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JAC Advance Access published online on August 18, 2006
Journal of Antimicrobial Chemotherapy, doi:10.1093/jac/dkl348
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© The Author 2006. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For Permissions, please e-mail: journals.permissions@oxfordjournals.org
Received February 28, 2006
Revised July 18, 2006
Accepted August 2, 2006

Breif report

Intracellular and plasma efavirenz concentrations in HIV-infected patients switching from successful protease inhibitor-based highly active antiretroviral therapy (HAART) to efavirenz-based HAART (SUSTIPHAR Study)

Sarah Djabarouti 1, Dominique Breilh 1 *, Isabelle Pellegrin 2, Michel Lavit 3, Fabrice Camou 4, Olivier Caubet 4, Hervé Fleury 2, Marie-Claude Saux 5, and Jean-Luc Pellegrin 4

1 Department of Clinical Pharmacokinetics EA525, Victor Segalen Bordeaux 2 University, Bordeaux, France; Pharmacy Haut-Lévêque Hospital, CHU Bordeaux, Pessac, France
2 Department of Clinical Virology, Pellegrin Hospital, CHU Bordeaux, France
3 Department of Pharmacokinetics and Toxicology, Rangueil-Larrey Hospital, Toulouse, France
4 Department of Internal Medicine and Infectious Diseases, Haut-Lévêque Hospital, CHU Bordeaux, Pessac, France
5 Department of Clinical Pharmacokinetics EA525, Victor Segalen Bordeaux 2 University, Bordeaux, France, and Pharmacy Haut-Lévêque Hospital, CHU Bordeaux, Pessac, France

* To whom correspondence should be addressed.
Dominique Breilh, E-mail: dominique.breilh{at}chu-bordeaux.fr


  Abstract

Objectives: To assess intracellular and plasma efavirenz concentrations in HIV-infected patients who switched to efavirenz-based highly active antiretroviral therapy (HAART) from successful protease inhibitor-based HAART.

Patients and methods: A total of 49 patients were included in this observational cohort study. At inclusion, all patients had plasma HIV-RNA levels <50 copies/mL and switched to efavirenz combined with two nucleoside reverse transcriptase inhibitors. Intracellular and plasma concentrations were measured 12 h post-dose, 1 month (M1) and 6 months (M6) after starting efavirenz. Virological success (VS) was defined as plasma HIV-RNA level <50 copies/mL within the first 12 months and remaining undetectable at the end of the follow-up.

Results: VS was documented in 48 patients for at least 12 months (range 12-78 months). High inter-patient variabilities of intracellular and plasma efavirenz concentrations were observed (coefficients of variation >40%). At M1 and M6, respectively, median [Q1; Q3] intracellular efavirenz concentrations were 5300 [2830; 11 530] and 6790 [3870; 8790] ng/mL, median plasma efavirenz concentrations were 2050 [1600; 3100] and 2100 [1410; 2500] ng/mL. No correlation was found between intracellular and plasma concentrations. Plasma efavirenz levels exceeded the proposed threshold of 1000 ng/mL in 96% of patients from M1.

Conclusions: For moderately pre-treated HIV-infected patients with few mutations who switched to efavirenz from previous successful HAART, the proposed plasma efficacy-threshold was reached without any dosage adaptation. VS was maintained beyond 12 months, despite high inter-patient and intra-patient variabilities of intracellular and plasma efavirenz concentrations.

Keywords: pharmacokinetics; therapeutic drug monitoring; drug efflux; drug metabolism.
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