Efavirenz pharmacokinetics in cerebrospinal fluid and plasma over a 24-hour dosing interval

Antimicrob Agents Chemother. 2012 Sep;56(9):4583-5. doi: 10.1128/AAC.06311-11. Epub 2012 Jun 11.

Abstract

We determined the pharmacokinetics of efavirenz in plasma and cerebrospinal fluid (CSF) over a 24-h dosing interval in a patient who had undergone a lumbar drain because of cryptococcal meningitis. Drug concentrations were determined by high-performance liquid chromatography-tandem mass spectrometry in paired CSF (n = 24) and plasma (n = 25) samples. The median plasma efavirenz concentration was 3,718 ng/ml (range, 2,439 to 4,952), and the median CSF concentration was 16.3 ng/ml (range, 7.3 to 22.3). The CSF/plasma area-under-the-curve ratio was 0.0044 corresponding to a CSF penetration of 0.44% of plasma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes
  • Anti-HIV Agents / blood
  • Anti-HIV Agents / cerebrospinal fluid
  • Anti-HIV Agents / pharmacokinetics*
  • Antifungal Agents / pharmacology
  • Area Under Curve
  • Benzoxazines / blood
  • Benzoxazines / cerebrospinal fluid
  • Benzoxazines / pharmacokinetics*
  • Chromatography, High Pressure Liquid
  • Coinfection
  • Cryptococcus neoformans / drug effects
  • Cryptococcus neoformans / growth & development
  • Cyclopropanes
  • HIV / drug effects
  • HIV / growth & development
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • Half-Life
  • Humans
  • Male
  • Meningitis, Cryptococcal / drug therapy*
  • Meningitis, Cryptococcal / microbiology
  • Middle Aged
  • Tandem Mass Spectrometry

Substances

  • Alkynes
  • Anti-HIV Agents
  • Antifungal Agents
  • Benzoxazines
  • Cyclopropanes
  • efavirenz