A prospective, controlled study assessing the effect of lopinavir on amprenavir concentrations boosted by ritonavir

• Published in: HIV medicine 2004-01, Vol.5 (1), p.15-17
• Main Authors: Mauss, S, Scholten, S, Wolf, E, Berger, F, Schmutz, G, Jaeger, H, Kurowski, M, Rockstroh, JK
• Format: Article
• Language: English
• Subjects: amprenavir; Anti-HIV Agents - administration & dosage; Anti-HIV Agents - blood; Anti-HIV Agents - pharmacology; Carbamates; Drug Interactions; Drug Therapy, Combination; HIV Protease Inhibitors - administration & dosage; HIV Protease Inhibitors - blood; HIV Protease Inhibitors - pharmacokinetics; HIV Seropositivity - drug therapy; Human immunodeficiency virus; Humans; Lopinavir; pharmacokinetics; Prospective Studies; Pyrimidinones - administration & dosage; Pyrimidinones - blood; Pyrimidinones - pharmacology; ritonavir; Ritonavir - administration & dosage; Ritonavir - blood; Ritonavir - pharmacology; Sulfonamides - administration & dosage; Sulfonamides - blood; Sulfonamides - pharmacokinetics
• ISSN: 1464-2662; 1468-1293
• DOI: 10.1111/j.1468-1293.2004.00179.x

In a controlled, prospective study, the efficacy of ritonavir 200 mg twice daily (bid) in inhibiting the decrease of amprenavir plasma concentrations caused by co‐administration of lopinavir was assessed. Twelve HIV‐seropositive patients were enrolled, and nine patients completed the 28‐day study. At day 14, plasma concentrations of amprenavir 600 mg bid and ritonavir 200 mg bid were determined over 12 h. At day 15, lopinavir 400 mg bid was added. At day 28, plasma concentrations of amprenavir, ritonavir and lopinavir were assessed. Co‐administration of lopinavir was found to decrease the amprenavir concentration, determined as the median area under the curve over 12 h (AUC12), by 25% (AUC12 24.9 μg/h/mL vs. 18.5 μg/h/mL; P