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Esomeprazole_magnesium: profile and news
New Esomeprazole Magnesium Data in Non-cardiac Chest Pain Nov 18, 2005 AstraZeneca files suit against Ranbaxy Nov 22, 2005 AstraZeneca Plc to sue Ranbaxy on ulcer drug Nov 22, 2005 ASTRAZENECA: AstraZeneca Commences Patent Infringement Litigation ... Nov 28, 2005 AstraZeneca files suit against Ranbaxy Nov 22, 2005 Suit seeks to block copy of Nexium Nov 22, 2005 AstraZeneca sues Ranbaxy over Nexium Nov 22, 2005 AstraZeneca files suit against Ranbaxy Nov 22, 2005 On the Move: Metro, STM, Air France-KLM Nov 22, 2005 AstraZeneca Provides Additional Support to Hurricane Victims Nov 17, 2005 AstraZeneca Provides Additional Support to Hurricane Victims Nov 17, 2005 (PRN) - Beaujolais Teams Up with European Olive Oils for a ... Nov 18, 2005 Astrazaneca’s Nexium threatened Oct 19, 2005 Ranbaxy challenges AstraZeneca's Nexium patent in US Oct 19, 2005 AstraZeneca: Nexium ANDA Oct 18, 2005 Indian company challenges Nexium Oct 19, 2005 Business Roundup Oct 19, 2005 AstraZeneca Pledges More Than $1 Million in Contributions and ... Sep 1, 2005 AstraZeneca Pledges More Than $1 Million in Contributions and ... Sep 1, 2005 AstraZeneca Signs on to PhRMA Guidelines as Part of the Company's ... Aug 2, 2005 AstraZeneca Signs on to PhRMA Guidelines as Part of the Company's ... Aug 2, 2005 Patent Term and Opportunities for Managing IT Jun 1, 2005 FDA Approves IV Esomeprazole magnesium for Short-term Treatment of ... Apr 1, 2005 FDA Approvals: Nexium IV, Zofran, Xibrom Apr 7, 2005 FDA approves AstraZeneca's intravenous Nexium Apr 5, 2005 FDA Approvals: Nexium IV, Zofran, Xibrom 08 Apr 2005 FDA Approves IV Esomeprazole magnesium for Short-term Treatment of ... Apr 1, 2005 FDA approves AstraZeneca's intravenous Nexium Apr 5, 2005 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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