Effects of hormonal contraception on antiretroviral drug metabolism, pharmacokinetics and pharmacodynamics

Am J Reprod Immunol. 2014 Jun;71(6):523-30. doi: 10.1111/aji.12210. Epub 2014 Feb 13.


Among women, human immunodeficiency virus type 1 (HIV-1) infection is most prevalent in those of reproductive age. These women are also at risk of unintended or mistimed pregnancies. Hormonal contraceptives (HCs) are one of the most commonly used methods of family planning worldwide. Therefore, concurrent use of HC among women on antiretroviral medications (ARVs) is increasingly common. ARVs are being investigated and have been approved for pre-exposure prophylaxis (PrEP), and therefore, drug-drug interactions must also be considered in HIV-1-negative women who want to prevent both unintended pregnancy and HIV-1 infection. This article will review four main interactions: (i) the effect of HCs on ARV pharmacokinetics (PK) and pharmacodynamics (PD) during therapy, (ii) the effect of ARVs on HC PK and PD, (iii) the role of drug transporters on drug-drug interactions, and (iv) ongoing research into the effect of HCs on pre-exposure prophylaxis PK and PD.

Keywords: Antiretrovirals; Drug-drug interactions; HIV mucosal acquisition; hormonal contraceptives.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Adenine / analogs & derivatives
  • Adenine / pharmacology
  • Anti-HIV Agents / metabolism
  • Anti-HIV Agents / pharmacokinetics*
  • Contraception / methods*
  • Contraceptives, Oral, Hormonal / metabolism
  • Contraceptives, Oral, Hormonal / pharmacokinetics*
  • Cytochrome P-450 CYP3A / metabolism
  • Cytochrome P-450 CYP3A Inhibitors / pharmacology
  • Deoxycytidine / analogs & derivatives
  • Deoxycytidine / pharmacology
  • Drug Interactions*
  • Emtricitabine
  • Family Planning Services
  • Female
  • HIV Infections / drug therapy*
  • HIV Infections / prevention & control
  • HIV-1 / drug effects
  • HIV-1 / pathogenicity
  • Humans
  • Organophosphonates / pharmacology
  • Pregnancy
  • Progestins / pharmacology
  • Tenofovir
  • Treatment Outcome


  • Anti-HIV Agents
  • Contraceptives, Oral, Hormonal
  • Cytochrome P-450 CYP3A Inhibitors
  • Organophosphonates
  • Progestins
  • Deoxycytidine
  • Tenofovir
  • Cytochrome P-450 CYP3A
  • Emtricitabine
  • Adenine