Pharmacokinetic evidence for the induction of lopinavir metabolism by efavirenz

Article date: July 2005

By: Eric Dailly, Clotilde Allavena, François Raffi, Pascale Jolliet, in Volume 60, Issue 1, pages 32-34

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 (k₁₀) and treatment with efavirenz. Mean k₁₀ 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.

DOI: 10.1111/j.1365-2125.2005.02369.x

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