-transparent.png){kind=logo}
The metabolism of omeprazole to its two major metabolites, hydroxyomeprazole (OH-OPZ) and omeprazole sulfone (OPZ-SFN) was studied in rat liver microsomes by a reversed phase HPLC assay. The formation of metabolites of OPZ depended on incubation time, substrate concentration, microsomal protein concentration, and was found to be optimal at pH 7.4. The Vmax and Km of OPZ hydroxylation in the rat liver microsomal preparation were 2033 nmol/(min.mg protein) and 46.8 mumol.L-1 respectively. The maximum rate of formation of OPZ-SFN (Vmax) was 187.9 nmol/(min.mg protein), with a Km value of 120.7 mumol.L-1 in rat liver microsome. Moreover, the effects of 7 drugs on OPZ metabolism were tested. The results showed that mephenytoin, benzodiazepines (DZ, NDZ, TMZ, FNZ, NZ) and papaverine caused inhibition of OPZ metabolism, among them papaverine was the only fairly strong inhibitor.
L Zhao, and
Y Q Lou
January 1991,
Drug metabolism and disposition: the biological fate of chemicals,
L Zhao, and
Y Q Lou
January 1991,
Archives of toxicology,
L Zhao, and
Y Q Lou
October 1993,
Pharmacology,
L Zhao, and
Y Q Lou
February 1981,
Chemico-biological interactions,
L Zhao, and
Y Q Lou
September 1970,
European journal of biochemistry,
L Zhao, and
Y Q Lou
February 2005,
Yao xue xue bao = Acta pharmaceutica Sinica,
L Zhao, and
Y Q Lou
January 1996,
Yao xue xue bao = Acta pharmaceutica Sinica,
L Zhao, and
Y Q Lou
January 1996,
Yao xue xue bao = Acta pharmaceutica Sinica,
L Zhao, and
Y Q Lou
July 2012,
Phytotherapy research : PTR,
L Zhao, and
Y Q Lou
January 1988,
Drug metabolism and disposition: the biological fate of chemicals,
