Index of drugs

Treatment of the following fungal infections in adult patients: cryptococcal meningitis; kokcydioidomykozy; invasive candidiasis; yeast infection of the mucous membranes, including throat infections, oesophageal esophageal infection, occurrence of yeasts in the urine and chronic yeast infections of the skin and mucous membranes; chronic atrophic candidiasis (associated with the use of dental prostheses), if oral hygiene or local treatment are insufficient; vaginal fever, acute or recurrent when local treatment is inadequate; yeast acorn inflammation when local treatment is inadequate; skin fungal infections including tinea pedis, trunk, shanks, dandruff dermatitis and dermal yeast infections when systemic therapy is recommended; onychomycosis when it is considered that other medicines are unsuitable.Prevention of the following fungal infections in adult patients: relapse of cryptococcal meningitis in patients with an increased risk of relapse; relapse of yeastitis of the mouth and throat or esophagus in HIV-infected patients who are at increased risk of recurrence; reduction of the rate of recurrence of vaginal candidiasis (4 or more infections during the year); prophylaxis of fungal infection in patients with prolonged neutropenia (eg in patients with blood cancers, receiving chemotherapy or in patients after transplantation of hematopoietic stem cells).The following infections in newborns, infants, children and adolescents aged 0 to 17 years: treatment of yeast infection (mouth, throat and esophagus), invasive candidiasis, cryptococcal meningitis; prevention of yeast infections in immunocompromised patients. The drug can be used as a maintenance treatment to prevent the recurrence of cryptococcal meningitis in children at high risk of relapse. Treatment may be started prior to receiving the results of culture or other laboratory tests; however, after receiving them, the available treatment should be adjusted accordingly. Official guidance on the proper use of antifungal drugs should be taken into account.

1 capsule contains 50 mg, 100 mg, 150 mg or 200 mg fluconazole; capsules contain lactose.

Antifungal medicine from the group of triazoles. It inhibits the synthesis of ergosterol, necessary for the synthesis of the fungal cell membrane. Works on:Candida spp. (exceptC. krusei), Cryptococcus neoformans, Cryptococcus gattii, Blastomyces dermatiditis, Coccidioides immitis, Histoplasma capsulatum, Paracoccidioides brasiliensis. The bioavailability after oral administration is> 90%; C_max it is reached 0.5-1.5 hours after administration. Plasma proteins bind in 11-12%. Fluconazole penetrates well into all body fluids. Fluconazole concentrations in saliva and sputum are similar to those in plasma. In patients with fungal meningitis, fluconazole concentrations in the cerebrospinal fluid reach 80% of the plasma concentration. High levels of fluconazole in the skin, exceeding the plasma concentrations, are achieved in the stratum corneum, epidermis and dermis and sweat glands. Fluconazole is only slightly metabolised (approximately 11%). The main route of excretion of the drug are kidneys, about 80% of the applied dose is present in the urine in unchanged form. T_0,5 is 30 hours.

Hypersensitivity to Fluconazole, to other azole derivatives or to any of the excipients. The use of QT prolonging drugs that are metabolised by CYP3A4, such as cisapride, astemizole, pimozide, quinidine, Erythromycin, is contraindicated. Terfenadine is contraindicated in patients receiving multiple doses of fluconazole, ≥400 mg / day.

