Nevirapine once daily: pharmacology, metabolic profile and efficacy data of the new extended-release formulation

Nevirapine (NVP), a non-nucleoside reverse transcriptase inhibitor, has been an important component of HIV infection treatment for many years. Currently, twice-a-day dosing is required for the successful application of NVP immediate release (IR), but there is potential for a more convenient once-a-day antiretroviral combination.

The purpose of this article is to review the recent data on once-daily NVP extended release (XR) looking at all the important pharmacologic, pharmacokinetic and clinical data on NVP IR/XR through a systematic MEDLINE database search as well as a review of abstracts presented at international HIV meetings on NVP XR studies up to December 2010. The article provides the reader with an overview of all the pharmacodynamic and pharmacokinetic aspects of NVP IR/XR, as well as its preclinical and clinical efficacy and its safety.

NVP XR is as effective as NVP IR among HIV-infected patients with a similar safety profile. NVP XR requires careful monitoring during initiation, but its favorable lipid profile may be of clinical benefit in reducing the risk for coronary artery disease in HIV-infected patients who are receiving long-term antiretroviral therapy. Further research is needed to predict short-term toxicity.