Composition of 1 capsule. fluconazole 50 mg excipients: lactose - 49.708 mg, corn starch - 16.5 mg, silicon colloidal dioxide - 0.117 mg, magnesium stearate - 1.058 mg, sodium lauryl - 0.117 mg. Pharmacological action Antifungal drug. Fluconazole is representative of a class of triazole antifungal agents, is a powerful inhibitor selective synthesis sterols in the cell mushrooms. At intake and at/in the introduction fluconazole was active on various models of fungal infections in animals. The demonstrated activity of the drug for opportunistic mycoses, including caused by Candida spp. including generalized candidiasis in animals with reduced immunity; Cryptococcus neoformans, including intracranial infections; Microsporum spp. and Trychoptyton spp. Established the activity of fluconazole on models of endemic mycoses in animals, including infections caused by Blastomyces dermatitidis, Coccidioides immitis, including intracranial infections, and Histoplasma capsulatum in animals with normal and immunocompromised. Fluconazole has high specificity for fungal enzymes dependent on cytochrome P450. Therapy with fluconazole at 50 mg/ for up to 28 days did not affect the concentrations of testosterone in plasma in males or steroid concentrations in women of childbearing age. Fluconazole at a dose of 200-400 mg/ had no clinically significant effect on levels of endogenous steroids and their response to ACTH stimulation in healthy male volunteers. Single or multiple receiving fluconazole at a dose of 50 mg does not affect the metabolism of antipyrine in their simultaneous reception. There were reports of cases of superinfection, caused by other than Candida albicans, strains of Candida, which often do not show sensitivity to fluconazole (e.g. Candida krusei). In such cases may require alternative antifungal therapy. Pharmacokinetics the Pharmacokinetics of fluconazole are similar in in/in the introduction and ingestion. Absorption After oral fluconazole is well absorbed, its levels in plasma (total and bioavailable) exceeds 90% of the levels of fluconazole in plasma at/in the introduction. Simultaneous eating does not affect the absorption when taken orally. Cmax achieved through 0.5-1.5 h after administration of fluconazole on an empty stomach. Concentration in blood plasma is proportional to dose. The distribution of 90% equilibrium concentration is reached by the 4-5-th day after the start of therapy (repeated 1 times). Introduction of shock dose (in 1 day), 2 times the average daily dose, allows to achieve a Css of 90% to the 2nd day. Apparent Vd is approaching to the total water content in the body. Linking blood plasma proteins is low (11-12%). Fluconazole penetrates well into all body fluids. The levels of fluconazole in saliva and sputum are similar to the concentration in the blood plasma. In patients with fungal meningitis fluconazole levels in the cerebrospinal fluid are about 80% of its levels in plasma. In the stratum corneum, epidermis-dermis and sweat are reached high concentrations, that exceed the whey. Fluconazole accumulates in the stratum corneum. When taken in the dose of 50 mg 1 time/ concentration of fluconazole after 12 days was 73 µg/g and 7 days after cessation of treatment only 5.8 ág/g When applied at a dose of 150 mg 1 times/week. the concentration of fluconazole in stratum corneum on the 7th day was 23.4 µg/g and 7 days after administration of the second dose – 7.1 µg/g. the Concentration of fluconazole in nails after 4 months of use at a dose of 150 mg 1 times/week amounted to 4.05 µg/g in healthy and 1.8 µg/g in diseased nails; 6 months after completion of therapy flukonazol still determined in nails. Metabolism and excretion of fluconazole is excreted mainly by the kidneys; about 80% imposed dose found in the urine in unchanged form. Fluconazole clearance is proportional to KK. Circulating metabolites were not detected. Long T1/2 from blood plasma allows to take fluconazole once in vaginal candidiasis and 1 time or 1 time/week. at other indications. Were compared to the concentrations in saliva and plasma after a single dose of fluconazole at a dose of 100 mg of a suspension for oral (rinse and save the mouth for 2 minutes and swallow) and capsules. Cmax for fluconazole in saliva after the suspension was observed after 5 min and 182 times higher than maximum concentration in saliva after ingestion of the capsule (achieved after 4 h). After about 4 h the concentration of fluconazole in saliva were the same. The average AUC0-96 in saliva was significantly higher during the suspension than capsules. Significant differences in the rate of excretion of saliva or pharmacokinetics in blood plasma using two forms of issue have not been identified.

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  • Product Code: 8
  • Availability: In Stock
  • $29.99