Penetration of SCH-39304, a new antifungal triazole, into cerebrospinal fluid of primates.

Abstract

We characterized the cerebrospinal fluid (CSF) penetration and pharmacokinetics of SCH-39304 in adult rhesus monkeys receiving a single oral dose of SCH-39304 (2.0 mg/kg of body weight). The mean CSF-to-plasma area under the curve ratio was 0.63 (+/- 0.18, standard error of the mean); maximum concentrations were 1.34 micrograms/ml (+/- 0.18) in CSF and 1.96 micrograms/ml (+/- 0.43) in plasma. The mean plasma half-life was 45.7 h (+/- 11), and mean CSF half-life was 38.7 h (+/- 3.5). The mean levels of SCH-39304 at 24 h were 1.48 micrograms/ml (+/- 0.3) in plasma and 0.96 microgram/ml (+/- 0.12) in CSF. We conclude that SCH-39304 effectively penetrates into CSF and achieves concentrations considered active against many opportunistic yeasts and that these concentrations are sustained in CSF for greater than or equal to 24 h.

• Authors: T J Walsh, C Lester-McCully, M G Rinaldi, J E Wallace, F M Balis, J W Lee, P A Pizzo, D G Poplack
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 34 Issue 6 Pg. 1281-4 (Jun 1990) ISSN: 0066-4804 [Print] United States
• PMID: 2393291 (Publication Type: Journal Article)

Chemical References

• Antifungal Agents
• Triazoles
• Sch 39304

Topics

• Animals
• Antifungal Agents (blood, cerebrospinal fluid, pharmacokinetics)
• Half-Life
• Macaca mulatta
• Male
• Triazoles (blood, cerebrospinal fluid, pharmacokinetics)