Aulcer - General Information
A highly effective inhibitor of gastric acid secretion used in the therapy of stomach ulcers and zollinger-ellison syndrome. The drug inhibits the H(+)-K(+)-ATPase (H(+)-K(+)-exchanging ATPase) in the proton pump of gastric parietal cells.
Pharmacology of Aulcer
Aulcer 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. Aulcer 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, omeprazole 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.
Aulcer for patients
PRILOSEC Delayed-Release Capsules should be taken before eating. Patients should be cautioned that the PRILOSEC Delayed-Release Capsule should not be opened, chewed or crushed, and should be swallowed whole.
For patients who have difficulty swallowing capsules, the contents of a PRILOSEC Delayed-Release Capsule can be added to applesauce. One tablespoon of applesauce should be added to an empty bowl and the capsule should be opened. All of the pellets inside the capsule should be carefully emptied on the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately with a glass of cool water to ensure complete swallowing of the pellets. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellets/applesauce mixture should not be stored for future use.
Omeprazole can prolong the elimination of diazepam, warfarin and phenytoin, drugs that are metabolized by oxidation in the liver. Although in normal subjects no interaction with theophylline or propranolol was found, there have been clinical reports of interaction with other drugs metabolized via the cytochrome P-450 system (e.g., cyclosporine, disulfiram, benzodiazepines). Patients should be monitored to determine if it is necessary to adjust the dosage of these drugs when taken concomitantly with omeprazole.
Because of its profound and long lasting inhibition of gastric acid secretion, it is theoretically possible that omeprazole may interfere with absorption of drugs where gastric pH is an important determinant of their bioavailability (e.g., ketoconazole, ampicillin esters, and iron salts). In the clinical trials, antacids were used concomitantly with the administration of omeprazole.
Combination Therapy with Clarithromycin
Co-administration of omeprazole and clarithromycin may result in increases in plasma levels of ompeprazole, clarithromycin, and 14-hydroxy-clarithromycin.
Concomitant administration of clarithromycin with cisapride, pimozide, or terfenadine is contraindicated.
There have been reports of an intereaction between erythromycin and astemizole resulting in QT prolongation and torsades de points. Concomitant administration of erythromycin and astemizole is contraindicated. Because clarithromycin is also metabolized by cytochrome P450, concomitant administration of clarithromycin with astemizole is not recommended.
Omeprazole delayed-release capsules are contraindicated in patients with known hypersensitivity to any component of the formulation.
Additional information about Aulcer
Aulcer Indication: For the treatment of gastroesophageal reflux disease.
Mechanism Of Action: Aulcer 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, omeprazole blocks the final step in acid production, thus reducing gastric acidity.
Drug Interactions: Alprazolam Aulcer increases the effect of benzodiazepine
Diazepam Aulcer increases the effect of benzodiazepine
Clonazepam Aulcer increases the effect of benzodiazepine
Clorazepate Aulcer increases the effect of benzodiazepine
Chlordiazepoxide Aulcer increases the effect of benzodiazepine
Estazolam Aulcer increases the effect of benzodiazepine
Flurazepam Aulcer increases the effect of benzodiazepine
Halazepam Aulcer increases the effect of benzodiazepine
Ketazolam Aulcer increases the effect of benzodiazepine
Midazolam Aulcer increases the effect of benzodiazepine
Prazepam Aulcer increases the effect of benzodiazepine
Quazepam Aulcer increases the effect of benzodiazepine
Triazolam Aulcer increases the effect of benzodiazepine
Mephenytoin Aulcer increases the effect of hydantoin
Phenytoin Aulcer increases the effect of hydantoin
Fosphenytoin Aulcer increases the effect of hydantoin
Ethotoin Aulcer increases the effect of hydantoin
Voriconazole Voriconazole increases the effect and toxicity of omeprazole
St. John's Wort St. John's Wort decreases the levels/effects of omeprazole
Methotrexate Aulcer increases the levels of methotrexate
Cilostazol Aulcer increases the effect of cilostazol
Atazanavir This gastric pH modifier decreases the levels/effects of atazanavir
Cyclosporine Aulcer increases the effect and toxicity of cyclosporine
Dasatinib Possible decreased levels of dasatinib
Enoxacin The agent decreases the absorption of enoxacin
Indinavir Aulcer decreases the absorption of indinavir
Itraconazole The proton pump inhibitor decreases the absorption of the imidazole
Ketoconazole The proton pump inhibitor decreases the absorption of the imidazole
Disopyramide The beta-blocker increases toxicity of disopyramide
Food Interactions: Avoid alcohol.
Take 30-60 minutes before meals.
Generic Name: Omeprazole
Synonyms: Omeprazol [Inn-Spanish]; Omeprazolum [Inn-Latin]; OMEP; OMZ; OMP; Omeprazole magnesium
Drug Category: Anti-Ulcer Agents; Proton-pump Inhibitors
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Omeprazole: Antra; Audazol; Aulcer; Belmazol; Ceprandal; Danlox; Demeprazol; Desec; Dizprazol; Dudencer; Elgam; Emeproton; Epirazole; Erbolin; Exter; Gasec; Gastrimut; Gastroloc; Gibancer; Indurgan; Inhibitron; Inhipump; Lensor; Logastric; Lomac; Losec; Mepral; Miol; Miracid; Mopral; Morecon; Nilsec; Nopramin; Ocid; Olexin; Omapren; Omebeta 20; Omed; Omegast; Omepral; Omeprazon; Omeprol; Omesek; Omezol; Omezolan; Omid; Omisec; Omizac; Ompanyt; Ortanol; Osiren; Ozoken; Paprazol; Parizac; Pepticum; Pepticus; Peptilcer; Prazentol; Prazidec; Prazolit; Prilosec; Procelac; Proclor; Prysma; Ramezol; Regulacid; Result; Sanamidol; Secrepina; Tedec Ulceral; Ulceral; Ulcesep; Ulcometion; Ulcozol; Ulcsep; Ulsen; Ultop; Ulzol; Victrix; Zefxon; Zegerid; Zepral; Zimor; Zoltum;
Absorption: Absorption is rapid, absolute bioavailability (compared to intravenous administration) is about 30-40% at doses of 20-40 mg.
Toxicity (Overdose): Symptoms of overdose include confusion, drowsiness, blurred vision, tachycardia, nausea, diaphoresis, flushing, headache, and dry mouth.
Protein Binding: 95%
Half Life: 0.5-1 hour
Dosage Forms of Aulcer: Capsule, delayed release Oral
Tablet, delayed release Oral
Chemical IUPAC Name: 6-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole
Chemical Formula: C17H19N3O3S
Omeprazole on Wikipedia: http://en.wikipedia.org/wiki/Omeprazole
Organisms Affected: Humans and other mammals