Composition fluconazole 50 mg excipients: potato starch 43 mg, low-molecular polyvinylpyrrolidone 6 mg magnesium stearate or calcium stearate 1 mg. composition of the capsule casing: titanium dioxide 2%, gelatin up to 100%. The composition of the operculum capsules: titanium dioxide 1%, indigotin (Е132) 0.1333%, gelatin up to 100%. Pharmacological action Antifungal agent, has a highly specific effect, inhibiting the enzyme activity of fungi that are dependent on cytochrome P450. Blocks the conversion of lanosterol cells in fungi ergosterol; increases the permeability of cell membrane, violates its growth and replication. Fluconazole, being highly selective for cytochrome P450 of fungi, practically does not inhibit these enzymes in the human body (in comparison with Itraconazole, clotrimazole, econazole and ketoconazole, to a lesser extent inhibits dependent cytochrome P450 oxidative processes in human liver microsomes). Does not have antiandrogenic activity. Active opportunistic mycoses, including caused by Candida spp. (including generalized forms of candidiasis on the background of immunosuppression), Cryptococcus neoformans and Coccidioides immitis (including meningitis and encephalitis), Microsporum spp. and Trichophyton spp; in endemic mycosis caused by Blastomyces dermatidis, Histoplasma capsulatum (including with immunosuppression). Pharmacokinetics After oral fluconazole is well absorbed, eating does not affect the rate of absorption of fluconazole, its bioavailability is 90%. The time of Cmax after ingestion on an empty stomach 150 mg of the drug is 0.5-1.5 h and is 90% of the plasma concentration in the on/in the introduction in a dose of 2.5-3.5 mg/l. T1/2 of fluconazole is 30 hours Linking plasma protein - 11-12%. Concentration in plasma is directly dependent on the dose. 90%, the equilibrium concentration is reached in 4-5 day of treatment (when receiving a 1 times/). The introduction of a "shock" dose (first day), 2 times the usual daily dose, achieves a level of concentration corresponding to 90% of equilibrium concentration for the second day. Fluconazole penetrates well into all body fluids organism. The concentration of active substance in breast milk, joint fluid, saliva, sputum, and peritoneal fluid is similar to that in plasma. Constant values in vaginal secretions is achieved 8 hours after ingestion and are held at this level for at least 24 h. fluconazole penetrates well into the cerebrospinal fluid (CSF), with fungal meningitis the concentration in CSF is about 85% from its level in plasma. In sweat, the epidermis and the stratum corneum (selective accumulation) achieved concentrations in excess of serum. After intake of 150 mg on day 7 the concentration in the Horny layer of the skin - 23.4 µg/g and 1 week after receiving a second dose - 7.1 µg/g; concentration in nails after 4 months of application at a dose of 150 mg 1 time per week - 4.05 µg/g in healthy and 1.8 µg/g in affected nails. Vd approaches the total water content in the body. Is an inhibitor of the CYP2C9 isoenzyme in the liver. Write mainly kidneys (80% unchanged and 11% as metabolites). Fluconazole clearance is proportional to creatinine clearance (CC). Metabolites of fluconazole in peripheral blood was not detected. Pharmacokinetics of fluconazole depends significantly on the functional state of the kidneys, there is an inverse relationship between T1/2 and clearance of creatinine. After dialysis for 3 h the concentration of fluconazole in plasma is reduced by 50%.

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  • Product Code: 10
  • Availability: In Stock
  • $9.90