Active substanceFluconazoleFluconazole
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  • Dosage form: & nbspsolution for infusions
    Composition:
    1 bottle contains:
    Active substance: fluconazole - 200 mg
    Excipients: sodium chloride, disodium edetate, water for injection.

    Description:
    A clear, colorless solution.

    Pharmacotherapeutic group:Antifungal agent.
    ATX: & nbsp

    J.02.A.C   Triazole derivatives

    J.02.A.C.01   Fluconazole

    Pharmacodynamics:
    Fluconazole is a representative of the class of triazole antifungal agents, it is a selective inhibitor of the synthesis of sterols in the fungal cell. The drug is active in mycoses caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichoptyton spp., Blastomyces dermatitides, Coccidioides immitis and Histoplasma capsulatum.

    Pharmacokinetics:
    After intravenous administration fluconazole well penetrates into tissues and body fluids. Concentrations of the drug in saliva and sputum are similar to those in plasma. In patients with fungal meningitis, the fluconazole content in the cerebrospinal fluid reaches 80% of the corresponding levels in the plasma.
    Concentrations in the plasma are in direct proportion to the dose. Ninety per cent level of equilibrium concentration is reached by 4-5 days after several administrations at a dose per day.
    The use on the first day of a dose that is twice the usual daily dose allows one to achieve plasma levels of the drug that approach 90% of the equilibrium concentrations by the second day. The apparent volume of distribution approximates the total volume of water in the body. A small fraction of fluconazole (11-12%) binds to plasma proteins.The half-life is long (30 hours). Fluconazole is excreted from the body mainly by the kidneys; while approximately 80% of the administered dose is excreted in the urine unchanged. The clearance of fluconazole is in direct proportional dependence on the creatinine clearance. Metabolites in the peripheral blood were not detected.

    Indications:
    Fluconazole is used to treat the following diseases:
    Cryptococcosis: cryptococcal meningitis, cryptococcal infections of the lungs and skin; prevention of recurrence of cryptococcosis in AIDS patients, organ transplantation or in other cases of immunodeficiency.
    Generalized Candidomycosis: candidemia, disseminated candidiasis and other forms of invasive candidiasis infections (infections of the abdominal cavity, endocardium, eyes, respiratory and urinary tracts).
    Candidomycosis of mucous membranes: oral cavity, pharynx, esophagus and non-invasive bronchopulmonary infections, candiduria.
    Vaginal candidiasis is acute or in a chronic recurrent form.
    Prevention of fungal infections in patients with malignant neoplasms that are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy.

    Contraindications:
    The use of fluconazole is contraindicated in patients with hypersensitivity to the drug or to a similar structure of azole compounds. Contraindicated simultaneous use of terfenadine, astemizole and cisapride.

    Carefully:
    Hepatic insufficiency, the appearance of rash on the background of fluconazole in patients with superficial fungal infection and invasive / systemic fungal infections, concurrent administration of terfenadine and fluconazole at a dose of less than 400 mg / day, potentially pro-rhythmic conditions in patients with multiple risk factors (organic heart disease, disorders electrolyte balance, simultaneous reception of drugs that cause arrhythmias).

    Pregnancy and lactation:
    The use of the drug in pregnancy is contraindicated, except for severe, generalized and potentially life-threatening fungal infections.
    If it is necessary to use during lactation, breastfeeding should be stopped.

