.9% Sodium Chloride solution or for 6 hours after reconstitution with 5% Dextrose solution. From a microbial point of view, the product should be used immediately. Any unused portion should be discarded.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.
Emep
Esomeprazole
Emep
Esomeprazole
Indication detailsView
Esomeprazole is indicated:
- To relieve from chronic heartburn symptoms and other symptoms associated with GERD
- For the healing of erosive esophagitis
- For maintenance of healing of erosive esophagitis
- In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
- Zollinger-Ellison Syndrome
- Acid related Dyspepsia
- Duodenal & Gastric ulcer
PharmacologyView
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
DosageView
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don't heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.
Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.
AdministrationView
Esomeprazole tablet or capsule: should be swallowed whole and taken one hour before a meal.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Side effectsView
The most frequently occurring adverse events reported with Esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.
ContraindicationsView
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.
PrecautionsView
General: Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
InteractionsView
Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Esomeprazole does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.
Pediatric usageView
Paediatric Use: Safety and effectiveness in paediatric patients have not been established.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Overdose effectsView
A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Esomeprazole. No specific antidote for Esomeprazole is known. Since Esomeprazole is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.
ReconstitutionView
Infusion: Reconstitute one sterile single-dose vial of Esomeprazole IV Injection with 5 ml of the solvent (WFI) provided and further diluting the resulting solution within 0.9% Sodium Chloride solution or 5% Dextrose solution to make a final volume of 50 ml. The resultant infusion should be given intravenously over a period of 10-30 minutes. Chemical and physical in-use stability has been demonstrated for 12 hours after reconstitution with 0.9% Sodium Chloride solution or for 6 hours after reconstitution with 5% Dextrose solution. From a microbial point of view, the product should be used immediately. Any unused portion should be discarded.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.
Emep
Esomeprazole
Emep
Esomeprazole
Indication detailsView
Esomeprazole is indicated:
- To relieve from chronic heartburn symptoms and other symptoms associated with GERD
- For the healing of erosive esophagitis
- For maintenance of healing of erosive esophagitis
- In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
- Zollinger-Ellison Syndrome
- Acid related Dyspepsia
- Duodenal & Gastric ulcer
PharmacologyView
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
Absorption: Esomeprazole capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once daily dosing, the systemic bioavailability is approximately 90% compared to 64% after a single dose. The AUC after administration of a single dose of esomeprazole is decreased by 33-53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack anti-secretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite.
Excretion: The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the faeces.
Combination Therapy with Antimicrobials: Esomeprazole magnesium 40 mg once daily is given in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. The mean steady state AUC and Cmax of Esomeprazole increased by 70% and 18%, respectively, during triple combination therapy compared to treatment with Esomeprazole alone. The pharmacokinetic parameters for clarithromycin and amoxicillin are similar during triple combination therapy and administration of each drug alone. However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by 19% and 22%, respectively, during triple combination therapy compared to treatment with clarithromycin alone. This increase in exposure to 14-hydroxyclarithromycin is not considered to be clinically significant.
DosageView
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don't heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.
Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.
AdministrationView
Esomeprazole tablet or capsule: should be swallowed whole and taken one hour before a meal.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Direction for use of Delayed-Release Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.
Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.
Side effectsView
The most frequently occurring adverse events reported with Esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.
ContraindicationsView
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.
PrecautionsView
General: Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
Information for patients: Esomeprazole capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Esomeprazole capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking esomeprazole.
InteractionsView
Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Esomeprazole does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Esomeprazole.
Combination Therapy with Clarithromycin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Pregnancy & lactationView
There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.
Pediatric usageView
Paediatric Use: Safety and effectiveness in paediatric patients have not been established.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out
Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.
Renal Insufficiency: The Pharmacokinetics of Esomeprazole in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Esomeprazole is excreted unchanged in the urine.
Overdose effectsView
A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Esomeprazole. No specific antidote for Esomeprazole is known. Since Esomeprazole is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.
ReconstitutionView
Infusion: Reconstitute one sterile single-dose vial of Esomeprazole IV Injection with 5 ml of the solvent (WFI) provided and further diluting the resulting solution within 0.9% Sodium Chloride solution or 5% Dextrose solution to make a final volume of 50 ml. The resultant infusion should be given intravenously over a period of 10-30 minutes. Chemical and physical in-use stability has been demonstrated for 12 hours after reconstitution with 0.9% Sodium Chloride solution or for 6 hours after reconstitution with 5% Dextrose solution. From a microbial point of view, the product should be used immediately. Any unused portion should be discarded.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.
Emer
Phenobarbital
Emer
Phenobarbital
Indications
Tonic-clonic status epilepticus
Indication detailsView
Phenobarbital is indicated for the following conditions:
- Sedatives
- Hypnotics for the short-term treatment of insomnia
- Pre-anesthetics
- Long-term anticonvulsants for the treatment of generalized tonic-clonic and cortical local seizures. And, in the emergency control of certain acute convulsive episodes, (those associated with status epilepticus, eclampsia meningitis, tetanus, and toxic reactions to Strychnine or local anesthetics).
Therapeutic classView
Adjunct anti-epileptic drugs, Barbiturates
PharmacologyView
Phenobarbital, the longest-acting barbiturate, is used for its anticonvulsant and sedative-hypnotic properties in the management of all seizure disorders except absence (petit mal). Phenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.
DosageView
Suggested doses of Phenobarbital for specific indications are as follows:
Pediatric Oral Dosage:
Pediatric Oral Dosage:
- Preoperative: 1 mg to 3 mg/kg.
- Anticonvulsant: 1 mg to 6 mg/kg per day
- Daytime sedative: 30 mg to 120 mg daily in 2 to 3 divided doses.
- Bedtime hypnotic: 100 mg to 320 mg.
- Anticonvulsant: 50 mg to 100 mg 2 to 3 times daily.
- 15 to 20 mg/kg IV over 10 to 15 min.
- Preoperative Sedation:1 to 3 mg/kg IM/IV;
- Anticonvulsant: 4 to 6 mg/kg IM/IV per day, for 10 days. Alternatively, use 10 to 15 mg/kg IM/IV per day to reach therapeutic level more quickly. Maxium IV rate 60 mg/min.
- Insomnia: 100 to 320 mg IM/IV;
- Convulsions: 100 to 320 mg IV. Repeat if needed (maximum, 600 mg per day);
- Status Epilepticus: 10 to 20 mg/kg IV. Repeat if needed.
Side effectsView
The most common adverse reaction is somnolence. Other less frequent adverse reactions are agitation, confusion, hyperkinesia, ataxia, CNS depression, nightmares, nervousness, psychiatric disturbance, hallucinations, insomnia, anxiety, dizziness, thinking abnormality, apnea, bradycardia, hypotension, nausea, vomiting and constipation.
ContraindicationsView
Phenobarbital is contraindicated in patients with known Phenobarbital sensitivity or a history of latent porphyria.
PrecautionsView
Tolerance and psychological and physical dependence may occur with continuing use. Phenobarbital should be administered with caution to patients who are mentally depressed, have suicidal tendencies, or a history of drug abuse. In patients with hepatic damage, Phenobarbital should be administered with caution and initially reduced doses.
InteractionsView
The concomitant use of Alcohol or other CNS depressants may produce additive CNS depressant effects.
Pregnancy & lactationView
Pregnancy Category D. Phenobarbital can cause fetal damage when administered to a pregnant woman. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be in risk of the potential hazard to the fetus. Caution should be taken when Phenobarbital is administered to a nursing woman since small amounts of Phenobarbital are excreted in the milk.
Overdose effectsView
The toxic dose of barbiturates varies considerably. In general, an oral dose of 1 gram of most barbiturates produces serious poisoning in an adult. Death commonly occurs after 2 to 10 grams of ingested barbiturate. Acute overdosage with barbiturates is manifested by CNS and respiratory depression Treatment of overdosage is mainly supportive and immediate hospitalization is necessary.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Emer
Phenobarbital
Emer
Phenobarbital
Indications
Tonic-clonic status epilepticus
Indication detailsView
Phenobarbital is indicated for the following conditions:
- Sedatives
- Hypnotics for the short-term treatment of insomnia
- Pre-anesthetics
- Long-term anticonvulsants for the treatment of generalized tonic-clonic and cortical local seizures. And, in the emergency control of certain acute convulsive episodes, (those associated with status epilepticus, eclampsia meningitis, tetanus, and toxic reactions to Strychnine or local anesthetics).
Therapeutic classView
Adjunct anti-epileptic drugs, Barbiturates
PharmacologyView
Phenobarbital, the longest-acting barbiturate, is used for its anticonvulsant and sedative-hypnotic properties in the management of all seizure disorders except absence (petit mal). Phenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.
