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Effects of twenty-three drugs on the metabolism of FK506 by human liver microsomes

Iwasaki, K.; Matsuda, H.; Nagase, K.; Shiraga, T.; Tokuma, Y.; Uchida, K.

Research Communications in Chemical Pathology and Pharmacology 82(2): 209-216

1993

ISSN/ISBN: 0034-5164
PMID: 7508138
Document Number: 419935
We investigated the effects of 23 drugs on the metabolism of FK506 by human liver microsomes. Acyclovir, amphotericin B, cefixime, cefotaxime, ciprofloxacin, cyclosporin A, diltiazem, enoxacin, erythromycin, ethinyl estradiol, fluconazole, fosfomycin, kanamycin, lincomycin, loxoprofen, minocyclin, nifedipine, nilvadipine, norethindrone, ofloxacin, phenobarbital, prednisolone, or rifampicin was added to the reaction media at equimolar or at ten times an excess molar ratio of the substrate concentration; their effects on FK506 metabolism were examined. Drugs known to be the substrate of cytochrome P-450 3A inhibited the metabolism of FK506, and among the drugs tested, the inhibition by cyclosporin A and nifedipine was the strongest.

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