Acute vaginal candidiasis when local therapy is not appropriate. Candida balanitis when local therapy is not appropriate.
active substance: fluconazole;
1 capsule contains 150 mg of fluconazole;
excipients: lactose monohydrate; corn starch; colloidal anhydrous silica; magnesium stearate; sodium lauryl sulfate.
Flucorik Dosage form
Main physical and chemical properties: blue / blue hard gelatin double-leaf capsules size 1 with the inscription “RANBAXY” black food ink on the lid and body of the capsule, the capsules contain white or almost white powder.
Flucorik Pharmacotherapeutic group
Antifungal agents for systemic use. Triazole derivatives. ATX code J02A C01.
Mechanism of action.
Fluconazole, an antifungal agent of the triazole class, is a potent and selective inhibitor of fungal enzymes required for ergosterol synthesis. Its primary mechanism of action is the inhibition of fungal 14 alpha-lanosterol demethylation mediated by cytochrome P450, which is an integral step in the biosynthesis of fungal ergosterol. Accumulation of 14 alpha-methyl-sterols correlates with subsequent loss of ergosterol by the fungal cell membrane and may be responsible for the antifungal activity of fluconazole. Fluconazole is more selective for fungal cytochrome P450 enzymes than for various mammalian cytochrome P450 enzyme systems.
The use of fluconazole at a dose of 50 mg per day for 28 days does not affect the level of testosterone in plasma in men or the level of endogenous steroids in women of reproductive age. Fluconazole at a dose of 200 – 400 mg per day has no clinically significant effect on the level of endogenous steroids or on the response to ACTH stimulation in healthy male volunteers.
Antipyrine interaction studies have shown that administration of 50 mg of fluconazole once or repeatedly does not affect antipyrine metabolism.
In vitro sensitivity.
Fluconazole in vitro shows antifungal activity against the most common Candida species (including C. albicans, C. parapsilosis, C. tropicalis). C.glabrata shows a wide range of sensitivity to fluconazole, while C.krusei is resistant to it.
Fluconazole also shows activity in vitro against Cryptococcus neoformans and Cryptococcus gattii, as well as against endemic fungi Blastomices dermatitidis, Coccidioides immitis, Histoplasma capsulatum and Paracoccidioides brasiliensis.
Mechanism of resistance.
Microorganisms of the genus Candida demonstrate numerous mechanisms of resistance to azole antifungal agents. Fluconazole shows a high minimum inhibitory concentration against fungal strains that have one or more mechanisms of resistance, which adversely affects efficacy in vivo and in clinical practice. Cases of superinfection of Candida spp., Other than C. albicans, with species that are often insensitive to fluconazole (eg Candida krusei) have been reported. Alternative antifungal agents should be used to treat such cases.
Acute vaginal candidiasis when topical therapy is not appropriate.
Candidal balanitis, when local therapy is not appropriate.
Hypersensitivity to fluconazole, other azole compounds or to any of the excipients.
Concomitant use of fluconazole and terfenadine in patients receiving fluconazole repeatedly at doses of 400 mg / day and above (according to the results of a study of the interaction of repeated use).
Concomitant use of fluconazole and other drugs that prolong the QT interval and are metabolized by the enzyme CYP2A4 (eg cisapride, astemizole, pimozide, quinidine and erythromycin).