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OMEPRAZOLE: EFFECTS ON OXIDATIVE DRUG METABOLISM IN THE RAT
Author(s) -
Henry D. A.,
Gerkens J. F.,
Brent P. J.,
Dosen P. J.
Publication year - 1986
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/j.1440-1681.1986.tb00916.x
Subject(s) - omeprazole , oxidative metabolism , drug metabolism , oxidative phosphorylation , metabolism , chemistry , drug , pharmacology , biochemistry , medicine
SUMMARY 1. Omeprazole, a substituted benzimidazole and a potent gastric antisecretory drug has been tested for inhibition of microsomal drug oxidative function in the rat. 2. A single dose of 40 mg/kg prolonged pentobarbitone sleeping times from 118 (range 73–168) min to 195 (159–222) min ( P < 0.01), pentobarbitone half‐lives from 89 (63–114) to 112 (54–146) min ( P < 0.05) and aminopyrine breath 14 CO 2 half‐lives from 43 (37–51) to 56 (49–79) min ( P < 0.05). Omeprazole in doses of 20 mg/kg or less had no significant effect. 3. In prolonging pentobarbitone sleeping times omeprazole 40 mg/kg and an equimolar (30 mg/kg) dose of cimetidine were approximately equipotent. 4. These results contrast with studies in man in which much smaller doses of omeprazole have been shown to produce clinically significant inhibition of drug metabolism.