Details

Description

Release form, composition and packaging

Capsules 1 capsule

fluconazole

50 mg

1 PC.

- contoured cell packages (aluminum / PVC) (1) - cardboard packs.

7 pcs.

- contour cell packages (aluminum / PVC) (1) - cardboard packs.

pharmachologic effect

Triazole derivative antifungal agent.

It is a selective inhibitor of sterol synthesis in the fungal cell.

Fluconazole is highly specific for cytochrome P450 dependent fungal enzymes.

Oral and intravenous administration fluconazole was active in various models of fungal infections in animals.

Fluconazole is active in opportunistic mycoses, incl. caused by Candida spp., including generalized candidiasis in animals with reduced immunity Cryptococcus neoformans, including intracranial infections Microsporum spp. and Trychoptyton spp. It is active in 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 reduced immunity. Pharmacokinetics The pharmacokinetics of fluconazole is similar when administered intravenously.

After oral administration, fluconazole is well absorbed, its plasma levels (and overall bioavailability) exceed 90% of the plasma levels of fluconazole when administered intravenously.

Concomitant food intake does not affect oral absorption.

Cmax is reached within 0.5-1.5 hours after taking fluconazole on an empty stomach.

Plasma concentration is proportional to the dose.

90% Css is reached by the 4th-5th day after the start of therapy (with repeated administration 1 time / day).

The introduction of a loading dose (on the 1st day), 2 times the average daily dose, makes it possible to achieve Css 90% by the 2nd day.

The apparent Vd approaches the total body water content.

Plasma protein binding is low (11-12%).

Fluconazole penetrates well into all body fluids.

Fluconazole levels in saliva and sputum are similar to those in blood plasma.

In patients with fungal meningitis, the levels of fluconazole in the cerebrospinal fluid are about 80% of its plasma levels.

In the stratum corneum, epidermis-dermis and sweat fluid, high concentrations are achieved, which exceed serum concentrations.

Fluconazole accumulates in the stratum corneum.

When taken in a dose of 50 mg 1 time / day, the concentration of fluconazole after 12 days was 73 Ојg / g, and 7 days after stopping treatment - only 5.8 Ојg / g.

When used in a dose of 150 mg 1 time / week.

the concentration of fluconazole in the stratum corneum on the 7th day was 23.4 Ојg / g, and 7 days after taking the second dose - 7.1 Ојg / g.

Concentration of fluconazole in nails after 4 months of use at a dose of 150 mg 1 time / week.

was 4.05 Ојg / g in healthy and 1.8 Ојg / g in affected nails

6 months after completion of therapy, fluconazole was still detectable in the nails.

Fluconazole is excreted mainly by the kidneys

approximately 80% of the administered dose is found unchanged in the urine.

Fluconazole clearance is proportional to CC.

No circulating metabolites were found.

Prolonged T1 / 2 from blood plasma allows you to take fluconazole once for vaginal candidiasis and 1 time / day or 1 time / week. for other indications. Indications for use Cryptococcosis, including cryptococcal meningitis and infections of other localization (eg, lungs, skin), incl. in patients with a normal immune response and in AIDS patients, organ transplant recipients and patients with other forms of immunodeficiency supportive therapy for the prevention of recurrence of cryptococcosis in AIDS patients.

Generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidiasis, such as infections of the peritoneum, endocardium, eyes, respiratory and urinary tract, incl.

in patients with malignant tumors in the ICU and receiving cytotoxic or immunosuppressive drugs, as well as in patients with other factors predisposing to the development of candida

Name ENG

FLUCONAZOLE

Clinical and pharmacological group

Antifungal drug

Dosage

150mg

Indications

Cryptococcosis, including cryptococcal meningitis and infections at other sites (eg, lungs, skin), incl.

in patients with a normal immune response and in AIDS patients, organ transplant recipients and patients with other forms of immunodeficiency

maintenance therapy to prevent relapse of cryptococcosis in AIDS patients.

Generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidiasis, such as infections of the peritoneum, endocardium, eyes, respiratory and urinary tract, incl.

in patients with malignant tumors in the ICU and receiving cytotoxic or immunosuppressive drugs, as well as in patients with other factors predisposing to the development of candidiasis.

Candidiasis of the mucous membranes, including the mucous membranes of the oral cavity and pharynx, esophagus, non-invasive bronchopulmonary infections, candiduria, mucocutaneous and chronic atrophic oral candidiasis (associated with wearing dentures), incl.

in patients with normal and suppressed immune function

prevention of recurrence of oropharyngeal candidiasis in AIDS patients.

Genital candidiasis

acute or recurrent vaginal candidiasis

prevention in order to reduce the frequency of relapses of vaginal candidiasis (3 or more episodes per year)

candidal balanitis.

Mycoses of the skin, including mycoses of the feet, body, groin, pityriasis versicolor, onychomycosis and skin candidal infections.

Deep endemic mycoses in patients with normal immunity, coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis.

Prevention of fungal infections in patients with malignant tumors predisposed to the development of such infections as a result of cytotoxic chemotherapy or radiation therapy.

Contraindications

Simultaneous use of terfenadine during repeated use of fluconazole at a dose of 400 mg / day or more

concomitant use of cisapride

hypersensitivity to fluconazole

hypersensitivity to azole derivatives with a structure similar to fluconazole.

Storage conditions and periods

At a temperature not higher than 25 degrees.

Expiration date: 3 years

INN / Active ingredient

fluconazole

Specifications