Omeprazole: profile and news






STABILITY OF OMEPRAZOLE SODIUM AND PANTOPRAZOLE SODIUM DILUTED FOR ...  Apr 21, 2006
Currently, the manufacturers of omeprazole and pantoprazole injections recommend that infusions prepared by dilution in NaCl 0.9% should be used within 12 or 3 ... - The Journal of Pharmacy Technology

'Medicare Part D': What the Benefit Means For Medical Technology  May 15, 2006
In this case, the very effective and safe proton-pump inhibitor (PPI) drugs (such as omeprazole) actually have a viable alternative in the form of minimally ... - ePrairie,

EXCELLUS BLUECROSS BLUESHIELD LAUNCHES CAMPAIGN TO HELP CONSUMERS ...  May 15, 2006
...very expensive brand drugs. "One of the most overlooked generic options for treating heartburn is omeprazole. About 10 percent of ... - Empire Information Services, Inc. (press release),

Santarus Reports First Quarter 2006 Financial Results; Conference ...  May 4, 2006
...-- US Food and Drug Administration (FDA) approval of a New Drug Application (NDA) for ZEGERID(R) (omeprazole/sodium bicarbonate) Capsules in late February. ... - Genetic Engineering News,

Goitre and reduced acid secretion  May 10, 2006
...reduction included infection with the ulcer germ H pylori, an autoimmune inflammation of the stomach or taking the acid lowering medication omeprazole – Losec ... - ABC Message Stick,

Zentiva NV 1st Quarter Results 2006  May 2, 2006
...three months of 2006 included the anti-inflammatory Coxtral (nimesulide), the analgesic Tralgit (tramadol), the anti-ulcer drug Helicid (omeprazole) and the ... - PharmaLive.com (press release),

Nasal spray dependence is a hard habit to break  May 10, 2006
...over the counter. These drugs were the standard treatment for acid reflux before Prilosec (omeprazole) was developed. Q: I have ... - Daily Press,

Schwarz Pharma First-Quarter Profit Doubles (Update2)  Apr 24, 2006
The product, generic omeprazole, helped sales peak at 1.5 billion euros in 2003 and is still its single-biggest source of revenue. ... - Bloomberg

Off-Label Drug Use  May 2, 2006
In the gastrointestinal system, we recently saw the human drug omeprazole licensed for use in the horse for the treatment of gastric ulcers (GastroGard). ... - TheHorse.com,

Schwarz Pharma Oper Profit Above Forecast  Apr 25, 2006
1014 GMT [Dow Jones] Schwarz Pharma (SRZ.XE) operating profit is ahead of expectations due to strong omeprazole sales and lower R&D expenses, says Bear Stearns ... - newratings.com

NSAIDs: Pain Relief or Pain in the Gut?  May 2, 2006
Anti-ulcer medication (eg omeprazole, ranitidine, cimetidine) can be used in horses which have to be on NSAIDs long term due to musculoskeletal problems. ... - TheHorse.com,

Thyroxine in Goiter, Helicobacter pylori Infection, and Chronic ...  Apr 26, 2006
...was prospectively studied in 11 patients treated with thyroxine before and after H. pylori infection and both before and during treatment with omeprazole in 10 ... - New England Journal of Medicine (subscription),

A method for weaning yourself off nasal spray  May 2, 2006
...over the counter. These drugs were the standard treatment for acid reflux before Prilosec (omeprazole) was developed. Q. I have ... - Charlotte Observer,

POZEN Reports First Quarter 2006 Results  Apr 27, 2006
...on a Special Protocol Assessment (SPA) for the pivotal Phase III clinical trial for its product candidate PN 200, the combination of omeprazole and naproxen ... - Genetic Engineering News,

Santarus to Present at UBS Global Specialty Pharmaceuticals ...  Apr 18, 2006
...life for patients. The company's products are immediate-release formulations of omeprazole, a widely prescribed PPI. The company's ... - Genetic Engineering News,

Santarus to Hold First Quarter 2006 Financial Results Conference ...  Apr 24, 2006
...patients. The company's products are immediate-release formulations of omeprazole, a widely prescribed proton pump inhibitor (PPI). ... - Genetic Engineering News,

Indigestion defined  Apr 29, 2006
...adenosine triphosphate enzyme system�. Examples are omeprazole, pantoprazole, esomeprazole and lansoprazole. H. pylori can be ... - Malaysia Star,

First Quarter Report 2006: Schwarz Pharma with a Good Start  Apr 25, 2006
The company’s US subsidiary KUDCo maintained last year’s level of generic omeprazole sales in the first three months of 2006. ... - PharmaLive.com (press release),


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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