DosageView
Suggested doses of Phenobarbital for specific indications are as follows:
Pediatric Oral Dosage:
Pediatric Oral Dosage:
- Preoperative: 1 mg to 3 mg/kg.
- Anticonvulsant: 1 mg to 6 mg/kg per day
- Daytime sedative: 30 mg to 120 mg daily in 2 to 3 divided doses.
- Bedtime hypnotic: 100 mg to 320 mg.
- Anticonvulsant: 50 mg to 100 mg 2 to 3 times daily.
- 15 to 20 mg/kg IV over 10 to 15 min.
- Preoperative Sedation:1 to 3 mg/kg IM/IV;
- Anticonvulsant: 4 to 6 mg/kg IM/IV per day, for 10 days. Alternatively, use 10 to 15 mg/kg IM/IV per day to reach therapeutic level more quickly. Maxium IV rate 60 mg/min.
- Insomnia: 100 to 320 mg IM/IV;
- Convulsions: 100 to 320 mg IV. Repeat if needed (maximum, 600 mg per day);
- Status Epilepticus: 10 to 20 mg/kg IV. Repeat if needed.
Side effectsView
The most common adverse reaction is somnolence. Other less frequent adverse reactions are agitation, confusion, hyperkinesia, ataxia, CNS depression, nightmares, nervousness, psychiatric disturbance, hallucinations, insomnia, anxiety, dizziness, thinking abnormality, apnea, bradycardia, hypotension, nausea, vomiting and constipation.
ContraindicationsView
Phenobarbital is contraindicated in patients with known Phenobarbital sensitivity or a history of latent porphyria.
PrecautionsView
Tolerance and psychological and physical dependence may occur with continuing use. Phenobarbital should be administered with caution to patients who are mentally depressed, have suicidal tendencies, or a history of drug abuse. In patients with hepatic damage, Phenobarbital should be administered with caution and initially reduced doses.
InteractionsView
The concomitant use of Alcohol or other CNS depressants may produce additive CNS depressant effects.
Pregnancy & lactationView
Pregnancy Category D. Phenobarbital can cause fetal damage when administered to a pregnant woman. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be in risk of the potential hazard to the fetus. Caution should be taken when Phenobarbital is administered to a nursing woman since small amounts of Phenobarbital are excreted in the milk.
Overdose effectsView
The toxic dose of barbiturates varies considerably. In general, an oral dose of 1 gram of most barbiturates produces serious poisoning in an adult. Death commonly occurs after 2 to 10 grams of ingested barbiturate. Acute overdosage with barbiturates is manifested by CNS and respiratory depression Treatment of overdosage is mainly supportive and immediate hospitalization is necessary.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Emer
Phenobarbital
Emer
Phenobarbital
Indications
Tonic-clonic status epilepticus
Indication detailsView
Phenobarbital is indicated for the following conditions:
- Sedatives
- Hypnotics for the short-term treatment of insomnia
- Pre-anesthetics
- Long-term anticonvulsants for the treatment of generalized tonic-clonic and cortical local seizures. And, in the emergency control of certain acute convulsive episodes, (those associated with status epilepticus, eclampsia meningitis, tetanus, and toxic reactions to Strychnine or local anesthetics).
Therapeutic classView
Adjunct anti-epileptic drugs, Barbiturates
PharmacologyView
Phenobarbital, the longest-acting barbiturate, is used for its anticonvulsant and sedative-hypnotic properties in the management of all seizure disorders except absence (petit mal). Phenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.
DosageView
Suggested doses of Phenobarbital for specific indications are as follows:
Pediatric Oral Dosage:
Pediatric Oral Dosage:
- Preoperative: 1 mg to 3 mg/kg.
- Anticonvulsant: 1 mg to 6 mg/kg per day
- Daytime sedative: 30 mg to 120 mg daily in 2 to 3 divided doses.
- Bedtime hypnotic: 100 mg to 320 mg.
- Anticonvulsant: 50 mg to 100 mg 2 to 3 times daily.
- 15 to 20 mg/kg IV over 10 to 15 min.
- Preoperative Sedation:1 to 3 mg/kg IM/IV;
- Anticonvulsant: 4 to 6 mg/kg IM/IV per day, for 10 days. Alternatively, use 10 to 15 mg/kg IM/IV per day to reach therapeutic level more quickly. Maxium IV rate 60 mg/min.
- Insomnia: 100 to 320 mg IM/IV;
- Convulsions: 100 to 320 mg IV. Repeat if needed (maximum, 600 mg per day);
- Status Epilepticus: 10 to 20 mg/kg IV. Repeat if needed.
Side effectsView
The most common adverse reaction is somnolence. Other less frequent adverse reactions are agitation, confusion, hyperkinesia, ataxia, CNS depression, nightmares, nervousness, psychiatric disturbance, hallucinations, insomnia, anxiety, dizziness, thinking abnormality, apnea, bradycardia, hypotension, nausea, vomiting and constipation.
ContraindicationsView
Phenobarbital is contraindicated in patients with known Phenobarbital sensitivity or a history of latent porphyria.
PrecautionsView
Tolerance and psychological and physical dependence may occur with continuing use. Phenobarbital should be administered with caution to patients who are mentally depressed, have suicidal tendencies, or a history of drug abuse. In patients with hepatic damage, Phenobarbital should be administered with caution and initially reduced doses.
InteractionsView
The concomitant use of Alcohol or other CNS depressants may produce additive CNS depressant effects.
Pregnancy & lactationView
Pregnancy Category D. Phenobarbital can cause fetal damage when administered to a pregnant woman. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be in risk of the potential hazard to the fetus. Caution should be taken when Phenobarbital is administered to a nursing woman since small amounts of Phenobarbital are excreted in the milk.
Overdose effectsView
The toxic dose of barbiturates varies considerably. In general, an oral dose of 1 gram of most barbiturates produces serious poisoning in an adult. Death commonly occurs after 2 to 10 grams of ingested barbiturate. Acute overdosage with barbiturates is manifested by CNS and respiratory depression Treatment of overdosage is mainly supportive and immediate hospitalization is necessary.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Emer
Phenobarbital
Emer
Phenobarbital
Indications
Tonic-clonic status epilepticus
Indication detailsView
Phenobarbital is indicated for the following conditions:
- Sedatives
- Hypnotics for the short-term treatment of insomnia
- Pre-anesthetics
- Long-term anticonvulsants for the treatment of generalized tonic-clonic and cortical local seizures. And, in the emergency control of certain acute convulsive episodes, (those associated with status epilepticus, eclampsia meningitis, tetanus, and toxic reactions to Strychnine or local anesthetics).
Therapeutic classView
Adjunct anti-epileptic drugs, Barbiturates
PharmacologyView
Phenobarbital, the longest-acting barbiturate, is used for its anticonvulsant and sedative-hypnotic properties in the management of all seizure disorders except absence (petit mal). Phenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.
DosageView
Suggested doses of Phenobarbital for specific indications are as follows:
Pediatric Oral Dosage:
Pediatric Oral Dosage:
- Preoperative: 1 mg to 3 mg/kg.
- Anticonvulsant: 1 mg to 6 mg/kg per day
- Daytime sedative: 30 mg to 120 mg daily in 2 to 3 divided doses.
- Bedtime hypnotic: 100 mg to 320 mg.
- Anticonvulsant: 50 mg to 100 mg 2 to 3 times daily.
- 15 to 20 mg/kg IV over 10 to 15 min.
- Preoperative Sedation:1 to 3 mg/kg IM/IV;
- Anticonvulsant: 4 to 6 mg/kg IM/IV per day, for 10 days. Alternatively, use 10 to 15 mg/kg IM/IV per day to reach therapeutic level more quickly. Maxium IV rate 60 mg/min.
- Insomnia: 100 to 320 mg IM/IV;
- Convulsions: 100 to 320 mg IV. Repeat if needed (maximum, 600 mg per day);
- Status Epilepticus: 10 to 20 mg/kg IV. Repeat if needed.
Side effectsView
The most common adverse reaction is somnolence. Other less frequent adverse reactions are agitation, confusion, hyperkinesia, ataxia, CNS depression, nightmares, nervousness, psychiatric disturbance, hallucinations, insomnia, anxiety, dizziness, thinking abnormality, apnea, bradycardia, hypotension, nausea, vomiting and constipation.
ContraindicationsView
Phenobarbital is contraindicated in patients with known Phenobarbital sensitivity or a history of latent porphyria.
