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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

*  and
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)
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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 antiretrovirals; pharmacokinetics; drug interactions; protease inhibitors; non-nucleoside reverse transcriptase inhibitors; chemokine receptor antagonists; integrase inhibitors; therapeutic drug monitoring
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Rathbun, R.C.; Liedtke, M.D. Antiretroviral Drug Interactions: Overview of Interactions Involving New and Investigational Agents and the Role of Therapeutic Drug Monitoring for Management. Pharmaceutics 2011, 3, 745-781.

AMA Style

Rathbun RC, Liedtke MD. Antiretroviral Drug Interactions: Overview of Interactions Involving New and Investigational Agents and the Role of Therapeutic Drug Monitoring for Management. Pharmaceutics. 2011; 3(4):745-781.

Chicago/Turabian Style

Rathbun, R. Chris; Liedtke, Michelle D. 2011. "Antiretroviral Drug Interactions: Overview of Interactions Involving New and Investigational Agents and the Role of Therapeutic Drug Monitoring for Management." Pharmaceutics 3, no. 4: 745-781.


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