Clinical Pharmacokinetics

, Volume 51, Issue 10, pp 639–659 | Cite as

Pharmacokinetic Optimization of Antiretroviral Therapy in Pregnancy

  • Kajal Buckoreelall
  • Tim R. Cressey
  • Jennifer R. KingEmail author
Review Article


Antiretroviral therapy suppresses replication of HIV allowing restoration and/or preservation of the immune system. Providing combination antiretroviral therapy during pregnancy can treat maternal HIV infection and/or reduce perinatal HIV transmission. However, providing treatment to pregnant women is challenging due to physiological changes that can alter antiretroviral pharmacokinetics. Suboptimal drug exposure can result in HIV RNA rebound, the selection of resistant virus or an increased risk of HIV-1 transmission to the infant. Increased drug exposure can produce unwarranted maternal adverse effects and/or fetal toxicity. Subsequently, dose adjustments may be necessary during pregnancy to achieve comparable antiretroviral exposure to non-pregnant adults. For several antiretrovirals, systemic exposure is decreased during the last trimester of pregnancy. By 6–12 weeks postpartum, concentrations return to those prior to pregnancy. Also, the extent of antiretroviral placental transfer to the fetus and degree of antiretroviral excretion into breast milk varies within, and between, antiretroviral drug classes. It is necessary to consider the pharmacological characteristics of each antiretroviral when optimizing combination therapy during pregnancy to treat maternal HIV infection and prevent perinatal HIV transmission.


Efavirenz Nevirapine Saquinavir Nelfinavir Atazanavir 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



Jennifer R. King has received salary support from grants IK23AI0074390-01 and U01-AI41089 from the National Institute of Allergy and Infectious Diseases. No sources of funding were used to assist in the preparation of this review. The authors have no conflicts of interest that are directly relevant to the content of this review.


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Copyright information

© Springer International Publishing Switzerland 2012

Authors and Affiliations

  • Kajal Buckoreelall
    • 1
  • Tim R. Cressey
    • 2
    • 3
    • 4
  • Jennifer R. King
    • 1
    Email author
  1. 1.Division of Clinical Pharmacology, Department of Pharmacology and ToxicologyUniversity of Alabama at Birmingham School of MedicineBirminghamUSA
  2. 2.Program for HIV Prevention and Treatment, Department of Medical Technology, Faculty of Associated Medical SciencesChiang Mai UniversityChiang MaiThailand
  3. 3.Department of Immunology and Infectious DiseasesHarvard School of Public HealthBostonUSA
  4. 4.Institut de Recherche pour le Développement (IRD), UMI 174MarseilleFrance

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