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Fluconazole penetration into cerebrospinal fluid in humans
G Foulds1, D R Brennan, C Wajszczuk
1Central Research Division, Pfizer Inc., Groton, Connecticut 06340.
Journal of Clinical Pharmacology
|April 1, 1988
Summary
Fluconazole effectively penetrates the cerebrospinal fluid in healthy individuals and patients with meningitis. Intravenous fluconazole achieves significant concentrations in cerebrospinal fluid, indicating potential for treating central nervous system fungal infections.
Area of Science:
- Pharmacology
- Infectious Diseases
- Neuroscience
Background:
- Fluconazole is a widely used antifungal medication.
- Understanding its penetration into the central nervous system is crucial for treating fungal meningitis.
Purpose of the Study:
- To quantify fluconazole concentrations in cerebrospinal fluid (CSF) after intravenous administration.
- To assess the ratio of CSF to serum fluconazole concentrations.
Main Methods:
- Healthy subjects received intravenous fluconazole (50 mg/d for 6 days or 100 mg/d for 7 days).
- Cerebrospinal fluid and serum fluconazole levels were measured one hour after the final dose.
- CSF concentrations were also assessed in four patients diagnosed with meningitis.
Main Results:
- CSF fluconazole concentrations were 1.26 mg/L and 2.74 mg/L for the 50 mg/d and 100 mg/d doses, respectively.
- CSF concentrations represented 52% and 62% of serum concentrations.
- Significant CSF fluconazole levels were observed in patients with meningitis.
Conclusions:
- Intravenous fluconazole achieves substantial concentrations in the cerebrospinal fluid.
- These findings support the use of fluconazole for treating fungal infections of the central nervous system, including meningitis.