PrecautionsView
Tolerance and psychological and physical dependence may occur with continuing use. Phenobarbital should be administered with caution to patients who are mentally depressed, have suicidal tendencies, or a history of drug abuse. In patients with hepatic damage, Phenobarbital should be administered with caution and initially reduced doses.
InteractionsView
The concomitant use of Alcohol or other CNS depressants may produce additive CNS depressant effects.
Pregnancy & lactationView
Pregnancy Category D. Phenobarbital can cause fetal damage when administered to a pregnant woman. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be in risk of the potential hazard to the fetus. Caution should be taken when Phenobarbital is administered to a nursing woman since small amounts of Phenobarbital are excreted in the milk.
Overdose effectsView
The toxic dose of barbiturates varies considerably. In general, an oral dose of 1 gram of most barbiturates produces serious poisoning in an adult. Death commonly occurs after 2 to 10 grams of ingested barbiturate. Acute overdosage with barbiturates is manifested by CNS and respiratory depression Treatment of overdosage is mainly supportive and immediate hospitalization is necessary.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Emeren
Ondansetron
Emeren
Ondansetron
Indications
Post-operative nausea and vomiting
Indication detailsView
Ondansetron is a serotonin subtype 3 (5-HT3) receptor antagonist indicated:
- Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy.
- Prevention and treatment of post-operative nausea and vomiting.
- Prevention of radiotherapy-induced nausea and vomiting.
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Ondansetron is a potent, highly selective 5HT3 receptor-antagonist. Its precise mode of action in the control of nausea and vomiting is not known. Chemotherapeutic agents and radiotherapy may cause release of 5HT in the small intestine initiating a vomiting reflex by activating vagal afferents via 5HT3 receptors. Ondansetron blocks the initiation of this reflex. Activation of vagal afferents may also cause a release of 5HT in the area postrema, located on the floor of the fourth ventricle, and this may also promote emesis through a central mechanism. Thus, the effect of ondansetron in the management of the nausea and vomiting induced by cytotoxic chemotherapy and radiotherapy is probably due to antagonism of 5HT3 receptors on neurons located both in the peripheral and central nervous system. The mechanisms of action in post-operative nausea and vomiting are not known but there may be common pathways with cytotoxic induced nausea and vomiting.
DosageView
Chemotherapy-Induced Nausea and Vomiting-
Adults, Pediatric patients (6 months to 18 years):
Adults:
Adults:
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:
Adults, Pediatric patients (6 months to 18 years):
- 8 mg tablet/orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: Initial Dose: 8 mg orally 1 to 2 hours before radiotherapy. Post Radiotherapy: 8 mg orally every 8 hours for up to 5 days after a course of treatment.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: 16 mg given as two 8 mg tablets
- 4 mg orodispersible tablet: 16 mg
- Injection: 4 mg
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
- Highly emetogenic cancer chemotherapy: 30 ml (24 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy.
- Moderate emetogenic cancer chemotherapy: 10 ml (8 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy. A further 10 ml dose should be administered after 8 hours of the first dose. One 10 ml dose should be administered twice a day (every 12 hours) for 1-2 days after completion of chemotherapy.
Oral solution:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):- The recommended oral dosage: 10 ml (8 mg) Ondansetron Oral Solution 3 times daily.
- For total body irradiation: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before each fraction of radiotherapy administered each day.
- For single high-dose fraction radiotherapy to the abdomen: one 10 ml Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for 1 to 2 days after completion of radiotherapy.
- For daily fractionated radiotherapy to the abdomen: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for each day radiotherapy is given.
- 20 ml (16 mg) Ondansetron Oral Solution 1 hour before induction of anesthesia
Oral Soluble Film:
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:- Adult oral dose: 24 mg given successively as three 8 mg films 30 minutes before the start of chemotherapy.
- Adults and pediatric patients 12 years of age and older: One 8 mg film 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later. Administer one 8 mg film twice a day (every 12 hours) for 1 to 2 days after completion of chemotherapy.
- Pediatric patients 4 through 11 years of age: One 4 mg film three times a day. Administer the first dose 30 minutes before chemotherapy, with subsequent doses 4 and 8 hours later. Administer one 4 mg film three times a day (every 8 hours) for 1 to 2 days after completion of chemotherapy.
- Prevention of nausea and vomiting associated with radiotherapy: The adult dosage is one 8 mg film three times a day.
- Postoperative nausea and vomiting: The adult dose is 16 mg given successively as two 8 mg films 1 hour before anesthesia.
AdministrationView
Administration of Oral Soluble Film:
- Step 1: Tear the pouch carefully along with the edge tear mark.
- Step 2: Put the Ondansetron film on top of your tongue. It will dissolve within 20 seconds
- Step 3: Do not chew or swallow the film whole.
- Step 4: Swallow after the Onsaf oral soluble film dissolves. You may swallow the dissolved film with or without liquid.
- Step 5: Wash your hands after taking Onsaf oral soluble film
Side effectsView
Frequently reported adverse events were headache, constipation and diarrhea, but the majority have been mild or moderate in nature. In chemotherapy-induced nausea and vomiting, rash has occurred in approximately 1% of patients receiving Ondansetron. There also have been reports to a sensation of flushing or warmth, hiccups and liver enzyme abnormalities. Rare cases of anaphylaxis, brochospasm, tachycardia, angina (chest pain), hypokalemia, shortness of breath have also been reported, except for bronchospasm and anaphylaxis, the relationship to Ondansetron is unclear. There have been no evidence to extrapyramidal reactions, in rare case oculogyric crisis appearing alone, as well as with other dystonic reactions without definitive clinical evidence. In case of PONV, with the exception of headache, rates of these events were not significantly different in the Ondansetron and placebo groups.
ContraindicationsView
Contraindicated in patients known to have hypersensitivity to the drug or any of its components. Concomitant use of apomorphine.
PrecautionsView
Hypersensitivity reactions have been reported in patients who have exhibited hypersensitivity to other selective 5-HT3 receptor antagonists. Ondansetron is not a drug that stimulates gastric or intestinal peristalsis. It should not be used instead of nasogastric suction. The use of Ondansetron in patients following abdominal surgery or in patients with chemotherapy-induced nausea and vomiting may mask a progressive ileus and/or gastric distension.
InteractionsView
Ondansetron does not itself appear to induce or inhibit the cytochrome P-450 drug-metabolizing enzyme system of the liver. Because Ondansetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes, inducers or inhibitors of these enzymes may change the clearance and hence, the half-life of Ondansetron. On the basis of available data, no dosage adjustment of Ondasetron is recommended for patients on these drugs.
Pregnancy & lactationView
Carcinogenic effects were not seen in 2-year studies in rats and mice with oral Ondansetron doses up to 10 and 30 mg/kg per day, respectively. Ondansetron was not mutagenic in standard tests for mutagenicity. Oral administration of Ondansetron up to 15 mg/kg per day did not affect fertility or general reproduction performance of male and female rats.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Pediatric usageView
Dosage Adjustment for Patients With Impaired Renal Function: The dosage recommendation is the same as for the general population.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
StorageView
Store at temperature not exceeding 30ºC in a dry place. Protect from light and moisture.
Emeren
Ondansetron
Emeren
Ondansetron
Indications
Post-operative nausea and vomiting
Indication detailsView
Ondansetron is a serotonin subtype 3 (5-HT3) receptor antagonist indicated:
- Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy.
- Prevention and treatment of post-operative nausea and vomiting.
- Prevention of radiotherapy-induced nausea and vomiting.
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Ondansetron is a potent, highly selective 5HT3 receptor-antagonist. Its precise mode of action in the control of nausea and vomiting is not known. Chemotherapeutic agents and radiotherapy may cause release of 5HT in the small intestine initiating a vomiting reflex by activating vagal afferents via 5HT3 receptors. Ondansetron blocks the initiation of this reflex. Activation of vagal afferents may also cause a release of 5HT in the area postrema, located on the floor of the fourth ventricle, and this may also promote emesis through a central mechanism. Thus, the effect of ondansetron in the management of the nausea and vomiting induced by cytotoxic chemotherapy and radiotherapy is probably due to antagonism of 5HT3 receptors on neurons located both in the peripheral and central nervous system. The mechanisms of action in post-operative nausea and vomiting are not known but there may be common pathways with cytotoxic induced nausea and vomiting.