Fluconazole has not been shown to be more effective than Griseofulvin in the treatment of tinea head skin in children, and the overall recovery rate was less than 20%, therefore fluconazole should not be used to treat mycosis of the scalp. Data on the efficacy of fluconazole in the treatment of cryptococcosis in other locations (eg cryptococcosis of the lung or skin) are limited - no precise dosing recommendations. Data on the efficacy of fluconazole in the treatment of other forms of endemic mycosis such as paracoccidioidomycosis, lymphocutaneous sporotrichosis and histoplasmosis are limited - no precise dosing recommendations. Use with caution in patients with impaired renal or hepatic function. Patients receiving fluconazole should be monitored for symptoms of hepatic dysfunction (such as severe asthenia, anorexia, prolonged nausea, vomiting and jaundice). If abnormal liver function tests occur during fluconazole treatment, the patient should be carefully monitored for any serious damage to the organ. Carefully use in patients with a predisposition to arrhythmia. for example, with myocardial diseases, electrolyte disturbances and concomitantly treated with preparations that may cause arrhythmia. Co-administration of fluconazole and halofantrine is not recommended due to the risk of QT interval prolongation. Patients receiving terfenadine and fluconazole at doses of <400 mg / day should be carefully monitored. Use caution when using fluconazole in combination with drugs with which it interacts, especially drugs with a narrow therapeutic range, metabolised by CYP2C9, CYP2C19, CYP3A4. Discontinue use in patients with superficial mycosis if a rash associated with fluconazole develops. The occurrence of rash in patients with invasive or systemic infections is an indication for accurate observation and discontinuation of the drug in the case of developing bullous lesions or erythema multiforme. Due to the lactose content, the capsules should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

Standard doses of fluconazole (<200 mg / day) and short-term treatment should not be used during pregnancy unless absolutely necessary. High doses of fluconazole should not be used during pregnancy, particularly those given in a prolonged period, except for life-threatening infections. Breastfeeding may be continued after a single dose of fluconazole ≤200 mg. Breast-feeding should be discontinued during treatment with multiple and / or higher doses.

Common: headache, abdominal pain, vomiting, diarrhea, nausea, increased alkaline phosphatase, AST and ALT, rash. Uncommon: anemia, decreased appetite, insomnia, drowsiness, convulsions, disturbances of taste, constipation, dyspepsia, bloating, dry mouth, jaundice, cholestasis, increased bilirubin, drug eruption, urticaria, pruritus , severe sweating, muscle pain, tiredness, feeling unwell, asthenia, fever. Rare: agranulocytosis, leukopenia, neutropenia, thrombocytopenia, anaphylaxis, hypercholesterolemia, hypertriglyceridaemia, hypokalaemia, tremor, QT interval prolongation, torsade de pointes, hepatic failure, hepatic cell necrosis, hepatitis, liver cell damage (the use of fluconazole was rarely associated with severe toxic liver damage, including fatalities, mainly in patients with severe underlying diseases), toxic epidermal necrolysis, Stevens syndrome - Johnson, acute generalized pustular exanthema, exfoliative dermatitis, angioneurotic edema, swelling of the face, alopecia.

