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Accumulation of fluconazole in sebum
T Zimmermann1, H Laufen, R A Yeates
1Pfizer Research and Development, Illertissen, Germany.
International Journal of Clinical Pharmacology and Therapeutics
|September 21, 2001
Summary
This study shows that fluconazole accumulates significantly in sebum, with higher weekly doses leading to greater concentrations. These findings are important for treating fungal infections affecting the scalp and sebaceous glands.
Area of Science:
- Pharmacokinetics
- Dermatology
- Mycology
Background:
- Fluconazole is an antifungal medication.
- Sebum plays a role in the distribution of topical and systemic antifungals.
- Understanding drug accumulation in sebum is crucial for treating skin fungal infections.
Purpose of the Study:
- To determine fluconazole concentrations in human sebum and plasma.
- To compare fluconazole accumulation in sebum versus plasma.
- To evaluate the impact of different weekly dosages on fluconazole levels.
Main Methods:
- Two groups of 8 healthy subjects received either 150 mg or 300 mg of fluconazole weekly for 4 weeks.
- Plasma and sebum samples were collected before and after dosing, up to 2 weeks post-treatment.
- Fluconazole concentrations were measured using gas chromatography.
Main Results:
- Both dosages were well-tolerated.
- Fluconazole concentrations in sebum were significantly higher than in plasma.
- Higher weekly doses resulted in greater fluconazole accumulation in sebum, with median sebum/plasma ratios of 2.4 and 9.1.
Conclusions:
- Fluconazole demonstrates significant accumulation in sebum.
- The findings support the relevance of fluconazole for treating dermal mycoses, particularly those involving the sebaceous glands like tinea capitis.
- Weekly dosing regimens can achieve substantial drug levels in sebum.
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