Assessment of Nevirapine Prophylactic and Therapeutic Dosing Regimens for Neonates

J Acquir Immune Defic Syndr. 2017 Aug 15;75(5):554-560. doi: 10.1097/QAI.0000000000001447.

Abstract

Background: Nevirapine (NVP) is a key component of antiretroviral prophylaxis and treatment for neonates. We evaluated current World Health Organization (WHO) weight-band NVP prophylactic dosing recommendations and investigated optimal therapeutic NVP dosing for neonates.

Methods: The PHPT-5 study in Thailand assessed the efficacy of "Perinatal Antiretroviral Intensification" to prevent mother-to-child transmission of HIV in women with <8 weeks of antiretroviral treatment before delivery (NCT01511237). Infants received a 2-week course of zidovudine/lamivudine/NVP (NVP syrup/once daily: 2 mg/kg for 7 days; then 4 mg/kg for 7 days). Infant samples were assessed during the first 2 weeks of life. NVP population pharmacokinetics (PK) parameters were estimated using nonlinear mixed-effects models. Simulations were performed to estimate the probability of achieving target NVP trough concentrations for prophylaxis (>0.10 mg/L) and for therapeutic efficacy (>3.0 mg/L) using different infant dosing strategies.

Results: Sixty infants (55% male) were included. At birth, median (range) weight was 2.9 (2.3-3.6) kg. NVP concentrations were best described by a 1-compartment PK model. Infant weight and postnatal age influenced NVP PK parameters. Based on simulations for a 3-kg infant, ≥92% would have an NVP trough >0.1 mg/L after 48 hours through 2 weeks using the PHPT-5 and WHO-dosing regimens. For NVP-based therapy, a 6-mg/kg twice daily dose produced a trough >3.0 mg/L in 87% of infants at 48 hours and 80% at 2 weeks.

Conclusion: WHO weight-band prophylactic guidelines achieved target concentrations. Starting NVP 6 mg/kg twice daily from birth is expected to achieve therapeutic concentrations during the first 2 weeks of life.

Publication types

  • Clinical Trial, Phase III
  • Multicenter Study
  • Research Support, N.I.H., Extramural

MeSH terms

  • Anti-HIV Agents / administration & dosage*
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / therapeutic use
  • Breast Feeding
  • Chemoprevention / methods*
  • Clinical Protocols
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Female
  • HIV Infections / drug therapy*
  • HIV Infections / prevention & control*
  • HIV Infections / transmission
  • Humans
  • Infant, Newborn
  • Infectious Disease Transmission, Vertical / prevention & control*
  • Lamivudine / administration & dosage
  • Lamivudine / pharmacokinetics
  • Lamivudine / therapeutic use
  • Male
  • Nevirapine / administration & dosage
  • Nevirapine / pharmacokinetics*
  • Nevirapine / therapeutic use
  • Practice Guidelines as Topic
  • Pregnancy
  • Pregnancy Complications, Infectious* / virology
  • Thailand
  • World Health Organization
  • Zidovudine / administration & dosage
  • Zidovudine / pharmacokinetics
  • Zidovudine / therapeutic use

Substances

  • Anti-HIV Agents
  • Lamivudine
  • Zidovudine
  • Nevirapine