FLUKAM

Trade name: Flukam

International name: Fluconazole

Dosage band and prescription: Capsules 150mg for oral intake

Formula:

• Active substance: Fluconazole
• Additives: lactose monohydrate, colloid silicon dioxide, magnesium stearate, corn starch, sodium lauryl sulfate.

Pharmacotheraputical group:

Flukam belongs to the antifungal group of preparations.

Pharmacological qualities

Pharmacodynamics.

Fluconazole belongs to antifungal agents of triazole group; it is a strong selective inhibitor of sterol synthesis in fungus cell membranes, mechanism of action is subject to cytochrome P-450 block. Candida spp., Cryptococcus spp., Microsporum spp. и Tricbophyton spp. are most sensitive to fluconazole. Fluconazole is active in endemic mycoses, caused by Blastomyces dermatitidis, Coccidioides immitis (including intracranial infections) and Histoplasma capsulatum.

Candida krusei и Candida glabrata strains are resistant to fluconazole; fluconazole should not be prescribed during aspergillosis and zygomycosis treatment.

Pharmacokinetics:

After intake fluconazole is quickly absorbed in gastrointestinal tract, its concentration levels in plasma and comparative bioavailability exceed 90% of fluconazole concentration levels when injected intravenously. Simultaneous food intake does not affect absorption of the preparation. After fasting oral intake, concentration peak of fluconazole in plasma is observed in 30–90 minutes; half-life is 30 hours.

Fluconazole concentration levels in plasma are in direct proportion to the injected dose, the level of 90% equilibrium concentration in plasma when taken once daily is reached on the 4th-5th day of treatment.

The intake of the loading dose (in the first day of treatment) twice as much as the daily dose, allows to reach the level of 90% equilibrium concentration in plasma on the second day of treatment. Distribution volume of the preparation approximates total water content in the body. Protein binding comprises 11–12%.

Fluconazole properly penetrates into the tissues, in all biological body fluids; its concentration levels in saliva and phlegm are similar to its concentration levels in plasma. The content of fluconazole in cerebrospinal fluid in patients with fungal meningitis reaches approximately 80% of its content in plasma.

In epidermis, derma, exuding sweat, concentrations exceeding serum concentrations are reached. Fluconazole is accumulated in the horny layer, in single intake of the daily dose of 50mg, fluconazole concentration comprised 73mkg/g in 12 days, and 5,8mkg/g in 7 days after the end of treatment. In application of 150g once a week fluconazole concentration in the horny layer comprised 23,4mkg/g, and 7,1mkg/g in 7 days after the intake of the second dose. Fluconazole concentration in nails after 4-month course of preparation application in the dose of 150mg once a week comprised 4,05mkg/g in healthy nails, 1,8mkg/g in affected nails. Fluconazole is observed in nails in 6 months after the end of treatment course.

Fluconazole is eliminated mainly through kidneys; up to 80% of the taken dose is eliminated with urine in the unchanged form. Fluconazole clearance is in direct proportion to creatinine clearance.

No fluconazole metabolites were observed in the peripheral blood.

Long-term half-life of fluconazole allows to prescribe the preparation once in genital candidiasis and apply the preparation once daily or weekly in course treatment according to other indications.

Indications:

Medical treatment can be started before getting the results of cultural diagnostics and other laboratory tests, but after getting the results of mycological examination the scheme of treatment has to be appropriately adjusted.

Fluconazole is indicated for the treatment and prevention of the following illnesses caused by pathogenic fungus:

— Cryptococcosis, including cryptococcal meningitis and other localizations of this infection (lungs, skin and other).

— General candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidal infections, including candidal damage of peritoneum, endocardium, eyes, respiratory and urinary tract, and other organs.

— Candidiasis of mucous coat, including mucous coat damage of oral cavity, pharynx, esophagus; noninvasive bronchopulmonary candidiasis, candiduria, skin moniliasis, atrophic oropharyngeal candidiasis, caused by wearing dental prosthesis.

— Genital candidiasis, including vaginal candidiasis (acute or chronic recurrent).

