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Esomeprazole: profile and news
The Utility of Nexium in Chronic Cough and Reflux Disease Feb 10, 2006 HEARTBURN PATIENTS UNAWARE OF LONG-TERM RISK Feb 23, 2006 The Asthma-Acid Reflux Connection Feb 17, 2006 AstraZeneca launches Toprol-XL appeal Feb 17, 2006 Toprol XL uncertainty weighs heavy on AstraZeneca Feb 3, 2006 Breaking News ** Profits surge at AstraZeneca in Q4 Feb 2, 2006 Other information Indication For the treatment of acid-reflux disorders (GERD) and peptic ulcer disease Pharmacology Esomeprazole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and H. pylori eradication to reduce the risk of duodenal ulcer recurrence. Esomeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell. 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. Mechanism Of Action Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, Esomeprazole blocks the final step in acid production, thus reducing gastric acidity. Drug Category Antihistamines; Anti-Ulcer Agents; Enzyme Inhibitors; Proton-pump Inhibitors; ATC:A02BC05 Brand Names/Synonyms Esomeprazole; Esomeprazole Magnesium; Esomeprazole Sodium; Esomeprazole and Salts; Esomperazole; Nexiam; Nexium; Nexium Iv; Omeprazole; Prilosec; Zegerid Dosage Forms TABLET (DELAYED-RELEASE); DELAYED-RELEASE CAPSULES; IV Injection Solution; IV Iufusion Solution Absorption 90% Interactions -->Interactions for Esomeprazole: 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. Post-marketing reports of changes in prothrombin measures have been received among patients on concomitant warfarin and esomeprazole therapy. Increases in INR and prothrombin time may lead to abnormal bleeding and even death. Patients treated with proton pump inhibitors and warfarin concomitantly may need to be monitored for increases in INR and prothrombin time. Esomeprazole may potentially interfere with CYP2C19, the major esomeprazole metabolizing enzyme. Coadministration of esomeprazole 30 mg and diazepam, a CYP2C19 substrate, resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam were observed 12 hours after dosing and onwards. However, at that time, the plasma levels of diazepam were below the therapeutic interval, and thus this interaction is unlikely to be of clinical relevance. Esomeprazole inhibits gastric acid secretion. Therefore, esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (eg, ketoconazole, iron salts and digoxin). Coadministration of oral contraceptives, diazepam, phenytoin, or quinidine did 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. Concomitant administration of clarithromycin with pimozide is contraindicated. Chemical IUPAC Name 5-methoxy-2-[(4-methoxy-3,5-dimethyl-pyridin-2-yl)methylsulfinyl]-3H-benzoimidazole Chemical Formula C17H19N3O3S Half Life 1-1.5 hours Drug Type Approved Drug # Accession No APRD00363 CAS Registry Number 161796-78-7 |
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