Esomeprazole Dr
FDA Drug Information • Also known as: Esomeprazole Dr
- Brand Names
- Esomeprazole Dr
- Route
- ORAL
- Dosage Form
- CAPSULE, DELAYED RELEASE
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
The active ingredient in the proton pump inhibitor esomeprazole magnesium delayed-release capsules, USP for oral administration is 1H-Benzimidazole, 5-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl]methyl] Sulfinyl], Magnesium Salt (2:1) Trihydrate. Esomeprazole is S-enantiomer of omeprazole. (Initial U.S. approval of esomeprazole magnesium: 2001). Its molecular formula is C34H36MgN6O6S2.3H2O with molecular weight of 767.17 as a trihydrate. The structural formula is: Figure 1 [Esomeprazolemagnesiumfigure1] The magnesium salt is a white to slightly colored powder. It contains 3 moles of water. Slightly soluble in methanol, insoluble in water and in n-Heptane. The stability of esomeprazole magnesium is a function of pH; it rapidly degrades in acidic media, but it has acceptable stability under alkaline conditions. Esomeprazole magnesium is supplied in delayed-release capsules. Each delayed-release capsule contains 20 mg, or 40 mg of esomeprazole (present as 22.25 mg, or 44.5 mg esomeprazole magnesium trihydrate, USP) in the form of enteric-coated granules with the following inactive ingredients: glyceryl monostearate, hydroxy propyl cellulose, hypromellose, magnesium stearate, methacrylic acid ethyl acrylate copolymer, polysorbate 80, simethicone, sugar spheres (contains sucrose and starch), talc and triethyl citrate. The capsule shells have the following inactive ingredients: gelatin, titanium dioxide and sodium lauryl sulfate. The printing ink contains shellac, propylene glycol, strong ammonia solution, black iron oxide and potassium hydroxide.
What Is Esomeprazole Dr Used For?
1.1 Treatment of Gastroesophageal Reflux Disease (GERD) Healing of Erosive Esophagitis Esomeprazole magnesium delayed-release capsules are indicated for the short-term treatment (4 to 8 weeks) in the healing and symptomatic resolution of diagnostically confirmed erosive esophagitis. For those patients who have not healed after 4 to 8 weeks of treatment, an additional 4 to 8 week course of esomeprazole magnesium delayed-release capsules may be considered. Maintenance of Healing of Erosive Esophagitis Esomeprazole magnesium delayed-release capsules are indicated to maintain symptom resolution and healing of erosive esophagitis. Controlled studies do not extend beyond 6 months. Symptomatic Gastroesophageal Reflux Disease Esomeprazole magnesium delayed-release capsules are indicated for short-term treatment (4 to 8 weeks) of heartburn and other symptoms associated with GERD in adults and children 1 year or older. 1.2 Risk Reduction of NSAID-Associated Gastric Ulcer Esomeprazole magnesium delayed-release capsules are indicated for the reduction in the occurrence of gastric ulcers associated with continuous NSAID therapy in patients at risk for developing gastric ulcers. Patients are considered to be at risk due to their age (≥ 60) and/or documented history of gastric ulcers. Controlled studies do not extend beyond 6 months. 1.3 H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence Triple Therapy (esomeprazole magnesium delayed-release capsules plus amoxicillin and clarithromycin): Esomeprazole magnesium delayed-release capsules, in combination with amoxicillin and clarithromycin, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or history of within the past 5 years) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence [see Dosage and Administration (2) and Clinical Studies (14)]. In patients who fail therapy, susceptibility testing should be done. If resistance to clarithromycin is demonstrated or susceptibility testing is not possible, alternative antimicrobial therapy should be instituted [see Clinical Pharmacology (12.4) and the prescribing information for clarithromycin]. 1.4 Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome Esomeprazole magnesium delayed-release capsules are indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison Syndrome.
