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Review article: immediate‐release proton‐pump inhibitor therapy – potential advantages
Author(s) -
HOWDEN C. W.
Publication year - 2005
Publication title -
alimentary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.308
H-Index - 177
eISSN - 1365-2036
pISSN - 0269-2813
DOI - 10.1111/j.1365-2036.2005.02709.x
Subject(s) - omeprazole , proton pump inhibitor , antacid , sodium bicarbonate , pharmacology , bicarbonate , gastric acid , pharmacokinetics , medicine , chemistry , stomach
Summary The absorption of most oral proton‐pump inhibitors is delayed by the enteric coating required to protect the acid‐labile proton‐pump inhibitor from degradation in the stomach and, as a result, antisecretory effect is also delayed. This article provides an overview of the pharmacokinetics and pharmacodynamics of a new immediate‐release omeprazole [(IR‐OME) Zegerid power for oral suspension; Santarus Inc., San Diego, CA, USA] and its potential advantages over delayed‐release proton‐pump inhibitors. Immediate‐release omeprazole has a higher mean peak plasma omeprazole concentration ( C max ) and a significantly shorter mean time to reach C max ( t max ) than delayed‐release omeprazole. Immediate‐release omeprazole 40 mg has a prolonged antisecretory effect with median intragastric pH above 4.0 for 18.6 h/day at steady‐state, after 7 days of once daily dosing. The sodium bicarbonate in immediate‐release omeprazole protects the uncoated omeprazole from degradation by gastric acid. The accelerated antisecretory action of immediate‐release omeprazole compared with delayed‐release omeprazole may be due to the activation of proton pumps by the rapid neutralization of intragastric acid by the sodium bicarbonate. The faster onset of action seen with immediate‐release omeprazole is not achieved by using an antacid with a delayed‐release proton‐pump inhibitor, because administering antacids with conventional delayed‐release proton‐pump inhibitors does not significantly enhance absorption of the proton‐pump inhibitor. In conclusion, immediate‐release omeprazole is associated with rapid absorption of omeprazole and rapid onset of antisecretory effect, without compromising the duration of acid suppression.