Effect of mibefradil on CYP3A4 in vivo

• Published in: Journal of clinical pharmacology Vol. 43; no. 10; p. 1091
• Main Authors: Veronese, Maria L, Gillen, Lisa P, Dorval, Ellen P, Hauck, Walter W, Waldman, Scott A, Greenberg, Howard E
• Format: Journal Article
• Language: English
• Published: England 01.10.2003
• Subjects: Adult; Breath Tests - methods; Carbon Radioisotopes; Cross-Over Studies; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System - drug effects; Cytochrome P-450 Enzyme System - metabolism; Drug Combinations; Drug Interactions; Erythromycin - administration & dosage; Erythromycin - analogs & derivatives; Erythromycin - metabolism; Erythromycin - pharmacokinetics; Erythromycin - urine; Humans; Intestines - enzymology; Liver - enzymology; Male; Metabolic Clearance Rate - drug effects; Mibefradil - administration & dosage; Mibefradil - blood; Mibefradil - pharmacokinetics; Midazolam - blood; Midazolam - pharmacokinetics; Molecular Probes; Single-Blind Method

Mibefradil, a calcium channel blocker, was removed from the market because of adverse drug interactions with coadministered CYP3A4 substrates. This study examined the effect of mibefradil on the activity of hepatic and intestinal CYP3A4 in vivo, employing the erythromycin breath test (EBT) and oral...