DosageView
Chemotherapy-Induced Nausea and Vomiting-
Adults, Pediatric patients (6 months to 18 years):
Adults:
Adults:
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:
Adults, Pediatric patients (6 months to 18 years):
- 8 mg tablet/orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: Initial Dose: 8 mg orally 1 to 2 hours before radiotherapy. Post Radiotherapy: 8 mg orally every 8 hours for up to 5 days after a course of treatment.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: 16 mg given as two 8 mg tablets
- 4 mg orodispersible tablet: 16 mg
- Injection: 4 mg
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
- Highly emetogenic cancer chemotherapy: 30 ml (24 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy.
- Moderate emetogenic cancer chemotherapy: 10 ml (8 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy. A further 10 ml dose should be administered after 8 hours of the first dose. One 10 ml dose should be administered twice a day (every 12 hours) for 1-2 days after completion of chemotherapy.
Oral solution:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):- The recommended oral dosage: 10 ml (8 mg) Ondansetron Oral Solution 3 times daily.
- For total body irradiation: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before each fraction of radiotherapy administered each day.
- For single high-dose fraction radiotherapy to the abdomen: one 10 ml Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for 1 to 2 days after completion of radiotherapy.
- For daily fractionated radiotherapy to the abdomen: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for each day radiotherapy is given.
- 20 ml (16 mg) Ondansetron Oral Solution 1 hour before induction of anesthesia
Oral Soluble Film:
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:- Adult oral dose: 24 mg given successively as three 8 mg films 30 minutes before the start of chemotherapy.
- Adults and pediatric patients 12 years of age and older: One 8 mg film 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later. Administer one 8 mg film twice a day (every 12 hours) for 1 to 2 days after completion of chemotherapy.
- Pediatric patients 4 through 11 years of age: One 4 mg film three times a day. Administer the first dose 30 minutes before chemotherapy, with subsequent doses 4 and 8 hours later. Administer one 4 mg film three times a day (every 8 hours) for 1 to 2 days after completion of chemotherapy.
- Prevention of nausea and vomiting associated with radiotherapy: The adult dosage is one 8 mg film three times a day.
- Postoperative nausea and vomiting: The adult dose is 16 mg given successively as two 8 mg films 1 hour before anesthesia.
AdministrationView
Administration of Oral Soluble Film:
- Step 1: Tear the pouch carefully along with the edge tear mark.
- Step 2: Put the Ondansetron film on top of your tongue. It will dissolve within 20 seconds
- Step 3: Do not chew or swallow the film whole.
- Step 4: Swallow after the Onsaf oral soluble film dissolves. You may swallow the dissolved film with or without liquid.
- Step 5: Wash your hands after taking Onsaf oral soluble film
Side effectsView
Frequently reported adverse events were headache, constipation and diarrhea, but the majority have been mild or moderate in nature. In chemotherapy-induced nausea and vomiting, rash has occurred in approximately 1% of patients receiving Ondansetron. There also have been reports to a sensation of flushing or warmth, hiccups and liver enzyme abnormalities. Rare cases of anaphylaxis, brochospasm, tachycardia, angina (chest pain), hypokalemia, shortness of breath have also been reported, except for bronchospasm and anaphylaxis, the relationship to Ondansetron is unclear. There have been no evidence to extrapyramidal reactions, in rare case oculogyric crisis appearing alone, as well as with other dystonic reactions without definitive clinical evidence. In case of PONV, with the exception of headache, rates of these events were not significantly different in the Ondansetron and placebo groups.
ContraindicationsView
Contraindicated in patients known to have hypersensitivity to the drug or any of its components. Concomitant use of apomorphine.
PrecautionsView
Hypersensitivity reactions have been reported in patients who have exhibited hypersensitivity to other selective 5-HT3 receptor antagonists. Ondansetron is not a drug that stimulates gastric or intestinal peristalsis. It should not be used instead of nasogastric suction. The use of Ondansetron in patients following abdominal surgery or in patients with chemotherapy-induced nausea and vomiting may mask a progressive ileus and/or gastric distension.
InteractionsView
Ondansetron does not itself appear to induce or inhibit the cytochrome P-450 drug-metabolizing enzyme system of the liver. Because Ondansetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes, inducers or inhibitors of these enzymes may change the clearance and hence, the half-life of Ondansetron. On the basis of available data, no dosage adjustment of Ondasetron is recommended for patients on these drugs.
Pregnancy & lactationView
Carcinogenic effects were not seen in 2-year studies in rats and mice with oral Ondansetron doses up to 10 and 30 mg/kg per day, respectively. Ondansetron was not mutagenic in standard tests for mutagenicity. Oral administration of Ondansetron up to 15 mg/kg per day did not affect fertility or general reproduction performance of male and female rats.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Pediatric usageView
Dosage Adjustment for Patients With Impaired Renal Function: The dosage recommendation is the same as for the general population.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
StorageView
Store at temperature not exceeding 30ºC in a dry place. Protect from light and moisture.
Emeren
Ondansetron
Emeren
Ondansetron
Indications
Post-operative nausea and vomiting
Indication detailsView
Ondansetron is a serotonin subtype 3 (5-HT3) receptor antagonist indicated:
- Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy.
- Prevention and treatment of post-operative nausea and vomiting.
- Prevention of radiotherapy-induced nausea and vomiting.
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Ondansetron is a potent, highly selective 5HT3 receptor-antagonist. Its precise mode of action in the control of nausea and vomiting is not known. Chemotherapeutic agents and radiotherapy may cause release of 5HT in the small intestine initiating a vomiting reflex by activating vagal afferents via 5HT3 receptors. Ondansetron blocks the initiation of this reflex. Activation of vagal afferents may also cause a release of 5HT in the area postrema, located on the floor of the fourth ventricle, and this may also promote emesis through a central mechanism. Thus, the effect of ondansetron in the management of the nausea and vomiting induced by cytotoxic chemotherapy and radiotherapy is probably due to antagonism of 5HT3 receptors on neurons located both in the peripheral and central nervous system. The mechanisms of action in post-operative nausea and vomiting are not known but there may be common pathways with cytotoxic induced nausea and vomiting.
DosageView
Chemotherapy-Induced Nausea and Vomiting-
Adults, Pediatric patients (6 months to 18 years):
Adults:
Adults:
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:
Adults, Pediatric patients (6 months to 18 years):
- 8 mg tablet/orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: Initial Dose: 8 mg orally 1 to 2 hours before radiotherapy. Post Radiotherapy: 8 mg orally every 8 hours for up to 5 days after a course of treatment.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: 16 mg given as two 8 mg tablets
- 4 mg orodispersible tablet: 16 mg
- Injection: 4 mg
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
- Highly emetogenic cancer chemotherapy: 30 ml (24 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy.
- Moderate emetogenic cancer chemotherapy: 10 ml (8 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy. A further 10 ml dose should be administered after 8 hours of the first dose. One 10 ml dose should be administered twice a day (every 12 hours) for 1-2 days after completion of chemotherapy.
Oral solution:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):- The recommended oral dosage: 10 ml (8 mg) Ondansetron Oral Solution 3 times daily.
- For total body irradiation: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before each fraction of radiotherapy administered each day.
- For single high-dose fraction radiotherapy to the abdomen: one 10 ml Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for 1 to 2 days after completion of radiotherapy.
- For daily fractionated radiotherapy to the abdomen: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for each day radiotherapy is given.
- 20 ml (16 mg) Ondansetron Oral Solution 1 hour before induction of anesthesia
Oral Soluble Film:
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:- Adult oral dose: 24 mg given successively as three 8 mg films 30 minutes before the start of chemotherapy.
- Adults and pediatric patients 12 years of age and older: One 8 mg film 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later. Administer one 8 mg film twice a day (every 12 hours) for 1 to 2 days after completion of chemotherapy.
- Pediatric patients 4 through 11 years of age: One 4 mg film three times a day. Administer the first dose 30 minutes before chemotherapy, with subsequent doses 4 and 8 hours later. Administer one 4 mg film three times a day (every 8 hours) for 1 to 2 days after completion of chemotherapy.
- Prevention of nausea and vomiting associated with radiotherapy: The adult dosage is one 8 mg film three times a day.
- Postoperative nausea and vomiting: The adult dose is 16 mg given successively as two 8 mg films 1 hour before anesthesia.
AdministrationView
Administration of Oral Soluble Film:
- Step 1: Tear the pouch carefully along with the edge tear mark.
- Step 2: Put the Ondansetron film on top of your tongue. It will dissolve within 20 seconds
- Step 3: Do not chew or swallow the film whole.
- Step 4: Swallow after the Onsaf oral soluble film dissolves. You may swallow the dissolved film with or without liquid.