— Prophylaxis of mycotic lesion in patients with malignant growths inclined to such infections as the result of cytostatic treatment and radiotherapy.

— Dermatomycosis, including foot mycosis, inguinal region mycosis, chromophytosis, onychomycosis, skin moniliasis.

— Systemic endemic mycosis, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with average immunity.

Contraindications:

Preparation is contraindicated in patients who have shown hypersensitivity to

fluconazole or to those, similar in composition to azoles, to other constituents of preparation.

It is not recommended to prescribe the preparation during pregnancy or lactation period.

Overdosage:

Single application of excessive dosage of fluconazole may lead to breakdown. See Your doctor immediately or resort to the nearest medical institution.

Take capsules with water.

It is recommended to take capsules at one and the same time of the day.

Preparation can be taken both during mealtimes and during intervals between food intake.

Method of application and dosage:

Preparation should be taken according to doctor’s prescription in order to avoid complications.

Daily doze of fluconazole depends on the type and severity of fungal infections.

Treatment, as the rule, involves multiple intake of the preparation up to the full disappearance of clinical and laboratory symptoms.

In case of early interruption of treatment relapse is possible.

ADULTS:

• Oropharyngeal candidiasis- 50-100mg once daily during 7–14 days and more.
• Oropharyngeal infections caused by wearing dental prosthesis- 50mg once daily during 14 days (on condition of prosthesis disinfection).
• Candidal infections of esophagus, noninvasive lung infections, urinary tract infections, and conditions caused by mucocutaneous candidiasis- 50-100mg once daily during 14–30 days.
• Prevention of oropharyngeal candidiasis relapse in patients with AIDS- 150mg once a week.
• Treatment of genital candidiasis- 150mg once.
• Treatment of women with relapse of vaginal candidiasis (3 or more times a year) — 150mg once a month during 4–12 months and more if required.
• Fungal skin infections- 50mg once daily and 150mg once a week during 2–4 weeks.
• Feet dermatomycosis’s required length of treatment may come up to 6 weeks.
• Chromophytosis- 300mg once a week during 2 weeks. Some patients might require third dose of 300 mg a week, while 300-400mg of Fluconazole once are enough for other patients. Another scheme of treatment — 50mg daily during 2–4 weeks.
• Onychomycosis- 150mg once a week, usually during 3–6 months (hands) and 6–12 months (feet).
• Candidiasis of internal organs — 400mg (first day), then 200-400mg once daily. In cases of candidal infections that are life-threatening, the dose can be increased up to 800mg daily.
• Prevention of candidal infections relapse -50- 4mg once daily during the risky period of development of infection.
• Cryptococcal infections of internal organs- 400mg (first day), then 200-400mg once daily. In cases of cryptococcal infections that are life-threatening, the dose can be increased up to 800mg once daily.
• For suppression of relapse of cryptococcal meningitis in patients with AIDS- 200mg daily during uncertain length of time.
• Coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis- 200-400mg once daily during 2 оr more years.

Children at the age of 4-15years:

• Oropharyngeal candidal infections- 3mg/kg once daily (first day), further 6mg/kg daily.
• Candidal or cryptococcal infections of internal organs- 6–12 mg/kg once daily.
• Prevention of fungal infections during the risky period of their development- 3–12 mg/kg daily.

Age 3–4 weeks- same dose is taken in 48 hours.

Age 2 weeks- same dose is taken in 72 hours.

Elderly people

If case of absence of kidney diseases, the preparation is prescribed in the same dose as for adults.

Patients with kidney deseases

Doctor can change the dose according to the function of kidneys. Doctors sometimes prescribe the preparation in other doses.

If You missed the intake of preparation, do not worry and take another dose at the usual time

Side effect:

Usually Flukam is tolerated well by patients. There are rarely dyspeptic effects, headache.

Form of issue:

Capsules. Fluconazole 150mg.1 capsule in a blister.

Conditions of delivery at chemistry stores:

Delivered without prescription.

Terms of storage:

Should be stored under temperature -not above 25˚ С and kept out of reach of children.

Expiry period:

Do not take the preparation after the expiry date printed on the package.