Affiliation:
1. Section of Infectious Diseases, National Cancer Institute, Bethesda, Maryland 20892.
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.
Publisher
American Society for Microbiology
Subject
Infectious Diseases,Pharmacology (medical),Pharmacology
Reference26 articles.
1. Treatment of infections in patients with the acquired immunodeficiency syndrome;Armstrong D.;Ann. Intern. Med.,1985
2. Fluconazole penetration into cerebrospinal fluid: implications for treating fungal infections of the central nervous system;Arndt C. A. S.;J. Infect. Dis.,1988
3. A comparison of amphotericin B alone and combined with flucytosine in the treatment of cryptococcal meningitis;Bennett J. E.;N. Engl. J. Med.,1979
4. Brammer K. W. and M. H. Tarbit. 1987. A review of the pharmacokinetics of fluconazole (VK-49 858) in laboratory animals and man p. 141-149. In R. A. Fromtling (ed.) Recent trends in the discovery development and evaluation of antifungal agents. J. R. Prous Science Publishers Barcelona Spain.
5. Clinical pharmacokinetics of systemic antifungal drugs;Daneshmend T. K.;Clin. Pharmacokinet.,1983
Cited by
11 articles.
订阅此论文施引文献
订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献