Fluconazole Penetration into Cerebrospinal Fluid: Implications for Treating Fungal Infections of the Central Nervous System

Fluconazole is a new triazole antifungal agent that has unique pharmacokinetic and pharmacological properties. The bioavailability after oral administration in humans is 80%. Fluconazole has been shown to be effective in treating cryptococcal meningitis in animal models and has been proposed as a th...

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Bibliographic Details
Published in:The Journal of infectious diseases 1988-01, Vol.157 (1), p.178-179
Main Authors: Arndt, Carola A. S., Walsh, Thomas J., McCully, Cynthia Lester, Balis, Frank M., Pizzo, Philip A., Poplack, David G.
Format: Article
Language:English
Subjects:
Animals
Antifungals
Applied sciences
Blood plasma
Central nervous system
Central Nervous System Diseases - drug therapy
Cerebrospinal fluid
Concise Clinical and Laboratory Communications
Cryptococcosis - drug therapy
Cryptococcus
Exact sciences and technology
Fluconazole
Health care administration
Humans
Infectious diseases
Internships
Macaca mulatta
Male
Medication administration
Other techniques and industries
Pharmacokinetics
Triazoles - cerebrospinal fluid
Triazoles - pharmacokinetics
Triazoles - therapeutic use
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Summary:Fluconazole is a new triazole antifungal agent that has unique pharmacokinetic and pharmacological properties. The bioavailability after oral administration in humans is 80%. Fluconazole has been shown to be effective in treating cryptococcal meningitis in animal models and has been proposed as a therapeutic alternative to long-term therapy with amphotericin B in patients with AIDS who have cryptococcal meningoencephalitis. For human and subhuman primates, no pharmacokinetic data exist, however, that examine simultaneous sequential CSF and plasma levels of fluconazole to document and characterize penetration of this drug into the CSF. The current study was performed to evaluate CSF penetration of fluconazole by using a subhuman primate model that reliably predicts CSF penetration and pharmacokinetics of drugs in humans and has been demonstrated to serve as a valid substitute for human experimentation.
ISSN:0022-1899
1537-6613
DOI:10.1093/infdis/157.1.178