Flusum Mechanism of Action

Pharmacotherapeutic group: Antifungal agent. ATC code: D01AC15.
Pharmacology: Pharmacodynamics: Flusum contains fluconazole which is antifungal belonging to a new class of triazole agents, which is a potent and specific inhibitor of fungal sterol synthesis. Administered orally or intravenously, proved active in several modes of fungal infections.
Its activity has been demonstrated to fungal infections, such as those of Candida spp., (including systemic candidiasis in animals and immunocompromised), of Cryptococcus neoformans (including intracranial infections), of Microsporum spp. and of Trichophyton spp.
Fluconazole has also been shown to be active in animal models of endemic mycoses, including of Blastomyces dermatitidis and of Coccidioides immitis (including intracranial infections) and of Histoplasma capsulatum in normal and immunocompromised animals. Fluconazole used topically is a broad-spectrum antifungal agent. It was effective against the microorganisms responsible for dermatomycoses, cutaneous candidiasis and versicolor pityriasis (i.e. Microsporum spp., Trichophyton spp., Epidermophyton spp., Candida spp. and Malassezia furfur or Pityrosporum orbiculata.)
Its activities are performed against dermatophytes, yeasts and molds. Fluconazole is highly specific for fungal enzymes dependent on cytochrome P-450. It inhibits lanosterol C-14 demethylase enzyme that converts lanosterol in to the sterol present in the membrane of fungi i.e. the ergosterol.
Pharmacokinetics: A pharmacokinetic study conducted with the fluconazole Gel, showed that plasma levels achieved by fluconazole are so low as to exclude a systemic effect of the drug.
Moreover, the characteristics of a gel combined with the type of emulsion O/W allows excellent tolerability. There have been no pharmacokinetic studies conducted with the fluconazole Gel in children, but studies in adults have shown that the drug has a very low absorption systemically. Fluconazole has also been widely studied systemically in pediatric patients and neonates and showed a good tolerability profile similar to that of the adult patient.
A study conducted to evaluate the dermal tolerance and phototoxicity of the drug showed that the fluconazole Gel is well tolerated by human skin and is not phototoxic, so it is suitable for use as a topical antifungal.