Identification of drugs inhibiting the in vitro metabolism of tacrolimus by human liver microsomes.
1. Tacrolimus, an immunosuppressive macrolide, is metabolized by enzymes of the cytochrome P450 3A subfamily. In this study, 34 drugs were tested for their interactions with tacrolimus metabolism by human liver microsomes. 2. Fifteen drugs which inhibit the in vitro metabolism of tacrolimus were identified: bromocriptine, corticosterone, dexamethasone, ergotamine, erythromycin, ethinyloestradiol, josamycin, ketoconazole, miconazole, midazolam, nifedipine, omeprazole, tamoxifen, troleandomycin and verapamil.
Christians
U
U
Institut für Allgemeine Pharmakologie, Medizinische Hochschule Hannover, Germany.
Schmidt
G
G
Bader
A
A
Lampen
A
A
Schottmann
R
R
Linck
A
A
Sewing
K F
KF
D001971:Bromocriptine / Q000494:pharmacology; D003345:Corticosterone / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008099:Liver / Q000187:drug effects / Q000378:metabolism*; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism*; D016559:Tacrolimus / Q000378:metabolism*
D001971:Bromocriptine; D003345:Corticosterone; D016559:Tacrolimus