- Step 5: Wash your hands after taking Onsaf oral soluble film
Side effectsView
Frequently reported adverse events were headache, constipation and diarrhea, but the majority have been mild or moderate in nature. In chemotherapy-induced nausea and vomiting, rash has occurred in approximately 1% of patients receiving Ondansetron. There also have been reports to a sensation of flushing or warmth, hiccups and liver enzyme abnormalities. Rare cases of anaphylaxis, brochospasm, tachycardia, angina (chest pain), hypokalemia, shortness of breath have also been reported, except for bronchospasm and anaphylaxis, the relationship to Ondansetron is unclear. There have been no evidence to extrapyramidal reactions, in rare case oculogyric crisis appearing alone, as well as with other dystonic reactions without definitive clinical evidence. In case of PONV, with the exception of headache, rates of these events were not significantly different in the Ondansetron and placebo groups.
ContraindicationsView
Contraindicated in patients known to have hypersensitivity to the drug or any of its components. Concomitant use of apomorphine.
PrecautionsView
Hypersensitivity reactions have been reported in patients who have exhibited hypersensitivity to other selective 5-HT3 receptor antagonists. Ondansetron is not a drug that stimulates gastric or intestinal peristalsis. It should not be used instead of nasogastric suction. The use of Ondansetron in patients following abdominal surgery or in patients with chemotherapy-induced nausea and vomiting may mask a progressive ileus and/or gastric distension.
InteractionsView
Ondansetron does not itself appear to induce or inhibit the cytochrome P-450 drug-metabolizing enzyme system of the liver. Because Ondansetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes, inducers or inhibitors of these enzymes may change the clearance and hence, the half-life of Ondansetron. On the basis of available data, no dosage adjustment of Ondasetron is recommended for patients on these drugs.
Pregnancy & lactationView
Carcinogenic effects were not seen in 2-year studies in rats and mice with oral Ondansetron doses up to 10 and 30 mg/kg per day, respectively. Ondansetron was not mutagenic in standard tests for mutagenicity. Oral administration of Ondansetron up to 15 mg/kg per day did not affect fertility or general reproduction performance of male and female rats.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Pediatric usageView
Dosage Adjustment for Patients With Impaired Renal Function: The dosage recommendation is the same as for the general population.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
StorageView
Store at temperature not exceeding 30ºC in a dry place. Protect from light and moisture.
Emeren
Ondansetron
Emeren
Ondansetron
Indications
Post-operative nausea and vomiting
Indication detailsView
Ondansetron is a serotonin subtype 3 (5-HT3) receptor antagonist indicated:
- Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy.
- Prevention and treatment of post-operative nausea and vomiting.
- Prevention of radiotherapy-induced nausea and vomiting.
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Ondansetron is a potent, highly selective 5HT3 receptor-antagonist. Its precise mode of action in the control of nausea and vomiting is not known. Chemotherapeutic agents and radiotherapy may cause release of 5HT in the small intestine initiating a vomiting reflex by activating vagal afferents via 5HT3 receptors. Ondansetron blocks the initiation of this reflex. Activation of vagal afferents may also cause a release of 5HT in the area postrema, located on the floor of the fourth ventricle, and this may also promote emesis through a central mechanism. Thus, the effect of ondansetron in the management of the nausea and vomiting induced by cytotoxic chemotherapy and radiotherapy is probably due to antagonism of 5HT3 receptors on neurons located both in the peripheral and central nervous system. The mechanisms of action in post-operative nausea and vomiting are not known but there may be common pathways with cytotoxic induced nausea and vomiting.
DosageView
Chemotherapy-Induced Nausea and Vomiting-
Adults, Pediatric patients (6 months to 18 years):
Adults:
Adults:
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:
Adults, Pediatric patients (6 months to 18 years):
- 8 mg tablet/orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: Initial Dose: 8 mg orally 1 to 2 hours before radiotherapy. Post Radiotherapy: 8 mg orally every 8 hours for up to 5 days after a course of treatment.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: 16 mg given as two 8 mg tablets
- 4 mg orodispersible tablet: 16 mg
- Injection: 4 mg
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
- Highly emetogenic cancer chemotherapy: 30 ml (24 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy.
- Moderate emetogenic cancer chemotherapy: 10 ml (8 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy. A further 10 ml dose should be administered after 8 hours of the first dose. One 10 ml dose should be administered twice a day (every 12 hours) for 1-2 days after completion of chemotherapy.
Oral solution:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):- The recommended oral dosage: 10 ml (8 mg) Ondansetron Oral Solution 3 times daily.
- For total body irradiation: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before each fraction of radiotherapy administered each day.
- For single high-dose fraction radiotherapy to the abdomen: one 10 ml Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for 1 to 2 days after completion of radiotherapy.
- For daily fractionated radiotherapy to the abdomen: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for each day radiotherapy is given.
- 20 ml (16 mg) Ondansetron Oral Solution 1 hour before induction of anesthesia
Oral Soluble Film:
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:- Adult oral dose: 24 mg given successively as three 8 mg films 30 minutes before the start of chemotherapy.
- Adults and pediatric patients 12 years of age and older: One 8 mg film 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later. Administer one 8 mg film twice a day (every 12 hours) for 1 to 2 days after completion of chemotherapy.
- Pediatric patients 4 through 11 years of age: One 4 mg film three times a day. Administer the first dose 30 minutes before chemotherapy, with subsequent doses 4 and 8 hours later. Administer one 4 mg film three times a day (every 8 hours) for 1 to 2 days after completion of chemotherapy.
- Prevention of nausea and vomiting associated with radiotherapy: The adult dosage is one 8 mg film three times a day.
- Postoperative nausea and vomiting: The adult dose is 16 mg given successively as two 8 mg films 1 hour before anesthesia.
AdministrationView
Administration of Oral Soluble Film:
- Step 1: Tear the pouch carefully along with the edge tear mark.
- Step 2: Put the Ondansetron film on top of your tongue. It will dissolve within 20 seconds
- Step 3: Do not chew or swallow the film whole.
- Step 4: Swallow after the Onsaf oral soluble film dissolves. You may swallow the dissolved film with or without liquid.
- Step 5: Wash your hands after taking Onsaf oral soluble film
Side effectsView
Frequently reported adverse events were headache, constipation and diarrhea, but the majority have been mild or moderate in nature. In chemotherapy-induced nausea and vomiting, rash has occurred in approximately 1% of patients receiving Ondansetron. There also have been reports to a sensation of flushing or warmth, hiccups and liver enzyme abnormalities. Rare cases of anaphylaxis, brochospasm, tachycardia, angina (chest pain), hypokalemia, shortness of breath have also been reported, except for bronchospasm and anaphylaxis, the relationship to Ondansetron is unclear. There have been no evidence to extrapyramidal reactions, in rare case oculogyric crisis appearing alone, as well as with other dystonic reactions without definitive clinical evidence. In case of PONV, with the exception of headache, rates of these events were not significantly different in the Ondansetron and placebo groups.
ContraindicationsView
Contraindicated in patients known to have hypersensitivity to the drug or any of its components. Concomitant use of apomorphine.
PrecautionsView
Hypersensitivity reactions have been reported in patients who have exhibited hypersensitivity to other selective 5-HT3 receptor antagonists. Ondansetron is not a drug that stimulates gastric or intestinal peristalsis. It should not be used instead of nasogastric suction. The use of Ondansetron in patients following abdominal surgery or in patients with chemotherapy-induced nausea and vomiting may mask a progressive ileus and/or gastric distension.
InteractionsView
Ondansetron does not itself appear to induce or inhibit the cytochrome P-450 drug-metabolizing enzyme system of the liver. Because Ondansetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes, inducers or inhibitors of these enzymes may change the clearance and hence, the half-life of Ondansetron. On the basis of available data, no dosage adjustment of Ondasetron is recommended for patients on these drugs.
Pregnancy & lactationView
Carcinogenic effects were not seen in 2-year studies in rats and mice with oral Ondansetron doses up to 10 and 30 mg/kg per day, respectively. Ondansetron was not mutagenic in standard tests for mutagenicity. Oral administration of Ondansetron up to 15 mg/kg per day did not affect fertility or general reproduction performance of male and female rats.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Pediatric usageView
Dosage Adjustment for Patients With Impaired Renal Function: The dosage recommendation is the same as for the general population.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
StorageView
Store at temperature not exceeding 30ºC in a dry place. Protect from light and moisture.
Emeset
Ondansetron
Emeset
Ondansetron
Indications
Post-operative nausea and vomiting
Indication detailsView
Ondansetron is a serotonin subtype 3 (5-HT3) receptor antagonist indicated:
- Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy.
- Prevention and treatment of post-operative nausea and vomiting.
- Prevention of radiotherapy-induced nausea and vomiting.
