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Inhibitory effect of omeprazole on the metabolism of midazolam in vitro

Inhibitory effect of omeprazole on the metabolism of midazolam in vitro

  1. Anonymous
    Arzneimittelforschung. 1990 Oct;40(10):1105-7.
    Li G, Klotz U

    To examine the effect of omeprazole on the hepatic drug metabolizing enzyme system microsomes from rat and human liver samples were incubated with midazolam (CAS 59467-70-8) in the absence and presence of various concentrations of omeprazole (CAS 73590-58-6), its sulfone metabolite and for comparison also with cimetidine. In the extracted incubation mixtures unchanged midazolam, a-OH-midazolam, 4-OH-midazolam and di-OH-midazolam were analyzed by HPLC. In both species omeprazole (and its sulfone) inhibited the formation of all three oxidized metabolites of midazolam and the corresponding IC50-values (range 0.2-1.3 mmol/l for rat microsomes and 0.2-1.5 mmol/l for human microsomes) were comparable to cimetidine (range 0.05 to 3.8 mmol/l). These results indicate that the oxidative metabolism of midazolam can be inhibited in vitro by omeprazole (and/or its sulfone metabolite) and this interaction should be considered if both drugs are administered concomitantly in man.