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Clinical Pharmacokinetics
Published in: Clinical Pharmacokinetics 12/2001

01-12-2001 | Review Articles

Clinical Pharmacokinetics of Non-Nucleoside Reverse Transcriptase Inhibitors

Authors: Dr Patrick F. Smith, Robert DiCenzo, Gene D. Morse

Published in: Clinical Pharmacokinetics | Issue 12/2001

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Abstract

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are a diverse group of compounds that induce allosteric changes in the human immunodeficiency virus type 1 (HIV-1) reverse transcriptase, thus rendering the enzyme incapable of converting viral RNA to DNA. Unlike nucleoside analogue inhibitors of reverse transcriptase, NNRTIs do not require sequential phosphorylation to elicit antiretroviral activity.
There are currently 3 approved NNRTIs: nevirapine, delavirdine and efavirenz. Although possessing a common mechanism of action, these agents can be differentiated by both molecular and pharmacokinetic characteristics. Each of the NNRTIs is metabolised to some degree by the cytochrome P450 (CYP) system of enzymes, making them prone to clinically significant drug interactions. In addition, they elicit variable effects on other medications, acting as either inducers or inhibitors of drugs metabolised by CYP. These drug interactions are an important consideration in the clinical use of these agents as a part of combination antiretroviral therapy. Additional factors such as the influence of food and pH on oral absorption, and protein binding, must also be considered.
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Metadata
Title
Clinical Pharmacokinetics of Non-Nucleoside Reverse Transcriptase Inhibitors
Authors
Dr Patrick F. Smith
Robert DiCenzo
Gene D. Morse
Publication date
01-12-2001
Publisher
Springer International Publishing
Published in
Clinical Pharmacokinetics / Issue 12/2001
Print ISSN: 0312-5963
Electronic ISSN: 1179-1926
DOI
https://doi.org/10.2165/00003088-200140120-00002