DIFLUCAN - capsules

INSTRUCTIONS for use: DIFLUCAN

PHARMACOLOGICAL PROPERTIES: fluconazole - antifungal for systemic use, derivative triazole, highly selective inhibitor of sterol synthesis in cells mushrooms.

Revealing the effectiveness of fluconazole in different models of fungal infections in animals. Installed activity of the drug for opportunistic mycosis, including caused by Candida spp., Including generalizovanny candidiasis in animals with depressed immunity; Cryptococcus neoformans, including intracranial infections; Microsporum spp. and Trichophyton spp.

Has also identified the activity of fluconazole in models endemic mycosis in animals, including infection caused by Blastomyces dermatitides, Coccidioides immitis, including intracranial infections, and Histoplasma capsulatum in animals with normal and depressed immunity.

There's a message on the development of superinfection caused by several fungi of the genus Candida spp., Insensitive to fluconazole (for example, Candida krusei).

Fluconazole highly specific acts on fungal enzymes, which are dependent on the cytochrome P450. Therapy of fluconazole in dose of 50 mg / day for 28 days no impact on the concentration of testosterone in the plasma of the blood of men, or the concentration of steroids in women of childbearing age. Fluconazole in dose of 200 mg / day does not demonstrate any clinically significant impact on the levels of endogenous steroid hormones, and their response to ACTH stimulation in healthy male volunteers.

After receiving oral fluconazole is well absorbed. Bioavailability when administered is more than 90% of the level of fluconazole in plasma of blood in the on / in the introduction. Simultaneous eating does not affect the absorption of the drug.

Maximum concentration in blood plasma is achieved through 30-90 minutes after taking fluconazole on an empty stomach, and elimination half-life is about 30 hours.

Concentration in blood plasma is proportional to dose. 90% of the equilibrium concentration is achieved in 4-5-th day of treatment (in the application of one time per day).

Introduction to the loading dose (day 1), twice the usual daily dose, allows to accelerate the achievement of 90% of the equilibrium concentration - to the 2-th day. The volume of distribution is close to the total water content in the body.
Linking blood plasma proteins is low (11-12%).

Fluconazole penetrates into all body fluids organism. Fluconazole concentration in saliva and sputum are the same as its concentration in the blood plasma.

In patients with fungal meningitis fluconazole level in the CSF is about 80% of its level in the blood plasma.

In the corneal layer, epidermis, the dermis and the secret of the sweat glands, the drug accumulates in concentrations that exceed its concentration in the blood plasma. Fluconazole is accumulated in the horny layer of the skin. When taken in the dose of 50 mg once a day, the concentration of fluconazole in rogovom layer of the skin after 12 days, was 73 g / g, and in seven days after the completion of the treatment course - 5.8 g / g. When used in the dose of 150 mg once a week concentration of fluconazole in rogovom layer of the skin on the 7th day of reach of 23.4 g / g, and in seven days after receiving second dose and 7.1 g / g. The concentration of fluconazole in the nails after 4 months of use in the dose of 150 mg once a week was 4,05 g / g in healthy nails and 1.8 g / g in affected; after six months after the end of therapy fluconazole still determined to tell.

The drug is completely excreted with the urine, approximately 80% in an unmodified form. Fluconazole clearance is proportional to creatinine clearance. Circulating metabolites have not been identified.

The long half-life period provides an opportunity to use fluconazole once a day or once a week (in the presence of certain evidence).

INDICATIONS:

Cryptococcosis, including cryptococcal meningitis and infection of other sites (for example, lung, skin). Treatment can be carried out as in patients with normal immune status, as well as in patients with Aids, recipients of organs, and in patients with other forms of immunosuppression. Diflucan can be used as a maintenance therapy to prevent recurrence of cryptococcosis in patients with Aids.
Generalizovanny candidiasis, including candidemia, disseminated candidiasis, a fungal infection of the abdominal cavity, endocardium, eyes, respiratory and urinary tract. The treatment can be performed in patients with malignant neoplasms, the patients of the intensive care unit, patients who receive cytotoxic or immunosuppressive funds, as well as in the presence of other factors, which may lead to the development of candidiasis.
Candidiasis mucous membranes, including the oral cavity and pharynx, esophagus, neinvaziynye bronchopulmonary infections, candiduria, skin and mucous membrane and chronic oral atroficski candidiasis (caused by wearing dentures). The treatment can be performed in patients with normal immune status or with immunosuppression. Prevention of the recurrence of oropharyngeal candidiasis in patients with Aids.
Genital candidiasis. Acute or recurrent vaginal candidiasis. Prophylactic use of to reduce the frequency of recurrent vaginal candidiasis (three or more episodes per year). Candidal balanitis.
Prevention of fungal infections in patients with malignant tumors, which can develop as a consequence of cytotoxic chemotherapy or radiation therapy.
Mikozy skin, including tinea pedis, body, inguinal region, Pityriasis versicolor, onychomycosis and cutaneous candidosis infections.
Deep endemic mycosis in patients with normal immune status, coccidioidomycosis, parakoktsidiomikoz, sporotrihoz, gistoplazmoz.
USE: daily dose depends on the nature and severity of fungal infection.

