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Monday 21 May 2012

Omeprazole


Class: Proton Pump Inhibitor
Mech.: Irreversible inhib. of H+/K+ ATPase → > 95% inhib. of acid secretion.

Absorption: Oral → 30-40% bioavail. Peak plasma levels at 0.5-3.5 hr. Give prior to meals, preferably in the morning. Additional dose, if necessary, should be given later in the day.
Dist.:
Metab.:
Excretion, t_: 0.5-1 hr.
Toxicity/S.E.s: Rare headache, diarrhea, rash. Inhib. of cyt. P-450 requires altered doses of warfarin, phenytoin, diazepam, and cyclosporin. Inhib. of vitamin. B12 absorption.

Utility: PUD, erosive esophagitis, Zollinger-Ellison synd., GERD.
Special Features: Mismatch between pharmacokinetics & pharmacodynamics. Short t_, but actions last > 24 hr (irreversible binding). Acid inhib. → ↑ gastrin

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