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Ondansetron is a potent, highly selective 5HT3 receptor-antagonist. Its precise mode of action in the control of nausea and vomiting is not known. Chemotherapeutic agents and radiotherapy may cause release of 5HT in the small intestine initiating a vomiting reflex by activating vagal afferents via 5HT3 receptors. Ondansetron blocks the initiation of this reflex. Activation of vagal afferents may also cause a release of 5HT in the area postrema, located on the floor of the fourth ventricle, and this may also promote emesis through a central mechanism. Thus, the effect of ondansetron in the management of the nausea and vomiting induced by cytotoxic chemotherapy and radiotherapy is probably due to antagonism of 5HT3 receptors on neurons located both in the peripheral and central nervous system. The mechanisms of action in post-operative nausea and vomiting are not known but there may be common pathways with cytotoxic induced nausea and vomiting.
DosageView
Chemotherapy-Induced Nausea and Vomiting-
Adults, Pediatric patients (6 months to 18 years):
Adults:
Adults:
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:
Adults, Pediatric patients (6 months to 18 years):
- 8 mg tablet/orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: Initial Dose: 8 mg orally 1 to 2 hours before radiotherapy. Post Radiotherapy: 8 mg orally every 8 hours for up to 5 days after a course of treatment.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: 16 mg given as two 8 mg tablets
- 4 mg orodispersible tablet: 16 mg
- Injection: 4 mg
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
- Highly emetogenic cancer chemotherapy: 30 ml (24 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy.
- Moderate emetogenic cancer chemotherapy: 10 ml (8 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy. A further 10 ml dose should be administered after 8 hours of the first dose. One 10 ml dose should be administered twice a day (every 12 hours) for 1-2 days after completion of chemotherapy.
Oral solution:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):- The recommended oral dosage: 10 ml (8 mg) Ondansetron Oral Solution 3 times daily.
- For total body irradiation: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before each fraction of radiotherapy administered each day.
- For single high-dose fraction radiotherapy to the abdomen: one 10 ml Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for 1 to 2 days after completion of radiotherapy.
- For daily fractionated radiotherapy to the abdomen: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for each day radiotherapy is given.
- 20 ml (16 mg) Ondansetron Oral Solution 1 hour before induction of anesthesia
Oral Soluble Film:
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:- Adult oral dose: 24 mg given successively as three 8 mg films 30 minutes before the start of chemotherapy.
- Adults and pediatric patients 12 years of age and older: One 8 mg film 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later. Administer one 8 mg film twice a day (every 12 hours) for 1 to 2 days after completion of chemotherapy.
- Pediatric patients 4 through 11 years of age: One 4 mg film three times a day. Administer the first dose 30 minutes before chemotherapy, with subsequent doses 4 and 8 hours later. Administer one 4 mg film three times a day (every 8 hours) for 1 to 2 days after completion of chemotherapy.
- Prevention of nausea and vomiting associated with radiotherapy: The adult dosage is one 8 mg film three times a day.
- Postoperative nausea and vomiting: The adult dose is 16 mg given successively as two 8 mg films 1 hour before anesthesia.
AdministrationView
Administration of Oral Soluble Film:
- Step 1: Tear the pouch carefully along with the edge tear mark.
- Step 2: Put the Ondansetron film on top of your tongue. It will dissolve within 20 seconds
- Step 3: Do not chew or swallow the film whole.
- Step 4: Swallow after the Onsaf oral soluble film dissolves. You may swallow the dissolved film with or without liquid.
- Step 5: Wash your hands after taking Onsaf oral soluble film
Side effectsView
Frequently reported adverse events were headache, constipation and diarrhea, but the majority have been mild or moderate in nature. In chemotherapy-induced nausea and vomiting, rash has occurred in approximately 1% of patients receiving Ondansetron. There also have been reports to a sensation of flushing or warmth, hiccups and liver enzyme abnormalities. Rare cases of anaphylaxis, brochospasm, tachycardia, angina (chest pain), hypokalemia, shortness of breath have also been reported, except for bronchospasm and anaphylaxis, the relationship to Ondansetron is unclear. There have been no evidence to extrapyramidal reactions, in rare case oculogyric crisis appearing alone, as well as with other dystonic reactions without definitive clinical evidence. In case of PONV, with the exception of headache, rates of these events were not significantly different in the Ondansetron and placebo groups.
ContraindicationsView
Contraindicated in patients known to have hypersensitivity to the drug or any of its components. Concomitant use of apomorphine.
PrecautionsView
Hypersensitivity reactions have been reported in patients who have exhibited hypersensitivity to other selective 5-HT3 receptor antagonists. Ondansetron is not a drug that stimulates gastric or intestinal peristalsis. It should not be used instead of nasogastric suction. The use of Ondansetron in patients following abdominal surgery or in patients with chemotherapy-induced nausea and vomiting may mask a progressive ileus and/or gastric distension.
InteractionsView
Ondansetron does not itself appear to induce or inhibit the cytochrome P-450 drug-metabolizing enzyme system of the liver. Because Ondansetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes, inducers or inhibitors of these enzymes may change the clearance and hence, the half-life of Ondansetron. On the basis of available data, no dosage adjustment of Ondasetron is recommended for patients on these drugs.
Pregnancy & lactationView
Carcinogenic effects were not seen in 2-year studies in rats and mice with oral Ondansetron doses up to 10 and 30 mg/kg per day, respectively. Ondansetron was not mutagenic in standard tests for mutagenicity. Oral administration of Ondansetron up to 15 mg/kg per day did not affect fertility or general reproduction performance of male and female rats.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Pediatric usageView
Dosage Adjustment for Patients With Impaired Renal Function: The dosage recommendation is the same as for the general population.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
StorageView
Store at temperature not exceeding 30ºC in a dry place. Protect from light and moisture.
Emeset
Ondansetron
Emeset
Ondansetron
Indications
Post-operative nausea and vomiting
Indication detailsView
Ondansetron is a serotonin subtype 3 (5-HT3) receptor antagonist indicated:
- Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy.
- Prevention and treatment of post-operative nausea and vomiting.
- Prevention of radiotherapy-induced nausea and vomiting.
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Ondansetron is a potent, highly selective 5HT3 receptor-antagonist. Its precise mode of action in the control of nausea and vomiting is not known. Chemotherapeutic agents and radiotherapy may cause release of 5HT in the small intestine initiating a vomiting reflex by activating vagal afferents via 5HT3 receptors. Ondansetron blocks the initiation of this reflex. Activation of vagal afferents may also cause a release of 5HT in the area postrema, located on the floor of the fourth ventricle, and this may also promote emesis through a central mechanism. Thus, the effect of ondansetron in the management of the nausea and vomiting induced by cytotoxic chemotherapy and radiotherapy is probably due to antagonism of 5HT3 receptors on neurons located both in the peripheral and central nervous system. The mechanisms of action in post-operative nausea and vomiting are not known but there may be common pathways with cytotoxic induced nausea and vomiting.
DosageView
Chemotherapy-Induced Nausea and Vomiting-
Adults, Pediatric patients (6 months to 18 years):
Adults:
Adults:
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:
Adults, Pediatric patients (6 months to 18 years):
- 8 mg tablet/orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: Initial Dose: 8 mg orally 1 to 2 hours before radiotherapy. Post Radiotherapy: 8 mg orally every 8 hours for up to 5 days after a course of treatment.
- 4 mg orodispersible tablet: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose.
- Injection: Three 0.15 mg/kg doses, up to a maximum of 16 mg per dose, infused intravenously over 15 minutes.
Adults:
- 8 mg tablet/orodispersible tablet: 16 mg given as two 8 mg tablets
- 4 mg orodispersible tablet: 16 mg
- Injection: 4 mg
Pediatrics (40 kg): Injection: 0.1 mg/kg
Chemotherapy-induced Nausea and Vomiting-
Adults/Geriatric/Child of 12 years or over:
- Highly emetogenic cancer chemotherapy: 30 ml (24 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy.
- Moderate emetogenic cancer chemotherapy: 10 ml (8 mg) Ondansetron Oral Solution administered 30 minutes before start of emetogenic chemotherapy. A further 10 ml dose should be administered after 8 hours of the first dose. One 10 ml dose should be administered twice a day (every 12 hours) for 1-2 days after completion of chemotherapy.
Oral solution:
Radiotherapy induced Nausea and Vomiting (Adults/Geriatric/Child of 12 years or over):- The recommended oral dosage: 10 ml (8 mg) Ondansetron Oral Solution 3 times daily.
- For total body irradiation: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before each fraction of radiotherapy administered each day.
