a9c2a64584268e2fc43e56c7827dce21

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a9c2a64584268e2fc43e56c7827dce21

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NEW 
100 % ORIGINAL

TRACKING NUMBER

THANK YOU FOR VISITING MY LOT

Composition Each capsule contains: active substance: fluconazole 50 mg; excipients: lactose 49,708 mg, corn starch 16.5 mg, silicon dioxide colloidal 0.117 mg, magnesium stearate 1,058 mg, sodium lauryl sulfate 0.117 mg; capsule shell: titanium dioxide (E171) 4.47 %, blue patent dye (E 131) 0.03 %, gelatin up to 100 %. Pharmacodynamics fluconazole, a triazole antifungal agent, is a potent selective inhibitor of Sterol synthesis in the fungal cell. Fluconazole has demonstrated activity in vitro and in clinical studies against most of the following microorganisms: Candida albicans, Candida glabrata (many strains are moderately sensitive), Candida parapsilosis, Candida tropicalis, Cryptococcus neoformans. Fluconazole activity has been shown in vitro against the following microorganisms, but the clinical significance of this is unknown: Candida dubliniensis, Candida guilliermondii, Candida kefyr, Candida lusitaniae. When taken orally, fluconazole is active on various models of fungal infections in animals. The activity of the drug in opportunistic mycoses, including those caused by Candida spp, has been demonstrated. (including generalized candidiasis in animals with suppressed immunity), Cryptococcus neoformans (including intracranial infections), Microsporum spp. and Trychophyton spp. Fluconazole activity was also established in models of endemic mycoses in animals, including infections caused by Blastomyces dermatitides, Coccidioides immitis (including intracranial infections) and Histoplasma capsulatum in animals with normal and suppressed immunity. Fluconazole has high specificity against fungal enzymes dependent on cytochrome P450. Fluconazole therapy at a dose of 50 mg / day for up to 28 days does not affect the concentration of testosterone in the blood plasma in men or the concentration of steroids in women of childbearing age. Fluconazole at a dose of 200-400 mg / day has no clinically significant effect on the levels of endogenous steroids and their response to stimulation of adrenocorticotropic hormone (ACTH) in healthy male volunteers. Mechanisms of development of resistance to fluconazole resistance to fluconazole can develop in the following cases: qualitative or quantitative change of the enzyme that is a target for fluconazole (lanosteril 14 -?- demethylase), reducing access to the target of fluconazole or a combination of these mechanisms. Point mutations in the ERG11 gene encoding the target enzyme lead to target modification and decreased affinity for azoles. An increase in ERG11 gene expression leads to the production of high concentrations of the target enzyme, which creates the need for an increase in the concentration of fluconazole in the intracellular fluid to suppress all enzyme molecules in the cell. The second significant mechanism of resistance is the active excretion of fluconazole from the intracellular space by activating two types of transporters involved in the active excretion (efflux) of drugs from the fungal cell. These transporters include the main mediator encoded by MDR (multidrug resistance) genes, and the ATP-binding cassette Transporter superfamily encoded by CDR genes (genes for resistance of Candida fungi to azole antimicotics). Overexpression of the MDR gene leads to resistance to fluconazole, while overexpression of CDR genes can lead to resistance to various azoles. Resistance to Candida glabrata is usually mediated by overexpression of the CDR gene, resulting in resistance to many azoles. For those strains in which the minimum inhibitory concentration (MIC) is defined as intermediate (16-32 µg/ml), maximum doses of fluconazole are recommended. Candida krusei should be considered as resistant to fluconazole. The mechanism of resistance is associated with reduced sensitivity of the target enzyme to the inhibitory effect of fluconazole. Pharmacokinetics the Pharmacokinetics of fluconazole are similar with intravenous administration and ingestion. After oral administration, fluconazole is well absorbed, its plasma concentrations (and total bioavailability) exceed 90 % of those of intravenous administration. Simultaneous eating does not affect the absorption of fluconazole. The plasma concentration is proportional to the dose and reaches a maximum (Cmax) in 0.5-1.5 h after fasting fluconazole, and the half-life is about 30 h. 90 % of the equilibrium concentration is achieved by 4-5 days after the start of therapy (with repeated administration of the drug once a day). The maximum concentration of fluconazole in saliva when taking the capsule is reached after 4 hours. The introduction of a shock dose (on day 1), twice the usual daily dose, makes it possible to achieve 90 % of the equilibrium concentration by day 2. The volume of distribution is close to the total water content in the body. Binding to plasma proteins is low (11-12 %). Fluconazole penetrates well into all body fluids. Concentrations of fluconazole in saliva and sputum are similar to its concentrations in blood plasma. In patients with fungal meningitis, the concentration of fluconazole in the cerebrospinal fluid is about 80 % of its concentration in blood plasma. In the stratum corneum, epidermis, dermis and sweat fluid are achieved high concentrations that exceed serum. Fluconazole accumulates in the stratum corneum. When taken at a dose of 50 mg once a day, the concentration of fluconazole after 12 days is 73 mcg/g, and 7 days after discontinuation of treatment — only 5.8 mcg/g. When used at a dose of 150 mg once a week, the concentration of fluconazole in the stratum corneum on the 7th day is 23.4 mcg/g, and 7 days after the second dose-7.1 mcg/g.

Dosage Inside. Capsules are swallowed whole. Therapy can be started before the results of sowing and other laboratory tests. However, antifungal therapy should be changed accordingly when the results of these studies become known. When transferring the patient from intravenous to oral administration of the drug or Vice versa, changes in the daily dose is not required. The daily dose of Diflucan depends on the nature and severity of the fungal infection. In infections requiring repeated administration of the drug, treatment should be continued until the disappearance of clinical or laboratory signs of active fungal infection. Patients with AIDS and cryptococcal meningitis or recurrent oropharyngeal candidiasis usually need supportive therapy to prevent relapses of infection. Use in adults 1. In cryptococcal meningitis and cryptococcal infections of other localization, 400 mg is usually used on the first day, and then treatment is continued at a dose of 200-400 mg once a day. The duration of treatment for cryptococcal infections depends on the presence of clinical and mycological effects; in cryptococcal meningitis, treatment is usually continued for at least 6-8 weeks. In cases of life-threatening infections, the daily dose can be increased to 800 mg.