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01-07-2014 | Review Article

Pharmacokinetics of Antiretrovirals in Genital Secretions and Anatomic Sites of HIV Transmission: Implications for HIV Prevention

Authors: Christine R. Trezza, Angela D. M. Kashuba

Published in: Clinical Pharmacokinetics | Issue 7/2014

Abstract

The incidence of HIV remains alarmingly high in many parts of the world. Prophylactic use of antiretrovirals, capable of concentrating in the anatomical sites of transmission, may reduce the risk of infection after an unprotected sexual exposure. To date, orally and topically administered antiretrovirals have exhibited variable success in preventing HIV transmission in large-scale clinical trials. Antiretroviral mucosal pharmacokinetics may help explain the outcomes of these investigations. Penetration and accumulation of antiretrovirals into sites of transmission can influence dosing strategies and pre-exposure prophylaxis clinical trial design. Antiretroviral tissue distribution varies widely within and between drug classes, attributed in part to their physicochemical properties and tissue-specific drug transporter expression. Nucleoside(-tide) reverse transcriptase inhibitors, the CCR5 antagonist maraviroc, and the integrase inhibitor raltegravir demonstrate the highest penetration into the male and female reproductive tracts and colorectal tissue relative to blood. This review describes antiretroviral exposure in anatomic sites of transmission, and places these findings in context with the prevention of HIV and the efficacy of pre-exposure prophylactic strategies.

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Title: Pharmacokinetics of Antiretrovirals in Genital Secretions and Anatomic Sites of HIV Transmission: Implications for HIV Prevention
Authors: Christine R. Trezza
Angela D. M. Kashuba
Publication date: 01-07-2014
Publisher: Springer International Publishing
Published in: Clinical Pharmacokinetics / Issue 7/2014
Print ISSN: 0312-5963
Electronic ISSN: 1179-1926
DOI: https://doi.org/10.1007/s40262-014-0148-z

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Pharmacokinetics of Antiretrovirals in Genital Secretions and Anatomic Sites of HIV Transmission: Implications for HIV Prevention

Abstract

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

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