Celecoxib inhibits metabolism of cytochrome P450 2D6 substrate metoprolol in humans

• Published in: Clinical pharmacology and therapeutics Vol. 74; no. 2; p. 130
• Main Authors: Werner, Ulrike, Werner, Dierk, Rau, Thomas, Fromm, Martin F, Hinz, Burkhard, Brune, Kay
• Format: Journal Article
• Language: English
• Published: United States 01.08.2003
• Subjects: Adrenergic beta-Antagonists - pharmacokinetics; Adult; Area Under Curve; Aryl Hydrocarbon Hydroxylases - genetics; Aryl Hydrocarbon Hydroxylases - metabolism; Biotransformation; Celecoxib; Cross-Over Studies; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Cyclooxygenase Inhibitors - pharmacology; Cytochrome P-450 CYP2C9; Cytochrome P-450 CYP2D6 - genetics; Cytochrome P-450 CYP2D6 Inhibitors; Double-Blind Method; Genotype; Humans; Isoenzymes - metabolism; Lactones - pharmacology; Male; Membrane Proteins; Metoprolol - pharmacokinetics; Prostaglandin-Endoperoxide Synthases - metabolism; Pyrazoles; Sulfonamides - pharmacology; Sulfones

In vitro data have shown that celecoxib inhibits the metabolism of cytochrome P450 (CYP) 2D6 substrates. However, very limited data are available on the influence of cyclooxygenase 2 inhibitors on the disposition of CYP2D6 substrates in humans. Therefore the objective of this study was to examine th...