    Dosing and Administration:
    Fluconazole in the form of a solution for infusion is administered intravenously drip at a rate of no more than 20 mg (10 ml) / min.When transferring from intravenous administration to taking capsules and vice versa, there is no need to change the daily dose.
    The infusion solution is compatible with the following solvents: 20% glucose solution, Ringer's solution, Hartman's solution, potassium chloride solution in glucose, 4.2% bicarbonate sodium solution, aminofusin, isotonic sodium chloride solution.
    Infusions of fluconazole can be carried out using conventional transfusion kits using one of the liquids listed above.
    Application of v adults
    In cryptococcal infections, the usual dose of fluconazole is 400 mg once a day on the first day of treatment, later on - 200-400 mg once a day. The duration of treatment for cryptococcal infections depends on the clinical efficacy, confirmed by mycological examination; usually varies from 6 to 8 weeks.
    For the prevention of recurrence of cryptococcal meningitis in AIDS patients, after completion of the full course of primary therapy, fluconazole is prescribed to the patient in doses of at least 200 mg / day for a long period.
    With candidemia, disseminated candidiasis and other invasive, candidal infections, the daily dose is 400 mg on the first day and 200 mg on subsequent days.Depending on the clinical effectiveness of the drug, the dose can be increased to 400 mg / day. The duration of treatment depends on clinical effectiveness.
    With oropharyngeal candidiasis, including patients with impaired immunity, the usual dose is 50-100 mg once a day for 7-14 days. If necessary, the treatment can be prolonged, especially with severe immunity disorders.
    In other candidiasis infections, for example, with esophagitis, non-invasive bronchopulmonary infections, candiduria, candidiasis of the skin and mucous membranes, the usual daily dose is 50-100 mg for 14-30 days.
    For the prevention of fungal infections in patients with malignant neoplasms, the dose of fluconazole should be 50 mg once a day until the patient is at a high risk because of cytostatic therapy or radiation therapy.
    Use in children
    As with similar infections in adults, the duration of treatment depends on the clinical and mycological effect. In children, the drug should not be used in a daily dose exceeding that of adults. Fluconazole apply daily once a day.For the treatment of generalized candidiasis and cryptococcal infection, the recommended dose is 6-12 mg / kg / day, depending on the severity of the disease.
    For the prevention of fungal infections in patients with reduced immunity, the drug is prescribed at 3-12 mg / kg / day.
    In newborns fluconazole is deduced more slowly, therefore in the first 2 weeks of life the drug is prescribed in the same dose (in mg / kg) as in older children, but at an interval of 72 hours. Children at the age of 3 and 4 weeks of life are administered the same dose at intervals of 48 hours.
    Application of the elderly
    In the absence of impaired renal function, the usual dosage recommendations should be followed. For patients with impaired renal function (creatinine clearance <50 mL / min), the dosage regimen should be adjusted as indicated below.
    The use of v in patients with renal insufficiency
    Fluconazole is excreted mainly with urine in unchanged form. With a single admission dose changes are not required. In patients (including children) with impaired renal function, when taking the drug again, a "shock" dose of 50 mg to 400 mg should be initially administered. After the introduction of the "shock" dose, the daily dose (depending on the indication) is determined according to the following table:

    Creatinine clearance (ml / min)

    %, recommended dose

    >50

    <50 (without dialysis) Patients permanently on dialysis

    100% 50%

    100% after each dialysis

    Side effects:
    Headache, dizziness, change in taste, nausea, vomiting, diarrhea, flatulence, abdominal pain, impaired liver function (jaundice, increased activity of alkaline phosphatase and aminotransferases, hyperbilirubinemia, hepatocellular necrosis), incl. fatal, kidney failure, seizures, neutropenia, agranulocytosis, prolongation of Q-T interval, blinking / ventricular flutter, hypercholesterolemia, hypertriglyceridemia, hypokalemia, alopecia, Stevens-Johnson syndrome, toxic epidermal necrolysis, leukopenia, thrombocytopenia, skin rash, anaphylactoid reactions.

    Overdose:
    Symptoms: hallucinations, paranoid behavior.
    When an overdose of the drug may be sufficient symptomatic treatment (with the use of ancillary activities and gastric lavage, if necessary).
    Fluconazole is excreted mainly with urine; The forced diuresis, probably, can accelerate deducing of a preparation from an organism. After a three-hour hemodialysis, the concentration of fluconazole in the blood plasma is reduced by approximately 50%.

