Pharmacokinetic evidence for the induction of lopinavir metabolism by efavirenz.

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.