When transferring a patient with on / in the introduction to oral medication or vice versa, there is no need to change the daily dose. With vaginal candidiasis in most cases effectively single application. The infections, which require repeated use of the drug, treatment should continue until the disappearance of clinical or laboratory signs of the active fungal infection. Insufficient duration of treatment may lead to reinfection. Aids patients and cryptococcal meningitis or patients with relapsing oropharyngeal candidiasis for the prevention of recurrence of the infection, as a rule, required to supporting therapy.
In cryptococcal meningitis and cryptococcal infection of other sites on the first day appoint 400 mg, and then continue to treatment with the drug in a dose of 400 mg 1 time per day. The duration of treatment of cryptococcal infection depends on clinical and mycological efficiency: in cryptococcal meningitis is still at least 6-8 weeks. With a view to the prevention of relapse of cryptococcal meningitis in patients with Aids after completing a full course of primary treatment therapy Diflyukanom in dose of 200 mg / day can be continued for a long time.
When candidemia, disseminirovannom 4-8 and other forms of invasive candida infections the dose, as a rule, is 400 mg on the first day, then 200 mg / day. Depending on the degree of clinical effect dose can be increased to 400 mg / sut. The duration of therapy depends on its clinical effectiveness.
In urinary tracts candida Diflucan, as a rule, appoint 50 mg once a day for 7-14 days. If necessary in patients with severe immunosuppression, treatment should be continued for longer periods of time. When atrophic candidiasis of the oral cavity, caused by the wearing of dental prostheses, the drug is usually administered in the dose of 50 mg / day for 14 days in combination with the use of antiseptic means for the treatment of dental prosthesis. In other candidal infection of the mucous membranes (with the exception of genital candidiasis) (see below), for example, esophagitis, noninvasive bronchopulmonary infections, candiduria, candidiasis the skin and mucous membranes, etc., The effective dose, as a rule, is 50-100 mg / day for the treatment duration of 14-30 days. For the prevention of recurrence of oropharyngeal candidiasis in patients with Aids after completing a full course of primary therapy Diflucan can be assigned to 150 mg one time per week.
In vaginal candidiasis Diflucan take once inside, in the dose of 150 mg. To reduce the frequency of recurrent vaginal candidosis the drug is used in the dose of 150 mg once a month. Duration of treatment is determined individually, it varies from 4 to 12 months. For the treatment of some patients may require more frequent use of the drug.
When Candida balanite Diflucan appoint one in the dose of 150 mg orally.
To prevent candidiasis, the recommended dose of Diflucan is 50-400 mg 1 time per day depending on the degree of risk of the development of fungal infection. With a high degree of risk of a generalized infection, for example in patients with the expressed or prolonged neutropenia the recommended dose is 400 mg one time per day. Diflucan is prescribed for a few days before the expected neutropenia; after the increase in the number of neutrophilic granulocytes in the blood up to the level of more than 1000 per 1 mm3 treatment is continued for 7 days.
For infections of the skin, including tinea pedis, the skin of the groin, and candidal infections the recommended dose is 150 mg one time per week or 50 mg once a day. In such cases, therapy lasts for 2-4 weeks, however, with mycosis stop may require more prolonged use of the drug (up to 6 weeks).
In Pityriasis versicolor, the recommended dose is 300 mg one time a week for two weeks; in some patients, it is necessary to appoint the third dose of 300 mg a week after the second dose, in some cases, a single admission to the dose of 300-400 mg. Alternative treatment scheme is the use of Diflucan 50 mg one time per day during 2-4 weeks.
Onychomycosis (Tinea unguium) recommended dose is 150 mg one time per week. Treatment should be continued until the replacement of the infected nail (the formation of disease-free nail). Re-growth of nails on the hands and feet requires 3-6 months, 6-12 months, respectively. However, the speed of nails growth may