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Pharmacokinetics and pharmacodynamics of esomeprazole, the S‐isomer of omeprazole
Author(s) -
Andersson T.,
RÖhss K.,
Bredberg E.,
HassanAlin M.
Publication year - 2001
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 - 10.1046/j.1365-2036.2001.01087.x
Subject(s) - esomeprazole , omeprazole , pharmacokinetics , proton pump inhibitor , pharmacodynamics , medicine , pentagastrin , pharmacology , gastric acid , crossover study , chemistry , stomach , alternative medicine , pathology , placebo
Background: Esomeprazole, the S‐isomer of omeprazole, is the first proton pump inhibitor developed as a single isomer for the treatment of acid‐related diseases. Aim: To examine the pharmacokinetics and pharmacodynamics of esomeprazole. Methods: In a crossover study, 12 healthy males received 5, 10 or 20 mg of esomeprazole, or 20 mg of omeprazole, once daily over 5 days. The pharmacokinetics and effects on pentagastrin‐stimulated peak acid output of esomeprazole and omeprazole were studied on days 1 and 5. Results: The area under the curve ( AUC ) of both esomeprazole and omeprazole increased from day 1 to day 5. The correlation between acid inhibition and AUC for esomeprazole could be well described with a sigmoid E max model. The mean inhibition values of the pentagastrin‐stimulated peak acid output on day 1 for 5, 10 and 20 mg of esomeprazole were 15%, 29% and 46%, respectively; the corresponding day 5 values were 28%, 62% and 90%. The mean inhibition values of the pentagastrin‐stimulated peak acid output for omeprazole were 35% (day 1) to 79% (day 5). Conclusions: The pharmacokinetics of esomeprazole are time and dose dependent. There was a good correlation between AUC and effect for esomeprazole. These data suggest an increased acid inhibitory effect of esomeprazole compared to omeprazole.