| Each capsule contains 150 mg fluconazole, №1

PHARMACOLOGIC PROPERTIES

АТC code: J02AC01, Antimycotics for systemic use, triazole derivatives

Fluconazole is a triazole antifungal agent. Its primary mode of action is the inhibition of fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylation, an essential step in fungal ergosterol biosynthesis. The accumulation of 14 alpha-methyl sterols correlates with the subsequent loss of ergosterol in the fungal cell membrane and may be responsible for the antifungal activity of fluconazole. Fluconazole has been shown to be more selective for fungal cytochrome P-450 enzymes than for various mammalian cytochrome P-450 enzyme systems.

Fluconazole achieves good penetration in all body fluids studied. The levels of fluconazole in saliva and sputum are similar to plasma levels. In patients with fungal meningitis, fluconazole levels in the CSF are approximately 80% the corresponding plasma levels.

High skin concentration of fluconazole, above serum concentrations, is achieved in the stratum corneum, epidermis-dermis and eccrine sweat. Fluconazole accumulates in the stratum corneum. At a dose of 50 mg once daily, the concentration of fluconazole after 12 days was 73 μg/g and 7 days after cessation of treatment the concentration was still 5.8 μg/g. At the 150 mg once-a-week dose, the concentration of fluconazole in stratum corneum on day 7 was 23.4 μg/g and 7 days after the second dose was still 7.1 μg/g.

Concentration of fluconazole in nails after 4 months of 150 mg once-a-week dosing was 4.05 μg/g in healthy and 1.8 μg/g in diseased nails; and, fluconazole was still measurable in nail samples 6 months after the end of therapy.

THERAPEUTIC INDICATIONS

FLUKAM is indicated in adults for the treatment of:

1. Cryptococcal meningitis;
2. Coccidioidomycosis;
3. Invasive candidiasis;
4. Mucosal candidiasis including or opharyngeal, oesophageal candidiasis, candiduria and chronic mucocutaneous candidiasis;
5. Chronic oral atrophic candidiasis (denture sore mouth) if dental hygiene or topical treatment are insufficient;
6. Vaginal candidiasis, acute or recurrent; when local therapy is not appropriate;
7. Candidal balanitis when local therapy is not appropriate;
8. Dermatomycosis including tinea pedis, tinea corporis, tinea cruris, tinea versicolor and dermal candida infections when systemic therapy is indicated.
9. Tinea unguinium (onychomycosis) when other agents are not considered appropriate.