Dosage and Administration
Esomeprazole magnesium is supplied as delayed-release capsules for oral administration. The recommended dosages are outlined in Table 1. Esomeprazole magnesium delayed-release capsules should be taken at least one hour before meals. The duration of proton pump inhibitor administration should be based on available safety and efficacy data specific to the defined indication and dosing frequency, as described in the prescribing information, and individual patient medical needs. Proton pump inhibitor treatment should only be initiated and continued if the benefits outweigh the risks of treatment. Table 1: Recommended Dosage Schedule for Esomeprazole Magnesium Delayed-Release Capsules Indication Dose Frequency Gastroesophageal Reflux Disease (GERD) Healing of Erosive Esophagitis 20 mg or 40 mg Once Daily for 4 to 8 Weeks1 Maintenance of Healing of Erosive Esophagitis 20 mg Once Daily2 Symptomatic Gastroesophageal Reflux Disease 20 mg Once Daily for 4 Weeks3 Pediatric GERD 12 to 17 Year Olds Healing of Erosive Esophagitis 20 mg or 40 mg Once Daily for 4 to 8 Weeks Symptomatic GERD 20 mg Once Daily for 4 Weeks 1 to 11 Year Olds4 Short-term Treatment of Symptomatic GERD 10 mg Once Daily for up to 8 Weeks Healing of Erosive Esophagitis weight < 20 kg 10 mg Once Daily for 8 Weeks weight ≥ 20 kg 10 mg or 20 mg Once Daily for 8 Weeks Risk Reduction of NSAID-Associated Gastric Ulcer 20 mg or 40 mg Once Daily for up to 6 months2 H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence Triple Therapy: Esomeprazole 40 mg Once Daily for 10 Day Amoxicillin 1000 mg Twice Daily for 10 Days Clarithromycin 500 mg Twice Daily for 10 Days Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome 40 mg6 Twice Daily7 1[See Clinical Studies (14.1)]The majority of patients are healed within 4 to 8 weeks. For patients who do not heal after 4 to 8 weeks, an additional 4 to 8 weeks of treatment may be considered. 2 Controlled studies did not extend beyond six months. 3 If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered. 4 Doses over 1 mg/kg/day have not been studied. 5. Doses over 1.33 mg/kg/day have not been studied. 6 The dosage of esomeprazole magnesium delayed-release capsules in patients with pathological hypersecretory conditions varies with the individual patient. Dosage regimens should be adjusted to individual patient needs. 7 Doses up to 240 mg daily have been administered [see Drug Interactions (7)] . Please refer to amoxicillin and clarithromycin prescribing information for Contraindications, Warnings, and dosing in elderly and renally-impaired patients. Specific Populations Hepatic Insufficiency In patients with mild to moderate liver impairment (Child-Pugh Classes A and B), no dosage adjustment is necessary. For patients with severe liver impairment (Child-Pugh Class C), a dose of 20 mg of esomeprazole magnesium delayed-release capsules should not be exceeded [see Clinical...
Side Effects (Adverse Reactions)
The following serious adverse reactions are described below and elsewhere in labeling:
Drug Interactions
7.1 Interference with Antiretroviral Therapy Concomitant use of atazanavir and nelfinavir with proton pump inhibitors is not recommended. Co-administration of atazanavir with proton pump inhibitors is expected to substantially decrease atazanavir plasma concentrations and may result in a loss of therapeutic effect and the development of drug resistance. Co-administration of saquinavir with proton pump inhibitors is expected to increase saquinavir concentrations, which may increase toxicity and require dose reduction. Omeprazole, of which esomeprazole is an enantiomer, has been reported to interact with some antiretroviral drugs. The clinical importance and the mechanisms behind these interactions are not always known. Increased gastric pH during omeprazole treatment may change the absorption of the antiretroviral drug. Other possible interaction mechanisms are via CYP2C19. Reduced concentrations of atazanavir and nelfinavir For some antiretroviral drugs, such as atazanavir and nelfinavir, decreased serum levels have been reported when given together with omeprazole. Following multiple doses of nelfinavir (1,250 mg, twice daily) and omeprazole (40 mg daily), AUC was decreased by 36% and 92%, Cmax by 37% and 89% and Cmin by 39% and 