Reduced indinavir exposure during pregnancy

Br J Clin Pharmacol. 2013 Sep;76(3):475-83. doi: 10.1111/bcp.12078.

Abstract

Aim: To describe the pharmacokinetics and safety of indinavir boosted with ritonavir (IDV/r) during the second and third trimesters of pregnancy and in the post-partum period.

Methods: IMPAACT P1026s is an on-going, prospective, non-blinded study of antiretroviral pharmacokinetics (PK) in HIV-infected pregnant women with a Thai cohort receiving IDV/r 400/100 mg twice daily during pregnancy through to 6-12 weeks post-partum as part of clinical care. Steady-state PK profiles were performed during the second (optional) and third trimesters and at 6-12 weeks post-partum. PK targets were the estimated 10(th) percentile IDV AUC (12.9 μg ml(-1)h) in non-pregnant historical Thai adults and a trough concentration of 0.1 μg ml(-1), the suggested minimum target.

Results: Twenty-six pregnant women were enrolled; thirteen entered during the second trimester. Median (range) age was 29.8 (18.9-40.8) years and weight 60.5 (50.0-85.0) kg at the third trimester PK visit. The 90% confidence limits for the geometric mean ratio of the indinavir AUC(0,12 h) and Cmax during the second trimester and post-partum (ante : post ratios) were 0.58 (0.49, 0.68) and 0.73 (0.59, 0.91), respectively; third trimester/post-partum AUC(0,12 h) and Cmax ratios were 0.60 (0.53, 0.68) and 0.63 (0.55, 0.72), respectively. IDV/r was well tolerated and 21/26 women had a HIV-1 viral load < 40 copies ml(-1) at delivery. All 26 infants were confirmed HIV negative.

Conclusion: Indinavir exposure during the second and third trimesters was significantly reduced compared with post-partum and ∼30% of women failed to achieve a target trough concentration. Increasing the dose of IDV/r during pregnancy to 600/100 mg twice daily may be preferable to ensure adequate drug concentrations.

Keywords: HIV; antiretrovirals; pregnancy; prevention of mother-to-child transmission.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Adolescent
  • Adult
  • Antiretroviral Therapy, Highly Active
  • Dose-Response Relationship, Drug
  • Female
  • HIV Infections / drug therapy
  • HIV Infections / metabolism*
  • HIV Infections / transmission
  • HIV Protease Inhibitors / administration & dosage
  • HIV Protease Inhibitors / blood
  • HIV Protease Inhibitors / pharmacokinetics*
  • HIV Protease Inhibitors / therapeutic use
  • Humans
  • Indinavir / administration & dosage
  • Indinavir / blood
  • Indinavir / pharmacokinetics*
  • Indinavir / therapeutic use
  • Infant
  • Infant, Newborn
  • Infectious Disease Transmission, Vertical / prevention & control
  • Postpartum Period
  • Pregnancy
  • Pregnancy Complications, Infectious / drug therapy
  • Pregnancy Complications, Infectious / metabolism*
  • Pregnancy Complications, Infectious / virology
  • Pregnancy Trimester, Second
  • Pregnancy Trimester, Third
  • Prospective Studies
  • Ritonavir / administration & dosage
  • Ritonavir / blood
  • Ritonavir / pharmacokinetics*
  • Ritonavir / therapeutic use
  • Young Adult

Substances

  • HIV Protease Inhibitors
  • Indinavir
  • Ritonavir