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• Liedtke, M
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Pharmaceutics 2011, 3(4), 745-781; doi:10.3390/pharmaceutics3040745

Review

Antiretroviral Drug Interactions: Overview of Interactions Involving New and Investigational Agents and the Role of Therapeutic Drug Monitoring for Management

R. Chris Rathbun*  and Michelle D. Liedtke

Department of Pharmacy: Clinical & Administrative Sciences, College of Pharmacy, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA

* Author to whom correspondence should be addressed.

Received: 5 August 2011; in revised form: 15 September 2011 / Accepted: 8 October 2011 / Published: 21 October 2011

(This article belongs to the Special Issue Drug Interactions of Antimicrobial Agents)

Download PDF Full-Text [302 KB, Updated Version, uploaded 25 October 2011 10:10 CEST]

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Abstract: Antiretrovirals are prone to drug-drug and drug-food interactions that can result in subtherapeutic or supratherapeutic concentrations. Interactions between antiretrovirals and medications for other diseases are common due to shared metabolism through cytochrome P450 (CYP450) and uridine diphosphate glucuronosyltransferase (UGT) enzymes and transport by membrane proteins (e.g., p-glycoprotein, organic anion-transporting polypeptide). The clinical significance of antiretroviral drug interactions is reviewed, with a focus on new and investigational agents. An overview of the mechanistic basis for drug interactions and the effect of individual antiretrovirals on CYP450 and UGT isoforms are provided. Interactions between antiretrovirals and medications for other co-morbidities are summarized. The role of therapeutic drug monitoring in the detection and management of antiretroviral drug interactions is also briefly discussed.

Keywords: antiretrovirals; pharmacokinetics; drug interactions; protease inhibitors; non-nucleoside reverse transcriptase inhibitors; chemokine receptor antagonists; integrase inhibitors; therapeutic drug monitoring

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