Coadministration of lopinavir/ritonavir and phenytoin results in two-way drug interaction through cytochrome P-450 induction

• Published in: Journal of acquired immune deficiency syndromes (1999) Vol. 36; no. 5; p. 1034
• Main Authors: Lim, Michael L, Min, Sherene S, Eron, Joseph J, Bertz, Richard J, Robinson, Marjorie, Gaedigk, Andrea, Kashuba, Angela D M
• Format: Journal Article
• Language: English
• Published: United States 15.08.2004
• Subjects: Adult; Anticonvulsants - administration & dosage; Anticonvulsants - adverse effects; Anticonvulsants - pharmacokinetics; Cytochrome P-450 Enzyme System - biosynthesis; Cytochrome P-450 Enzyme System - genetics; Drug Interactions; Female; HIV Infections - complications; HIV Infections - drug therapy; HIV Protease Inhibitors - administration & dosage; HIV Protease Inhibitors - adverse effects; HIV Protease Inhibitors - pharmacokinetics; Humans; Lopinavir; Male; Pharmacogenetics; Phenytoin - administration & dosage; Phenytoin - adverse effects; Phenytoin - pharmacokinetics; Pyrimidinones - administration & dosage; Pyrimidinones - adverse effects; Pyrimidinones - pharmacokinetics; Ritonavir - administration & dosage; Ritonavir - adverse effects; Ritonavir - pharmacokinetics; Seizures - complications; Seizures - drug therapy

Lopinavir/ritonavir (LPV/RTV) is a CYP3A4 inhibitor and substrate; it also may induce cytochrome P-450 (CYP) isozymes. Phenytoin (PHT) is a CYP3A4 inducer and CYP2C9/CYP2C19 substrate. This study quantified the pharmacokinetic (PK) drug interaction between LPV/RTV and PHT. Open-label, randomized, mu...