2005•British Journal of Clinical PharmacologyOpen access

Pharmacokinetic evidence for the induction of lopinavir metabolism by efavirenz

Éric Dailly, Clotilde Allavena, François Raffi, Pascale Jolliet

Abstract

AIMS: The influence of efavirenz on lopinavir pharmacokinetics was investigated using a population approach. METHODS: Forty-five HIV patients treated with lopinavir/ritonavir plus efavirenz (A) and 24 patients treated with lopinavir/ritonavir plus nucleoside/nucleotide reverse transcriptase inhibitors (B) were studied. RESULTS: A relationship (P < 0.01) was established between the elimination rate constant of lopinavir (k(10)) and treatment with efavirenz. Mean k(10) was higher in group A than in group B (0.3838 vs 0.2810 h(-1)) (P < 0.001, 95% confidence interval for difference between means 0.1004, 0.1052). CONCLUSIONS: These results suggest that lopinavir metabolism is induced by efavirenz.

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Key concepts: Lopinavir, Efavirenz, Ritonavir, Reverse-transcriptase inhibitor, Lopinavir/ritonavir, Pharmacokinetics, Confidence interval, Pharmacology