Esomeprazole Magnesium (5 brand names, 5 dosage forms, 1 route)
Available dosage forms: FOR SUSPENSION, DELAYED RELEASE, CAPSULE, DELAYED RELEASE, CAPSULE, DELAYED REL PELLETS, TABLET, DELAYED RELEASE, TABLET, ORALLY DISINTEGRATING, DELAYED RELEASE.
Routes of administration: ORAL.
Brand Names
- ESOMEPRAZOLE MAGNESIUM
- NAPROXEN AND ESOMEPRAZOLE MAGNESIUM
- NEXIUM
- NEXIUM 24HR
- VIMOVO
Dosage and Administration
N/A
Contraindications
• Esomeprazole magnesium is 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 tubulointerstitial nephritis, and urticaria [see Warnings and Precautions (5.2) , Adverse Reactions (6.2)] . • For information about contraindications of amoxicillin and clarithromycin, indicated in combination with esomeprazole magnesium for H. pylori eradication to reduce the risk of duodenal ulcer recurrence, refer to the Contraindications section of the respective prescribing information. • Proton pump inhibitors (PPIs), including esomeprazole magnesium, are contraindicated in patients receiving rilpivirine-containing products [see Drug Interactions (7) ].
Warnings and Precautions
N/A
Adverse Reactions
The following serious adverse reactions are described below and elsewhere in labeling: • Acute Tubulointerstitial Nephritis [ see Warnings and Precautions (5.2)] • Clostridium difficile-Associated Diarrhea [ see Warnings and Precautions (5.3)] • Bone Fracture [ see Warnings and Precautions (5.4)] • Severe Cutaneous Adverse Reactions [ see Warnings and Precautions (5.5)] • Cutaneous and Systemic Lupus Erythematosus [ see Warnings and Precautions (5.6)] • Cyanocobalamin (Vitamin B-12) Deficiency [ see Warnings and Precautions (5.8)] • Hypomagnesemia and Mineral Metabolism [ see Warnings and Precautions (5.9)] • Fundic Gland Polyps [ see Warnings and Precautions (5.13)]
Drug Interactions
Tables 3 and 4 include drugs with clinically important drug interactions and interaction with diagnostics when administered concomitantly with esomeprazole and instructions for preventing or managing them. Consult the labeling of concomitantly used drugs to obtain further information about interactions with PPIs. Table 3: Clinically Relevant Interactions Affecting Drugs Co-Administered with Esomeprazole and Interaction with Diagnostics Antiretrovirals Clinical Impact: The effect of PPIs on antiretroviral drugs is variable. The clinical importance and the mechanisms behind these interactions are not always known. • Decreased exposure of some antiretroviral drugs (e.g., rilpivirine atazanavir, and nelfinavir) when used concomitantly with esomeprazole may reduce antiviral effect and promote the development of drug resistance [ see Clinical Pharmacology (12.3)]. • Increased exposure of other antiretroviral drugs (e.g., saquinavir) when used concomitantly with esomeprazole may increase toxicity [ see Clinical Pharmacology (12.3)]. • There are other antiretroviral drugs which do not result in clinically relevant interactions with esomeprazole. Intervention: Rilpivirine-containing products: Concomitant use with esomeprazole magnesium is contraindicated [ see Contraindications (4)] . Atazanavir: See prescribing information for atazanavir for dosing information. Nelfinavir: Avoid concomitant use with esomeprazole magnesium. See prescribing information for nelfinavir. Saquinavir: See the prescribing information for saquinavir for monitoring of potential saquinavir-related toxicities. Other antiretrovirals: See prescribing information for specific antiretroviral drugs. Warfarin Clinical Impact: Increased INR and prothrombin time in patients receiving PPIs, including esomeprazole, and warfarin concomitantly. Increases in INR and prothrombin time may lead to abnormal bleeding and even death. Intervention: Monitor INR and prothrombin time and adjust the dose of warfarin, if neede
Mechanism of Action
Esomeprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell. Esomeprazole is protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphenamide. Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, esomeprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.
Overdosage
Manifestations in patients exposed to omeprazole, the racemic mixture, at doses up to 2,400 mg (120 times the usual recommended clinical dose) include confusion, drowsiness, blurred vision, tachycardia, nausea, diaphoresis, flushing, headache, dry mouth, and other adverse reactions similar to those seen at recommended dosages. See the full prescribing information for omeprazole for complete safety information. 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. If over-exposure occurs, call your Poison Control Center at 1-800-222-1222 for current information on the management of poisoning or overdosage.