Orally.Adults. cryptococcosis - Treatment of cryptococcal meningitis: 400 mg on day 1, then 200-400 mg / day, usually for 6-8 weeks; in life-threatening infections, the dose may be increased to 800 mg / day. Maintenance treatment to prevent the recurrence of cryptococcal meningitis in patients at high risk of recurrence: 200 mg / day, the duration of treatment is unlimited.coccidioidomycosis200-400 mg / day, usually 11-24 monthsor longer; for some infections a dose of 800 mg / day should be considered, especially in meningitis.Invasive candidiasis: 800 mg on day 1, then 400 mg / day; the usually recommended length of treatment for yeast blood infection is 2 weeks after the first negative blood culture result and the disappearance of the signs and symptoms characteristic of candidiasis.Treatment of candidiasis mucous membranes - Oral candidiasis: 200-400 mg on day 1, then 100-200 mg / day, usually for 7-21 days or longer for patients with severe immune function impairment. Esophageal candidiasis: 200-400 mg on day 1, then 100-200 mg / day, usually for 14-30 days or longer for patients with severe immune function impairment. Candidature: 200-400 mg / day, usually for 7-21 days or longer for patients with severe immune function impairment. Chronic atrophic candidiasis: 50 mg / day for 14 days. Chronic candidiasis of the skin and mucous membranes: 50-100 mg / day for 28 days or longer for patients with severe immune function impairment.Prevention of relapsed yeast inflammation in HIV-infected patients who are at high risk of recurrence - Oral candidiasis, esophageal candidiasis: 100-200 mg / day or 200 mg three times a week, the duration of treatment is unlimited.Genital candidosis - Acute candidiasis of the vagina, yeast inflammation of the glans: 150 mg once. Treatment and prophylaxis of recurrent vaginal candidiasis (4 or more episodes in a year): 150 mg every third day, a total of 3 doses (days 1, 4 and 7), followed by a maintenance dose of 150 mg once a week; maintain the maintenance dose for 6 monthsMycosis of the skin - Foot mycosis, athlete's torso, thrush of the lower leg, skin candidosis: 150 mg once a week or 50 mg once a day for 2-4 weeks; in foot tinea, it may be necessary to use up to 6 weeks. Dandruff versicolor: 300-400 mg once a week for 1-3 weeks or 50 mg once a day for 2-4 weeks. Onychomycosis: 150 mg once a day week .; treatment should be continued until the infected nail is replaced by a new, uninfected, i.e. about 3-6 months for hand nails or 6-12 months for the nails of the feet (after curing a chronic infection, nails may sometimes remain distorted).Prevention of fungal infections in patients with prolonged neutropenia: 200-400 mg / day, the treatment should start several days before the expected occurrence of neutropenia and continue for 7 days after an increase in the neutrophil count to> 1,000 / mm³. Children and youth. In the pediatric population, a dose of 400 mg / day should not be exceeded. Depending on the severity and degree of maturity, it should be estimated which dosage (for adults or children) is the most suitable for adolescents aged 12-17. Clinical data indicate that children have a greater clearance of fluconazole than adult patients. The doses of 100, 200 and 400 mg in adults correspond to 3, 6 and 12 mg / kg. doses in children. The safety and efficacy profile of fluconazole in the treatment of genital candidiasis in children and adolescents has not been established. If it is necessary to treat genital candidiasis in adolescents (aged 12-17 years), the same dosage should be used as in adults.Newborns from the 28th day of life, infants and children up to 11 years old - Mucosal candidosis: 6 mg / kg / day on day 1, then 3 mg / kg / day. Invasive candidiasis, cryptococcal meningitis: 6-12 mg / kg / day. Maintenance treatment to prevent the recurrence of cryptococcal meningitis in children at risk of relapse: 6 mg / kg / day. Prevention of yeast infections in immunocompromised children: 3-12 mg / kg / day depending on the severity and duration of neutropenia.Newborns up to the 27th day of lifeDuring the first and second weeks of a child's life (age 0-14 days), the same dose should be given in mg / kg as in infants and children, but administered every 72 hours (do not exceed the maximum dose) mg / kg, administered every 72 h); at the 3rd and 4th weeks of life (15-27 days) the same dose should be administered every 48 hours (do not exceed the maximum dose of 12 mg / kg administered every 48 hours). There is little pharmacokinetic data to support such a dosage regimen in newborns.Special groups of patients. Patients with impaired renal function. In the case of a single administration, no dose adjustment is necessary. In patients (including the pediatric population) with impaired renal function, a loading dose of 50 mg to 400 mg should be given at the beginning of multidose fluconazole therapy based on the recommended daily dose for the indication. After the loading dose, the daily dosage (as indicated) should be determined based on the creatinine clearance (CCr):> 50 ml / min - administered 100% of the recommended dose; ≤50 ml / min (patients not on dialysis) - 50% of the recommended dose; patients regularly dialyzed - 100% of the recommended dose after each dialysis (on days on which dialysis is not performed, patients should receive a reduced dose consistent with CCr). The pharmacokinetics of fluconazole in children with renal failure have not been studied. There is no need to change the dosage in elderly patients with normal renal function.Way of giving. The drug can be used regardless of the meals you take. Swallow the capsules whole.