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Pharmacological considerations on the use of antiretrovirals in pregnancy

Colbers, Angelaa,b; Greupink, Rickc; Burger, Davida,b

Current Opinion in Infectious Diseases: December 2013 - Volume 26 - Issue 6 - p 575–588
doi: 10.1097/QCO.0000000000000017
ANTIMICROBIAL AGENTS: Edited by Monica A. Slavin and Deenan Pillay

Purpose of review Treatment with combination antiretroviral therapy during pregnancy reduces the chance of mother to child transmission of HIV. Physiological changes during pregnancy can lead to lower exposure to antiretrovirals, possibly resulting in virological failure. For most antiretrovirals, data on exposure during pregnancy and transplacental passage are limited. This review summarizes the most recent information on pharmacokinetics (including transplacental passage), efficacy, as well as the safety of antiretrovirals during pregnancy.

Recent findings Intensive-sampling pharmacokinetic studies as well as observational studies using sparse sampling were performed to explore the exposure to antiretrovirals during pregnancy. Transplacental passage, efficacy (viral load at delivery and infection status of the newborn) and safety information were evaluated for several antiretrovirals.

Summary For most nucleoside/nucleotide reverse transcriptase inhibitors and protease inhibitors, recent research shows a decreased exposure during pregnancy. However, the advantage of a general dose increase during pregnancy still remains unclear. For newer compounds and efavirenz, limited or no data on pharmacokinetics during pregnancy or transplacentally are available, while the mechanisms of transplacental passage also remain unknown. For safety reasons, it will be important to monitor pregnancy outcomes in resource-limited settings during the implementation of the WHO guidelines (including the use of efavirenz during pregnancy).

aDepartment of Pharmacy

bNijmegen Institute for Infection, Inflammation and Immunity (N4i)

cDepartment of Pharmacology and Toxicology, Radboud university medical center, Nijmegen, The Netherlands

Correspondence to Angela Colbers, MSc, Radboud university medical center, Department of Pharmacy (internal post 864), Geert Grooteplein Zuid 10, 6525 GA Nijmegen, The Netherlands. Tel: +31 24 3616405; fax: +31 24 3668755; e-mail:

© 2013 Lippincott Williams & Wilkins, Inc.