Diflucan (Fluconazole)

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    Diflucan is the brand name of antifungal triazole, an international non-proprietary name of which Fluconazole. The drug was synthesized in the laboratory of the French company Pfizer in 1982, and in the early 90ies of the previous century was massively utilised in fungal infections therapy.

    The main active substance, fluconazole, provides inhibition of cell metabolism in fungi by virtue of binding substances, running concurrently with inhibition and producing cytochrome P-450, a largely represented element that contains in number of fungal cells. Even though the organism absorbs the substance, it works selectivity and considered to be a relatively safe treatment mean. In addition, Diflucan blocks the protective cell membranes formation by inhibiting sterols synthesis and improving their permeability, restoring damaged membranes. The primary scope of Diflucan action includes a long range of diseases: skin lesions, meningitis, vaginal candidiasis, etc.

    Pharmacological action

    The drug is rapidly absorbed from the gastrointestinal tract within 2 hours (and the availability of the drug in various forms of administration does not differ by more than 7%). The absorption of Diflucan is not affected by meals. The preparation is characterized by a relatively long long half-life; which means that taking the medication is recommended once a day only. However, to achieve the therapeutic effect in some cases, a single application is more than sufficient. The distribution of the preparation on body tissues (it doesn’t penetrate into the brain tissue and bone tissue) is comparable to the concentration in the blood plasma.

    No interaction with components of oral contraceptives has also been revealed. In accordance with clinical trials, Diflucan inhibits P-450 element processed in animal cells in 20-200 times less than ketoconazole, and it is unlikely that it can cause endocrine complications. Diflucan is rapidly absorbed from the gastrointestinal tract when taken periorally. Its bioavailability is independent of food intake and gastric pH, reaching 94%. Diflucan is weakly bound to plasma proteins (12% and less), having a long (about 30 hours) half-life period, rapidly penetrating tissue fluids. Approximately 70% of the dose is excreted unchanged in the urine. It was shown that 150 mg in a single dose of Diflucan generates plasma for 3-4 days, the drug concentration that exceed the minimum inhibitory concentration (MIC) for most strains of Candida albicans.

    Indications for use

    A new preparation of a broad spectrum of action is deprived of a number of shortcomings observed in various antimycotics; and used to treat fungal infections of different localization. Its mechanism of action, as well as in other imidazoles, are aimed at inhibition of P-450 enzymes – mediators that participate in sterol synthesis (an important component of the cell wall of the fungus). At the same time triazoles interfere with steroidogenesis in humans. However, in clinical trials the effect on metabolic profile in women, including endocrinological profile, lipid and carbohydrate metabolism was not observed.

    How to use Diflucan (Fluconazole)

    The preparation is designed to deal with fungal mucous membranes (primarily of genital nature: candida vulvitis, vulvovaginitis in women and candida balanoposthitis in males). In acute vulvovaginal candidiasis and vulvitis treatment, Diflucan is prescribed in the complex therapy only. A systematic use of Diflucan implies taking single doses of 150mg (meals do not affect the absorption), the drug should be washed down with plenty of water. The treatment with antifungal drugs in men implies using the medicament in the form of a cream/ ointment, while the dose and multiplicity of use should be equal as in women. Both partners are encouraged to strictly refrain from sexual activity.

    In chronic case of chronic vulvovaginal candidiasis/vulvitis, the treatment strategy consists in accurate determination of the cause, while the recommended dose of Diflucan equals 150 mg twice a day with 3 day pauses. In chronic vulvovaginal candidiasis and vulvitis, the treatment strategy consists in accurate determination of the cause, while the recommended dose of Diflucan is equal to 150mg divided into 2 intakes and with 3 day pauses in between.