Comparison of nevirapine plasma concentrations between lead-in and steady-state periods in Chinese HIV-infected patients

PLoS One. 2013;8(1):e52950. doi: 10.1371/journal.pone.0052950. Epub 2013 Jan 24.

Abstract

Objectives: To investigate the potential of nevirapine 200 mg once-daily regimen and evaluate the influence of patient characteristics on nevirapine concentrations.

Methods: This was a prospective, multicentre cohort study with 532 HIV-infected patients receiving nevirapine as a part of their initial antiretroviral therapy. Plasma samples were collected at trough or peak time at the end of week 2 (lead-in period) and week 4, 12, 24, 36, and 48 (steady-state period), and nevirapine concentrations were determined using a validated HPLC method. Potential influencing factors associated with nevirapine concentrations were evaluated using univariate and multivariate logistic regression.

Results: A total of 2348 nevirapine plasma concentrations were collected, including 1510 trough and 838 peak values. The median nevirapine trough and peak concentration during the lead-in period were 4.26 µg/mL (IQR 3.05-5.61) and 5.07 µg/mL (IQR 3.92-6.44) respectively, which both exceeded the recommended thresholds of nevirapine plasma concentrations. Baseline hepatic function had a moderate effect on median nevirapine trough concentrations at week 2 (4.25 µg/mL v.s. 4.86 µg/mL, for ALT <1.5 × ULN and ≥ 1.5 × ULN, respectively, P = 0.045). No significant difference was observed in median nevirapine trough concentration between lead-in and steady-state periods in patients with baseline ALT and AST level ≥ 1.5 × ULN (P = 0.171, P = 0.769), which was different from the patients with ALT/AST level <1.5ULN. The median trough concentrations were significantly higher in HIV/HCV co-infected patients than those without HCV at week 48 (8.16 µg/mL v.s. 6.15 µg/mL, P = 0.004).

Conclusions: The 200 mg once-daily regimen of nevirapine might be comparable to twice-daily in plasma pharmacokinetics in Chinese population. Hepatic function prior to nevirapine treatment and HIV/HCV coinfection were significantly associated with nevirapine concentrations.

Trial registration: ClinicalTrials.gov NCT00872417.

Publication types

  • Comparative Study
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Aged
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / blood*
  • China
  • Female
  • HIV Infections / blood
  • HIV Infections / drug therapy*
  • Humans
  • Male
  • Middle Aged
  • Nevirapine / administration & dosage
  • Nevirapine / blood*
  • Reverse Transcriptase Inhibitors / administration & dosage
  • Reverse Transcriptase Inhibitors / blood*
  • Young Adult

Substances

  • Anti-HIV Agents
  • Reverse Transcriptase Inhibitors
  • Nevirapine

Associated data

  • ClinicalTrials.gov/NCT00872417

Grants and funding

This work was supported by the National Natural Science Foundation of China (81071372); the National Key Technologies R&D Program for the 11th Five-year Plan (2008ZX10001-006); and Key Clinical Program of the Ministry of Health 2010–2012. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.