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Journal of Antimicrobial Chemotherapy (2000) 45, 417-420
© 2000 The British Society for Antimicrobial Chemotherapy


Leading article

NNRTIs—a new class of drugs for HIV

Susan M. Drake*

Department of Sexual Medicine, Heartlands Hospital, Birmingham B9 5SS, UK

The non-nucleoside reverse transcriptase inhibitors (NNRTIs), nevirapine and efavirenz, are now licensed for the treatment of human immunodeficiency virus (HIV) infections. A third compound, delavirdine, is licensed in the USA and available in Europe on expanded access programmes. The place of NNRTIs in HIV therapy is determined by their pharmacology, their potency and their acceptability to patients.

The pharmacologist's perspective

The NNRTIs are a disparate group of compounds that act by blocking HIV-1 reverse transcriptase by direct binding. They require neither intracellular phosphorylation nor significantly affect other enzyme systems. As the three drugs differ structurally they have different pharmacokinetic properties. Both efavirenz and nevirapine have long half-lives, such that efavirenz is given once daily and nevirapine twice daily (once daily for the first 2 weeks). Delavirdine requires a three times daily dosing regimen. All are well absorbed after administration without food restrictions, and efavirenz and nevirapine in particular have mean trough plasma concentrations . . . [Full Text of this Article]

The physician's perspective

The patient's perspective

The future

Notes

References


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E. N. Peletskaya, A. A. Kogon, S. Tuske, E. Arnold, and S. H. Hughes
Nonnucleoside Inhibitor Binding Affects the Interactions of the Fingers Subdomain of Human Immunodeficiency Virus Type 1 Reverse Transcriptase with DNA
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[Abstract] [Full Text] [PDF]