- For single high-dose fraction radiotherapy to the abdomen: one 10 ml Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for 1 to 2 days after completion of radiotherapy.
- For daily fractionated radiotherapy to the abdomen: 10 ml (8-mg) Ondansetron Oral Solution should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for each day radiotherapy is given.
- 20 ml (16 mg) Ondansetron Oral Solution 1 hour before induction of anesthesia
Oral Soluble Film:
Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:- Adult oral dose: 24 mg given successively as three 8 mg films 30 minutes before the start of chemotherapy.
- Adults and pediatric patients 12 years of age and older: One 8 mg film 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later. Administer one 8 mg film twice a day (every 12 hours) for 1 to 2 days after completion of chemotherapy.
- Pediatric patients 4 through 11 years of age: One 4 mg film three times a day. Administer the first dose 30 minutes before chemotherapy, with subsequent doses 4 and 8 hours later. Administer one 4 mg film three times a day (every 8 hours) for 1 to 2 days after completion of chemotherapy.
- Prevention of nausea and vomiting associated with radiotherapy: The adult dosage is one 8 mg film three times a day.
- Postoperative nausea and vomiting: The adult dose is 16 mg given successively as two 8 mg films 1 hour before anesthesia.
AdministrationView
Administration of Oral Soluble Film:
- Step 1: Tear the pouch carefully along with the edge tear mark.
- Step 2: Put the Ondansetron film on top of your tongue. It will dissolve within 20 seconds
- Step 3: Do not chew or swallow the film whole.
- Step 4: Swallow after the Onsaf oral soluble film dissolves. You may swallow the dissolved film with or without liquid.
- Step 5: Wash your hands after taking Onsaf oral soluble film
Side effectsView
Frequently reported adverse events were headache, constipation and diarrhea, but the majority have been mild or moderate in nature. In chemotherapy-induced nausea and vomiting, rash has occurred in approximately 1% of patients receiving Ondansetron. There also have been reports to a sensation of flushing or warmth, hiccups and liver enzyme abnormalities. Rare cases of anaphylaxis, brochospasm, tachycardia, angina (chest pain), hypokalemia, shortness of breath have also been reported, except for bronchospasm and anaphylaxis, the relationship to Ondansetron is unclear. There have been no evidence to extrapyramidal reactions, in rare case oculogyric crisis appearing alone, as well as with other dystonic reactions without definitive clinical evidence. In case of PONV, with the exception of headache, rates of these events were not significantly different in the Ondansetron and placebo groups.
ContraindicationsView
Contraindicated in patients known to have hypersensitivity to the drug or any of its components. Concomitant use of apomorphine.
PrecautionsView
Hypersensitivity reactions have been reported in patients who have exhibited hypersensitivity to other selective 5-HT3 receptor antagonists. Ondansetron is not a drug that stimulates gastric or intestinal peristalsis. It should not be used instead of nasogastric suction. The use of Ondansetron in patients following abdominal surgery or in patients with chemotherapy-induced nausea and vomiting may mask a progressive ileus and/or gastric distension.
InteractionsView
Ondansetron does not itself appear to induce or inhibit the cytochrome P-450 drug-metabolizing enzyme system of the liver. Because Ondansetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes, inducers or inhibitors of these enzymes may change the clearance and hence, the half-life of Ondansetron. On the basis of available data, no dosage adjustment of Ondasetron is recommended for patients on these drugs.
Pregnancy & lactationView
Carcinogenic effects were not seen in 2-year studies in rats and mice with oral Ondansetron doses up to 10 and 30 mg/kg per day, respectively. Ondansetron was not mutagenic in standard tests for mutagenicity. Oral administration of Ondansetron up to 15 mg/kg per day did not affect fertility or general reproduction performance of male and female rats.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Reproduction studies have been performed in pregnant rats and rabbits at daily oral doses up to 15 and 30 mg/kg per day, respectively, and have revealed no evidence of impaired fertility or harm to the fetus due to Ondansetron. There are, however, no adequate and well-controlled studies in pregnant women. Ondansetron is excreted in the breast milk of rats. So caution should be exercised when Ondansetron is administered to a nursing women.
Pediatric usageView
Dosage Adjustment for Patients With Impaired Renal Function: The dosage recommendation is the same as for the general population.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
Dosage Adjustment for Patients With Impaired Hepatic Function: In patients with severe hepatic impairment, a single maximal daily dose of 8 mg to be infused over 15 minutes beginning 30 minutes before the start of the emetogenic chemotherapy is recommended.
4 years of age or younger: Little information is available about dosage in pediatric patients 4 years of age or younger.
Over the age of 65: Dosage adjustment is not needed in patients over the age of 65.
StorageView
Store at temperature not exceeding 30ºC in a dry place. Protect from light and moisture.
Emestop
Aprepitant
Emestop
Aprepitant
Indications
Nausea and vomiting
Indication detailsView
Aprepitant is indicated for-
- Prevention of postoperative nausea and vomiting (PONV)
- Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Aprepitant is a selective high affinity antagonist of human substance P neurokinin 1 (NK1) receptors. When substance P attaches to these receptors, it causes nausea and vomiting. Aprepitant stops substance P from binding to the NK1 receptors. By blocking the receptors, Aprepitant can prevent nausea and vomiting, which often happens after chemotherapy or as a complication of surgery.
DosageView
Post Operative Nausea and Vomiting: The recommended oral dosage of Aprepitant is 40 mg within 3 hours prior to induction of anesthesia.
Chemotherapy-Induced Nausea and Vomiting:
** The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy-
** The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
Chemotherapy-Induced Nausea and Vomiting:
** The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy-
- Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): 24 mg 30 minutes before the start of chemotherapy.
- Day 2: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
- Day 3: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
- Day 4: Dexamethasone 8 mg orally
** The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
- Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): one 8 mg tablet 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later.
- Day 2: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day
- Day 3: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day.
AdministrationView
Aprepitant may be taken with or without food. No dosage adjustment is necessary for the elderly patients.
Side effectsView
Constipation, Hypotension, Pruritus, Pyrexia
ContraindicationsView
Aprepitant is contraindicated in patients who are hypersensitive to any component of the product. Aprepitant should not be used concurrently with Pimozide, Terfenadine, Astemizole & Cisapride.
InteractionsView
Aprepitant is a substrate, a weak-to-moderate (dose dependent) inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9. Precautions should be taken while coadministering Aprepitant with drugs that use CYP3A4 or CYP2C9, for example- Warfarin, Tolbutamide, Phenytoin, Ketoconazole, Itraconazole, Nefazodone, Troleandomycin, Clarithromycin, Ritonavir, Nelfinavir, Diltiazem, Rifampin, Carbamazepine etc.
Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or back-up methods of contraception should be used during treatment with Aprepitant and for 1 month following the last dose of Aprepitant.
Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or back-up methods of contraception should be used during treatment with Aprepitant and for 1 month following the last dose of Aprepitant.
Pregnancy & lactationView
Pregnancy Category B. This drug should be used during pregnancy only if clearly needed. It is not known whether this drug is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug based on patient’s importance.
Pediatric usageView
Patients with Renal Impairment: No dosage adjustment is necessary for patients with renal impairment or for patients with end-stage renal disease (ESRD) undergoing hemodialysis.
Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment.
Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment.
Overdose effectsView
No specific information is available on the treatment of overdosage with Aprepitant. Single doses up to 600 mg of Aprepitant were generally well tolerated in healthy subjects. Drowsiness and headache can be seen due to overdose. In the event of overdose, Aprepitant should be discontinued. General supportive treatment and monitoring should be provided. Because of the antiemetic activity of Aprepitant, medicine-induced emesis may not be effective. Aprepitant cannot be removed by hemodialysis.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Emestop
Aprepitant
Emestop
Aprepitant
Indications
Nausea and vomiting
Indication detailsView
Aprepitant is indicated for-
- Prevention of postoperative nausea and vomiting (PONV)
- Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)
Therapeutic classView
Anti-emetic drugs
PharmacologyView
Aprepitant is a selective high affinity antagonist of human substance P neurokinin 1 (NK1) receptors. When substance P attaches to these receptors, it causes nausea and vomiting. Aprepitant stops substance P from binding to the NK1 receptors. By blocking the receptors, Aprepitant can prevent nausea and vomiting, which often happens after chemotherapy or as a complication of surgery.
DosageView
Post Operative Nausea and Vomiting: The recommended oral dosage of Aprepitant is 40 mg within 3 hours prior to induction of anesthesia.
Chemotherapy-Induced Nausea and Vomiting:
** The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy-
** The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
Chemotherapy-Induced Nausea and Vomiting:
** The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy-
- Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): 24 mg 30 minutes before the start of chemotherapy.