75% respectively for nelfinavir and M8. Following multiple doses of atazanavir (400 mg, daily) and omeprazole (40 mg, daily, 2 hours before atazanavir), AUC was decreased by 94%, Cmax by 96%, and Cmin by 95%. Concomitant administration with omeprazole and drugs such as atazanavir and nelfinavir is therefore not recommended. Increased concentrations of saquinavir For other antiretroviral drugs, such as saquinavir, elevated serum levels have been reported, with an increase in AUC by 82%, in Cmax by 75%, and in Cmin by 106%, following multiple dosing of saquinavir/ritonavir (1,000/100 mg) twice daily for 15 days with omeprazole 40 mg daily co-administered days 11 to 15. Therefore, clinical and laboratory monitoring for saquinavir toxicity is recommended during concurrent use with esomeprazole magnesium delayed-release capsules. Dose reduction of saquinavir should be considered from the safety perspective for individual patients. There are also some antiretroviral drugs of which unchanged serum levels have been reported when given with omeprazole. 7.2 Drugs for Which Gastric pH Can Affect Bioavailability Due to its effects on gastric acid secretion, esomeprazole can reduce the absorption of drugs where gastric pH is an important determinant of their bioavailability. Like with other drugs that decrease the intragastric acidity, the absorption of drugs such as ketoconazole, atazanavir, iron salts, erlotinib, and mycophenolate mofetil (MMF) can decrease, while the absorption of drugs such as digoxin can increase during treatment with esomeprazole. Esomeprazole is an enantiomer of omeprazole. Concomitant treatment with omeprazole (20 mg daily) and digoxin in healthy subjects increased the bioavailability of digoxin by 10% (30%...
Contraindications
Esomeprazole magnesium delayed-release capsules are contraindicated in patients with known hypersensitivity to substituted benzimidazoles or to any component of the formulation. Hypersensitivity reactions may include anaphylaxis, anaphylactic shock, angioedema, bronchospasm, acute interstitial nephritis, and urticaria [see Adverse Reactions (6)]. For information about contraindications of antibacterial agents (clarithromycin and amoxicillin) indicated in combination with esomeprazole magnesium delayed-release capsules, refer to the CONTRAINDICATIONS section of their package inserts.
Overdosage
A single oral dose of esomeprazole at 510 mg/kg (about 124 times the human dose on a body surface area basis), was lethal to rats. The major signs of acute toxicity were reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. The symptoms described in connection with deliberate esomeprazole magnesium delayed-release capsules overdose (limited experience of doses in excess of 240 mg/day) are transient. Single doses of 80 mg of esomeprazole were uneventful. Reports of overdosage with omeprazole in humans may also be relevant. Doses ranged up to 2,400 mg (120 times the usual recommended clinical dose). Manifestations were variable, but included confusion, drowsiness, blurred vision, tachycardia, nausea, diaphoresis, flushing, headache, dry mouth, and other adverse reactions similar to those seen in normal clinical experience (see omeprazole package insert - Adverse Reactions). 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. For current information on treatment of any drug overdose contact a Poison Control Center at 1-800-222-1222.
How Supplied
Esomeprazole magnesium delayed-release capsules USP, 20 mg are White opaque size '4' hard gelatin capsule imprinted with ''H'' on cap and 'E2' on body filled with off white to pale yellow pellets. NDC 31722-664-30 bottles of 30 NDC 31722-664-90 bottles of 90 NDC 31722-664-10 bottles of 1000 Esomeprazole magnesium delayed-release capsules USP, 40 mg are white opaque size '3' hard gelatin capsule imprinted with ''H'' on cap and 'E3' on body filled with off white to pale yellow pellets. NDC 31722-665-30 bottles of 30 NDC 31722-665-90 bottles of 90 NDC 31722-665-10 bottles of 1000 Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Keep esomeprazole magnesium delayed-release capsules, USP container tightly closed. Dispense in a tight container if the esomeprazole magnesium delayed-release capsules, USP product package is subdivided.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.