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

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.

• Authors: Aylin Yilmaz, Victoria Watson, Laura Dickinson, David Back
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 56 Issue 9 Pg. 4583-5 (Sep 2012) ISSN: 1098-6596 [Electronic] United States
• PMID: 22687515 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

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

Topics

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