Medoflucon Mechanism of Action





Full Prescribing Info
Pharmacology: Pharmacodynamics: Fluconazole is a selective inhibitor of fungal enzymes needed for the synthesis of ergosterol.
It is an orally active bistriazole antifungal agent. Mode of action, in sensitive fungi, is by inhibition of fungal cytochrome P-450 dependent enzymes, which results in impairment of ergosterol synthesis in the fungal cell membrane, resulting in disruption of membrane associated functions. It is active against Blastomyces dermatitidis, Candida sp., Coccidioides immitis, Cryptococcus neoformans, Histoplasma capsulatum, Microsporum sp., and Trichophyton sp. Resistance has developed in some Candida sp.
Pharmacokinetics: Fluconazole is well absorbed following oral administration. The bioavailability orally is 90% or more of that from intravenous administration. Mean peak plasma levels of 6.27µg/ml have been reported in healthy volunteers following a 400mg oral dose. Peak plasma concentrations are reached in one to two hours following oral administration, and the plasma levels are proportional to the dose over the range 50mg to 400mg. Multiple dosing leads to an increase in peak plasma levels, steady state concentrations are achieved in six to ten days. Use of a loading dose means that steady state plasma concentrations can be achieved in two days. Fluconazole is widely distributed, with the apparent volume of distribution being close to that of total body water. The concentrations of fluconazole reached in joint fluid, breast milk, saliva, sputum, peritoneal fluid and vaginal fluids are similar to those in plasma. Cerebro-spinal fluid concentrations range from 50% to 90% of the plasma concentration, even in the absence of inflammation of the meninges.
Protein binding is about 12%.
Fluconazole is eliminated mainly in the urine, with 80% or more being excreted unchanged. About 11% is excreted as metabolites. The elimination half life is about thirty hours, and this is increased with impaired renal function. Fluconazole is removed by dialysis.
Fluconazole renal clearance for the elderly is generally lower than for the younger people.
Toxicology: Preclinical Safety Data: No further relevant information.
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