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Expert Opin Drug Metab Toxicol. 2015 Jun;11(6):893-905. doi: 10.1517/17425255.2015.1027682. Epub 2015 Mar 22.

Pharmacokinetics of antiretrovirals in mucosal tissue.

Author information

1
University of North Carolina, UNC Eshelman School of Pharmacy, Division of Pharmacotherapy and Experimental Therapeutics , 1094 Genetic Medicine Building, CB# 7361, 120 Mason Farm Road, Chapel Hill, NC 27599 , USA +1 919 966 9998 ; +1 919 962 0644 ; akashuba@unc.edu.

Abstract

INTRODUCTION:

In the absence of an HIV vaccine or cure, antiretroviral (ARV)-based prevention strategies are being investigated to reduce HIV incidence. These prevention strategies depend on achieving effective drug concentrations at the site of HIV exposure, which is most commonly the mucosal tissue of the lower gastrointestinal tract and the female genital tract.

AREAS COVERED:

This article collates all known data regarding drug exposure in these vulnerable mucosal tissues and reviews important mechanisms of ARV drug distribution. Research papers and abstracts describing ARV pharmacokinetics (PK) in the female genital tract and lower gastrointestinal mucosal tissues available in MEDLINE® or presented at scientific conferences prior to December 2014 are reviewed in detail. Important influences on ARV mucosal tissue distribution, including protein binding, active drug transport and endogenous hormones are also reviewed.

EXPERT OPINION:

ARVs exhibit highly variable PK in mucosal tissues. In general, ARV exposure is higher in the lower gastrointestinal tract compared with the female genital tract, but concentrations required for protective efficacy are largely unknown. The expected site of HIV exposure represents an important consideration when designing and optimizing ARV-based prevention strategies.

KEYWORDS:

HIV prevention; antiretroviral; mucosal tissue; pharmacokinetics

PMID:
25797064
PMCID:
PMC4498566
DOI:
10.1517/17425255.2015.1027682
[Indexed for MEDLINE]
Free PMC Article

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