Clinical uses of non-nucleoside reverse transcriptase inhibitors.

Important note: Information in this article was accurate in 2000. The state of the art may have changed since the publication date.

Clinical uses of non-nucleoside reverse transcriptase inhibitors.

Rev Med Virol. 2000 Jul-Aug;10(4):217-29. Unique Identifier : AIDSLINE MED/20351799
Harris M; Montaner JS; AIDS Research Program, St. Paul's Hospital, Vancouver, B.C.,; Canada.

Abstract: Three non-nucleoside reverse transcriptase inhibitors (NNRTIs) are currently available for treatment of HIV-1 as part of combination antiretroviral therapy. Oral dosing is administered three times daily for delavirdine (DLV), twice daily for nevirapine (NVP), and once daily for efavirenz (EFV). Rash is a common side effect of all three NNRTIs, and early CNS side effects are also frequent with EFV. Hepatotoxicity is relatively uncommon but requires appropriate monitoring. Drug interactions mediated by the cytochrome P450 system are an important consideration when the NNRTIs are administered concomitantly with other drugs, including protease inhibitors (PIs). HIV strains with reduced susceptibility to NNRTIs can occur with a single mutation in the reverse transcriptase (RT) gene. The available NNRTIs exhibit overlapping genotypic resistance patterns, but newer agents may overcome this problem. NNRTIs have been studied in combination with nucleoside RT inhibitors for first-line HIV therapy, where they have shown at least equivalent antiviral efficacy compared with PI-based regimens over 1-2 years of therapy. NVP and EFV have also been studied as a replacement for a PI within a virologically successful regimen, with the aim of preventing or reducing PI toxicities and simplifying the dosing regimen. Such 'switch' strategies are successful for certain patients in maintaining virologic suppression for 6 months or more and result in varying degrees of improvement in PI-associated toxicities. NNRTIs may offer a benefit when included in salvage regimens for patients failing PI-based therapy, particularly in patients who have not previously been treated with NNRTIs. NVP has been shown to have a substantial favourable impact on the rate of vertical HIV-1 transmission with a simple, cost-effective regimen. Copyright 2000 John Wiley & Sons, Ltd.

Keywords: JOURNAL ARTICLE REVIEW REVIEW, TUTORIAL Anti-HIV Agents/PHARMACOKINETICS/*THERAPEUTIC USE Delavirdine/THERAPEUTIC USE Drug Therapy, Combination Human HIV Infections/*DRUG THERAPY Nevirapine/THERAPEUTIC USE Oxazines/THERAPEUTIC USE Randomized Controlled Trials Reverse Transcriptase Inhibitors/PHARMACOKINETICS/*THERAPEUTIC USE

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