Contraceptive efficacy of oral and transdermal hormones when co-administered with protease inhibitors in HIV-1-infected women: Pharmacokinetic results of ACTG trial A5188

Mary A. Vogler, Kristine Patterson, Lori Kamemoto, Jeong Gun Park, Heather Watts, Francesca Aweeka, Karin L. Klingman, Susan E. Cohn

Research output: Contribution to journalArticlepeer-review

37 Scopus citations

Abstract

Background: Pharmacokinetic (PK) interactions between lopinavir/ritonavir (LPV/r) and transdermally delivered ethinyl estradiol (EE) and norelgestromin (NGMN) are unknown. Methods: Using a standard noncompartmental PK analysis, we compared EE area under the time-concentration curve (AUC) and NGMN AUC during transdermal contraceptive patch administration in HIV-1-infected women on stable LPV/r to a control group of women not on highly active antiretroviral therapy (HAART). In addition, EE AUC after a single dose of a combination oral contraceptive pill including EE and norethindrone was measured before patch placement and was compared with patch EE AUC in both groups. Contraceptive effects on LPV/r PKs were estimated by measuring LPV/r AUC at baseline and during week 3 of patch administration. Results: Eight women on LPV/r, and 24 women in the control group were enrolled. Patch EE median AUC0-168 h was 45% lower at 6010.36 pg•h•mL in those on LPV/r versus 10911.42 pg•h•mL in those on no HAART (P = 0.064). Pill EE median AUC0-48 hours was similarly 55% lower at 344.67 pg•h•mL in those on LPV/r versus 765.38 pg•h•mL in those on no HAART (P = 0.003). Patch NGMN AUC0-168 h however, was 138.39 ng•h•mL, 83% higher in the LPV/r group compared with the control AUC of 75.63 ng•h•mL (P = 0.036). After 3 weeks on the patch, LPV AUC0-8 h decreased by 19%, (P = 0.156). Conclusions: Although PKs of contraceptive EE and NGMN are significantly altered with LPV/r, the contraceptive efficacy of the patch is likely to be maintained. Larger studies are indicated to fully assess contraceptive efficacy versus risks of the transdermal contraceptive patch when co-administered with protease inhibitors.

Original languageEnglish (US)
Pages (from-to)473-482
Number of pages10
JournalJournal of Acquired Immune Deficiency Syndromes
Volume55
Issue number4
DOIs
StatePublished - Dec 1 2010

Keywords

  • HIV
  • hormonal contraceptive
  • lopinavir/ritonavir
  • pharmacokinetics

ASJC Scopus subject areas

  • Infectious Diseases
  • Pharmacology (medical)

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