    Interaction:
    Anticoagulants: in patients receiving fluconazole and coumarin anticoagulants, careful monitoring of prothrombin time is necessary, as it may increase.
    Sulfonylurea preparations: fluconazole, with simultaneous administration, may prolong the half-life of oral preparations of sulfonylurea derivatives, therefore, when combined, the possibility of developing hypoglycemia should be considered.
    Phenytoin: simultaneous use of fluconazole and phenytoin may be accompanied by an increase in the concentration of phenytoin in a clinically significant degree, which requires a reduction in its dose.
    Rifampicin: with simultaneous administration of rifampicin and fluconazole, the maximum concentration and half-life of the latter decrease, therefore; if necessary combined use, the dose of fluconazole should be increased.
    Rifabutin: The combined use of fluconazole and rifabutin is accompanied by
    increased serum levels of the latter, it is possible to develop uveitis.
    Cyclosporine: when combined with fluconazole and cyclosporine, it is recommended to monitor the concentration of the latter in the blood, as it may increase.Terfenadine and astemizole: Given the occurrence of serious, life-threatening, arrhythmias in patients receiving azole antifungal drugs in combination with terfenadine or astemizole, their joint administration is contraindicated.
    Cisapride: with simultaneous administration of fluconazole and cisapride, cases of adverse cardiac reactions, including paroxysms of ventricular tachycardia, have been described. Simultaneous reception is contraindicated.
    Zidovudine: when. combined use may increase the concentration of zidovudine in blood plasma. Patients receiving this combination should be observed to identify side effects of zidovudine.
    Theophylline: administration of fluconazole leads to a decrease in the average rate of clearance of creatinine from the blood plasma, hence the risk of toxic theophylline and overdose increases.
    Although no specific manifestations of pharmaceutical incompatibility are described, mixing of fluconazole solution with solutions of other drugs before infusion is not recommended.
    When using fluconazole in patients who simultaneously receive other drugs metabolized by the cytochrome P450 system, care must be taken.Increases the concentration of midazolam - increased risk of psychomotor effects (more pronounced when fluconazole is administered orally than intravenously); tacrolimus - risk of nephrotoxicity.
    Hydrochlorothiazide increases the concentration of fluconazole in plasma by 40%.

    Special instructions:
    In rare cases, the use of fluconazole was accompanied by a toxic effect on the liver, including fatal, mainly in patients with serious concomitant diseases. It is necessary to monitor liver function. If there are signs of liver damage that may be associated with the use of fluconazole, the drug should be discontinued.
    Treatment should continue until the appearance of clinical-hematologic remission. Premature termination of treatment leads to relapse.
    In the course of treatment, it is necessary to monitor blood counts, kidney and liver function. If there are violations of kidney and liver function, stop taking the drug.
    On the background of taking Forcan®, patients had rare cases of development of exfoliative skin reactions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis.Patients with AIDS and malignant neoplasms are more likely to develop severe skin reactions with many drugs. If the patient develops a superficial fungal infection of the rash during treatment, which can be associated with the use of fluconazole, the drug should be discontinued. When rashes appear in patients with invasive / systemic fungal infections, they should be carefully monitored and canceled fluconazole with the appearance of bullous lesions or erythema multiforme.
    It is necessary to control the prothrombin index while using the coumarinic anticoagulants simultaneously.

    Effect on the ability to drive transp. cf. and fur:

    Form release / dosage:
    Solution for infusions 2 mg / ml.

    Packaging:
    Form of issue
    Solution for infusions 2 mg / ml.
    100 ml of the solution are hermetically packed in a bottle of translucent and colorless low density polyethylene (LDPE) using the "FFS" technology. On the outside of the vial, thermoformed convex lines (labels) are applied to scale the volume of the vial: one line labeled "100" for the horizontal position of the vial, and eight lines with intermediate designations: "20", "40", "60" and "80 "- For the bottle in an inverted state.On the outside at the base of the bottle, the production code of the bottle "001608" is printed. From the outside of the bottom of the vial
    there is a special loop for it; fastening when used. On the top of the bottle there is a cap-cap of low-density polyethylene "LDPE" of white j color. 1 bottle is packed in a polyethylene bag of transparent and colorless polypropylene "PP" with diagonal; printed on both sides with a repeating company logo. 1 bottle packed in a package, together with instructions for use, is placed in a cardboard box.

    Storage conditions:
    At a temperature not higher than 25 ° C. Do not allow freezing Keep out of the reach of children!

    Shelf life:
    3 years. The drug should not be used after the expiry date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013634 / 02
    Date of registration:24.03.2009
    The owner of the registration certificate:Cipla Ltd.Cipla Ltd. India
    Manufacturer: & nbsp
    Information update date: & nbsp15.10.2015
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