Pharmacology: Pharmacodynamics: Fluconazole, a member of a new class of triazole antifungal agents, is a potent and specific inhibitor of fungal sterol synthesis.
Pharmacokinetics: Absorption: The pharmacokinetics of fluconazole are similar following IV or oral administration. The drug is rapidly and almost completely absorbed from the GI tract, and there is no evidence of first-pass metabolism. Oral bioavailability of fluconazole exceeds 90%, in healthy, fasting adults; peak plasma concentrations of the drug generally are attained within 1-2 hours after oral administration.
Distribution: Fluconazole is widely distributed into body tissues and fluids following oral or IV administration. Fluconazole, unlike some azole-derivative antifungal agents (e.g., itraconazole, ketoconazole), distributes readily into CSF following oral or IV administration; CSF concentrations of fluconazole may be 50-94% of concurrent plasma concentrations regardless of the degree of meningeal inflammation.
Elimination: The plasma elimination half-life of fluconazole in adults with normal renal function is approximately 30 hours. In patients with impaired renal function, plasma concentrations of fluconazole are higher and the half-life prolonged; elimination half-life of the drug is inversely proportional to the patient's creatinine clearance. Fluconazole is removed by hemodialysis and peritoneal dialysis.