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Itraconazole: pharmacokinetics and indications
1Facultad de Medicina, Universidad de Buenos Aires, Hospital de Enfermedades Infecciosas Francisco J. Muñiz, Argentina.
Archives of Medical Research
|January 1, 1993
Summary
Itraconazole, a broad-spectrum antifungal, demonstrates excellent oral absorption and achieves high tissue concentrations. It effectively treats various fungal infections by inhibiting ergosterol synthesis, with prolonged persistence in skin and nails.
Area of Science:
- Pharmacology
- Mycology
- Medicinal Chemistry
Background:
- Itraconazole is a lipophilic triazole antifungal agent.
- It exhibits poor solubility in some solvents but good digestive absorption.
Purpose of the Study:
- To detail the pharmacokinetic profile and mechanism of action of itraconazole.
- To review its efficacy in treating a wide range of fungal infections.
Main Methods:
- Pharmacokinetic analysis including absorption, distribution, metabolism, and excretion.
- Review of clinical efficacy data across various dermatomycoses and systemic mycoses.
Main Results:
- Excellent oral absorption with peak plasma levels at 3-4 hours.
- High protein binding (99.8%) and extensive tissue distribution (3-20 fold higher than plasma).
- Effective against most pathogenic fungi except Zygomycetes, with prolonged persistence in skin and nails.
Conclusions:
- Itraconazole is a well-absorbed, widely distributed antifungal with a favorable pharmacokinetic profile.
- Its mechanism involves ergosterol synthesis inhibition, making it effective for numerous fungal infections.