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. 1990 Jun;34(6):1281–1284. doi: 10.1128/aac.34.6.1281

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

T J Walsh 1, C Lester-McCully 1, M G Rinaldi 1, J E Wallace 1, F M Balis 1, J W Lee 1, P A Pizzo 1, D G Poplack 1
PMCID: PMC171803  PMID: 2393291

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.

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Selected References

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