Pharmacokinetics of fluconazole in cerebrospinal fluid and serum in human coccidioidal meningitis
Open Access
- 1 March 1988
- journal article
- research article
- Published by American Society for Microbiology in Antimicrobial Agents and Chemotherapy
- Vol. 32 (3), 369-373
- https://doi.org/10.1128/aac.32.3.369
Abstract
The pharmacokinetics of fluconazole, a new oral azole, were evaluated in cerebrospinal fluid and sera of eight patients with coccidioidal meningitis. At a dose of 50 mg/day, peak concentrations of 2.5 to 3.5 and 2.0 to 2.3 micrograms/ml occurred at 2 to 6 and 4 to 8 h in serum and cerebrospinal fluid, respectively. At 100 mg/day, peak concentrations of 4.5 to 8.0 and 3.4 to 6.2 micrograms/ml occurred at 2 to 4 and 4 to 12 h, respectively. The mean ratios of the concentration in cerebrospinal fluid to that in serum were 73.8% at 50 mg/day and 88.7% at 100 mg/day. Results suggested that there was a prolonged half-life in both cerebrospinal fluid and serum and that it was slightly longer in the former. Minimal toxicity was noted in 34 patient months of therapy (12 months on 50 mg daily; 22 months on 100 mg daily). After a mean of 4.5 months of therapy, five patients responded to therapy and three were unevaluable. The penetration of fluconazole into cerebrospinal fluid was substantial, toxicity was minimal, and early clinical experience was encouraging. Fluconazole holds promise as the sole or adjunctive therapy for fungal meningitis.This publication has 13 references indexed in Scilit:
- Treatment of cryptococcal meningitis in mice with fluconazoleJournal of Antimicrobial Chemotherapy, 1986
- Comparison of itraconazole and fluconazole in treatment of cryptococcal meningitis and candida pyelonephritis in rabbitsAntimicrobial Agents and Chemotherapy, 1986
- Pharmacokinetic evaluation of UK-49,858, a metabolically stable triazole antifungal drug, in animals and humansAntimicrobial Agents and Chemotherapy, 1985
- Miconazole in the Treatment of CoccidioidomycosisDrugs, 1983
- High-Dose Ketoconazole for Treatment of Fungal Infections of the Central Nervous SystemAnnals of Internal Medicine, 1983
- Ketoconazole inhibition of testicular secretion of testosterone and displacement of steroid hormones from serum transport proteinsAntimicrobial Agents and Chemotherapy, 1983
- Hepatic reactions during ketoconazole treatmentAmerican Journal Of Medicine, 1983
- Ketoconazole Blocks Adrenal Steroid SynthesisAnnals of Internal Medicine, 1982
- Disposition of ketoconazole, an oral antifungal, in humansAntimicrobial Agents and Chemotherapy, 1982
- Obfuscation of the Activity of Antifungal Antimicrobics by Culture MediaThe Journal of Infectious Diseases, 1972