- Day 2: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
- Day 3: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
- Day 4: Dexamethasone 8 mg orally
** The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
- Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): one 8 mg tablet 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later.
- Day 2: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day
- Day 3: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day.
AdministrationView
Aprepitant may be taken with or without food. No dosage adjustment is necessary for the elderly patients.
Side effectsView
Constipation, Hypotension, Pruritus, Pyrexia
ContraindicationsView
Aprepitant is contraindicated in patients who are hypersensitive to any component of the product. Aprepitant should not be used concurrently with Pimozide, Terfenadine, Astemizole & Cisapride.
InteractionsView
Aprepitant is a substrate, a weak-to-moderate (dose dependent) inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9. Precautions should be taken while coadministering Aprepitant with drugs that use CYP3A4 or CYP2C9, for example- Warfarin, Tolbutamide, Phenytoin, Ketoconazole, Itraconazole, Nefazodone, Troleandomycin, Clarithromycin, Ritonavir, Nelfinavir, Diltiazem, Rifampin, Carbamazepine etc.
Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or back-up methods of contraception should be used during treatment with Aprepitant and for 1 month following the last dose of Aprepitant.
Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or back-up methods of contraception should be used during treatment with Aprepitant and for 1 month following the last dose of Aprepitant.
Pregnancy & lactationView
Pregnancy Category B. This drug should be used during pregnancy only if clearly needed. It is not known whether this drug is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug based on patient’s importance.
Pediatric usageView
Patients with Renal Impairment: No dosage adjustment is necessary for patients with renal impairment or for patients with end-stage renal disease (ESRD) undergoing hemodialysis.
Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment.
Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment.
Overdose effectsView
No specific information is available on the treatment of overdosage with Aprepitant. Single doses up to 600 mg of Aprepitant were generally well tolerated in healthy subjects. Drowsiness and headache can be seen due to overdose. In the event of overdose, Aprepitant should be discontinued. General supportive treatment and monitoring should be provided. Because of the antiemetic activity of Aprepitant, medicine-induced emesis may not be effective. Aprepitant cannot be removed by hemodialysis.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Emez
Omeprazole
Emez
Omeprazole
Indications
Zollinger-Ellison syndrome
Indication detailsView
Omeprazole is indicated for the treatment of-
- Gastric and duodenal ulcer
- NSAID-associated duodenal and gastric ulcer
- As prophylaxis in patients with a history of NSAID-associated duodenal and gastric ulcer
- Gastro-esophageal reflux disease
- Long-term management of acid reflux disease
- Acid-related dyspepsia
- Severe ulcerating reflux esophagitis
- Prophylaxis of acid aspiration during general anesthesia
- Zollinger-Ellison syndrome
- Helicobacter pylori-induced peptic ulcer.
Therapeutic classView
Proton Pump Inhibitor
PharmacologyView
Omeprazole, a substituted benzimidazole, is an inhibitor of gastric acid secretion. It inhibits gastric acid secretion by blocking hydrogen-potassium-adenosine triphosphatase (H+/K+ ATPase) enzyme system in the gastric parietal cell. After oral administration, the onset of the antisecretory effect occurs within one hour, with the maximum effect occurring within two hours and inhibition of secretion lasts up to 72 hours. When the drug is discontinued, secretory activity returns gradually, over 3 to 5 days.
DosageView
Oral-
IV Injection-
- Benign gastric and duodenal ulcer: 20 mg once daily for 4 weeks in duodenal ulceration, 8 weeks in gastric ulceration; in severe or recurrent cases, dose to be increased to 40 mg daily; maintenance dose for recurrent duodenal ulcer, 20 mg once daily; in prevention of relapse in duodenal ulcer, 10-20 mg daily.
- NSAID-associated duodenal or gastric ulcer: 20 mg once daily for 4 weeks, continued for further 4 weeks, if not fully healed. 20 mg once daily is used as prophylaxis in patients with a history of NSAID-associated duodenal or gastric ulcers.
- Gastro-esophageal reflux disease: 20 mg once daily for 4 weeks, continued for further 4-8 weeks, if not fully healed; 40 mg once daily has been given for 8 weeks in gastro-esophageal reflux disease, refractory to other treatment; maintenance dose is 20 mg once daily.
- Long-term management of acid reflux disease: 10-20 mg daily.
- Acid-related dyspepsia: 10-20 mg once daily for 2-4 weeks.
- Prophylaxis of acid aspiration: 40 mg on the preceding evening, then 40 mg 2-6 hours before surgery.
- Zollinger-Ellison syndrome: Initially 60 mg once daily; usual range 20-120 mg daily (If daily dose is more than 80 mg, 2 divided dose should be used).
- Helicobacter pylori eradication regimen in peptic ulcer disease: Omeprazole is recommended at a dose of 20 mg twice daily in association with antimicrobial agents as detailed below: Amoxicillin 500 mg and Metronidazole 400 mg both three times a day for one week, or Clarithromycin 250 mg and Metronidazole 400 mg both twice a day for one week, or Amoxicillin 1 g and Clarithromycin 500 mg both twice a day for one week.
- Paeditaric use in severe ulcerating reflux esophagitis (Child>1 year): If body-weight 10-20 kg, 10-20 -mg once daily for 4-12 weeks; if body-weight over 20 kg, 20-40 mg once daily for 4-12 weeks.
IV Injection-
- Prophylaxis of acid aspiration: Omeprazole 40 mg to be given slowly (over a period of 5 minutes) as an intravenous injection, one hour before surgery.
- Duodenal ulcer, gastric ulcer or reflux oesophagitis: In patients with duodenal ulcer, gastric ulcer or reflux oesophagitis where oral medication is inappropriate, Omeprazole IV 40 mg once daily is recommended.
- Zollinger- Ellison syndrome (ZES): In patients with Zollinger-Ellison Syndrome the recommended initial dose of Omeprazole given intravenously is 60 mg daily. Higher daily doses may be required and the dose should be adjusted individually. When doses exceed 60 mg daily, the dose should be divided & given twice daily.
AdministrationView
Direction for use of IV Injection: Omeprazole lyophilized powder and water for injection is for intravenous administration only and must not be given by any other route. Omeprazole IV injection should be given as a slow intravenous injection. The solution for IV injection is obtained by adding 10 ml water for injection to the vial containing powder. After reconstitution the injection should be given slowly over a period of at least 2 to 5 minutes at a maximum rate of 4 ml/minute. Use only freshly prepared solution. The solution should be used within 4 hours of reconstitution.
Direction for use of IV Infusion: Omeprazole IV infusion should be given as an intravenous infusion over a period of 20-30 minutes or more. The contents of one vial must be dissolved in 100 ml saline for infusion or 100 ml 5% Dextrose for infusion. The solution should be used within 12 hours when Omeprazole is dissolved in saline and within 6 hours when dissolved in 5% Dextrose. The reconstituted solution should not be mixed or co-administered in the same infusion set with any other drug.
Direction for use of IV Infusion: Omeprazole IV infusion should be given as an intravenous infusion over a period of 20-30 minutes or more. The contents of one vial must be dissolved in 100 ml saline for infusion or 100 ml 5% Dextrose for infusion. The solution should be used within 12 hours when Omeprazole is dissolved in saline and within 6 hours when dissolved in 5% Dextrose. The reconstituted solution should not be mixed or co-administered in the same infusion set with any other drug.
Side effectsView
Omeprazole is generally well tolerated. Nausea, abdominal colic, paresthesia, dizziness and headache have been stated to be generally mild and transient and not requiring a reduction in dosage.
ContraindicationsView
Omeprazole is contraindicated in patients with known hypersensitivity to any of the components of the formulation.
PrecautionsView
When gastric ulcer is suspected, the possibility of gastric malignancy should be excluded before treatment with Omeprazole is instituted, as treatment may alleviate the symptoms and delay diagnosis.
InteractionsView
Omeprazole can prolong the elimination of diazepam, warfarin and phenytoin. So, reduction of warfarin or phenytoin dose may be necessary when Omeprazole is added to the treatment. There is no evidence of an interaction of Omeprazole with theophylline, propranolol or antacids.
Pregnancy & lactationView
US FDA pregnancy category of Omeprazole is C. However, results from three prospective epidemiological studies indicate no adverse effects of Omeprazole on pregnancy or on the health of the fetus/newborn child. There is no information available on the passage of Omeprazole into breast milk or its effects on the neonate. Breast-feeding should, therefore, be discontinued, if the use of Omeprazole is considered essential.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.