Active substanceFluconazoleFluconazole
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  • Dosage form: & nbspcapsules
    Composition:
    Composition:
    Capsule composition: 50 mg
    Active substance: fluconazole - 50 mg Excipients: lactose monohydrate - 138 mg, starch - 83.6 mg, sodium lauryl sulfate - 0.25 mg, talc - 5.5 mg, silicon dioxide colloid - 0.25 mg.
    Cover: dye indigocarmine 0.0224 mg, yellow quinoline dye 0.120 mg, titanium dioxide dye 0.151 mg, methyl parahydroxybenzoate 0.192 mg, propyl parahydroxybenzoate 0.048 mg water 3.48 mg sodium lauryl sulfate 0.0192 mg , gelatin (capsule base) - 19.9233 mg.
    Case: indigo carmine dye 0.0143 mg, yellow quinoline dye 0.0260 mg, titanium dioxide dye 0.7605 mg, methyl yaragroxybenzoate 0.3120 mg, propyl parahydroxybenzoate 0.0780 mg, water 5.655 mg, sodium lauryl sulfate, 0.0312 mg, gelatin (capsule base) - 32.1231 mg.
    Capsule composition: 150 mg
    Active substance: fluconazole - 150 mg Excipients: lactose monohydrate -112 mg, starch-99 mg, sodium lauryl sulfate - 0.40 mg, talc - 7.2 mg, silicon dioxide colloid -0.40 mg.
    Cover: dye brilliant blue - 0.2076 mg, dye crimson (Ponso 4R) - 0.2082 mg, dye sunset yellow - 0.0847 mg, methylparahydroxybenzoate - 0.232 mg, propyl parahydroxybenzoate 0.0580 mg, water 4.205 mg, sodium lauryl sulfate - 0.0232 mg, gelatin (capsule base) - 23.9813 mg.
    Body: dye sunset yellow - 0.6265 mg, titanium dioxide dye 0.6891 mg, methyl parahydroxybenzoate 0.3760 mg, propyl parahydroxybenzoate 0.0940 mg, water 6.815 mg, sodium lauryl sulfate 0.0376 mg, gelatin ( base capsule) - 38.3618 mg
    Capsule composition: 200 mg
    Active substance: fluconazole - 200 mg Excipients: lactose monohydrate - 178 mg, starch - 138.6 mg, sodium lauryl sulfate - 0.50 mg, talc - 10 mg, silicon dioxide colloid - 0.50 mg. Cover: dye diamond blue - 0.2649 mg, Crimson dye (Ponce 4R) - 0.2657 mg, dye sunset sunset yellow - 0.108 mg,
    methyl parahydroxybenzoate 0.296 mg, propyl parahydroxybenzoate 0.0740 mg, water: 5,365 mg, sodium lauryl sulfate - 0.0296 mg, gelatin (capsule base) - 30.5968 mg. Body: dye Azorubin 0.1364 mg, dye crimson (Ponso 4R) 0.2038 mg, titanium dye 0.6489 mg methyl parahydroxybenzoate 0.4720 mg, propyl parahydroxybenzoate 0.11180 mg, water 8.555 mg sodium lauryl sulfate - 0.0472 mg, gelatin (capsule base) - 48.7917 mg
    Description:
    Capsules of 50 mg - hard gelatin capsules in size "2" with a light green casing and a dark green lid. The contents of the capsule are from white to almost white amorphous powder.
    Capsules of 150 mg - hard gelatin capsules in size "1" with an orange casing and a black lid. The contents of the capsule are from white to almost white amorphous powder.
    Capsules of 200 mg - hard gelatin capsules in size "O" with a dark red body and a black lid. The contents of the capsule are from white to almost white amorphous powder.

    Pharmacotherapeutic group:Antifungal agent.
    ATX: & nbsp

    J.02.A.C   Triazole derivatives

    J.02.A.C.01   Fluconazole

    Pharmacodynamics:
    Fluconazole, a representative of the class of triazole antifungal agents, is a potent selective inhibitor of the synthesis of sig- roles in the fungal cell.
    The drug is effective in opportunistic fungal infections, incl.caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Also shown is the activity of fluconazole in endemic mycosis models, including infections caused by Blastomyces dermatitidis, Coccidiodes immitis and Histoplasma capsulatum.

    Pharmacokinetics:
    After oral administration fluconazole it is well absorbed, its bioavailability is 90%. The maximum concentration after ingestion, fasting 150 mg is 90% of the plasma content with internal administration at a dose of 2.5 - 3.5 mg / l. Simultaneous food intake does not affect the absorption of the drug taken internally. The concentration in the plasma reaches a peak 0.5-1.5 h after administration, the fluconazole half-life is about 30 h. The plasma concentrations are in direct proportion to the dose. 90% level of equilibrium concentration is reached by 4-5 days of treatment with the drug (with the administration of 1 time / day).
    The introduction of a shock dose (on the first day), which is 2 times higher than the usual daily dose, makes it possible to reach a level corresponding to 90% of the equilibrium concentration by the second day. The apparent volume of distribution approximates the total water content in the body. Binding to plasma proteins - 11-12%.
    Fluconazole well penetrates into all body fluids. Concentrations of the drug in saliva and sputum are similar to those in plasma.In patients with fungal meningitis, the content of fluconazole in the cerebrospinal fluid reaches 80% of its plasma level.
    In the stratum corneum of the epidermis, the dermis and the sweat fluid, high concentrations are reached, which exceed the serum levels.
    Fluconazole is excreted mainly by the kidneys; approximately 80% of the administered dose is excreted in the urine unchanged. The clearance of fluconazole is proportional to the creatinine clearance. Metabolites of fluconazole in peripheral blood were not detected.

    Indications:
    • cryptococcosis, including cryptococcal meningitis and other localizations of this infection (including lungs, skin), both in patients with normal immune response, and in patients with various forms of immunosuppression (including AIDS patients, organ transplantation ); the drug can be used as a supportive therapy for the prevention of cryptococcal infection in AIDS patients;
    • generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidiasis infections (peritoneal, endocardial, eye, respiratory and urinary tract infections). Treatment can be conducted in patients with malignant neoplasms, in patients with intensive care units,patients undergoing a course of cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis;
    • Candidiasis of mucous membranes, incl. oral cavity and pharynx, esophagus, non-invasive bronchopulmonary candidiasis, candiduria, candidiasis of skin and mucous membranes, as well as atrophic oral candidiasis associated with the wearing of dentures (treatment may be performed in patients with normal or decreased immunity function); prevention of recurrence of oropharyngeal candidiasis in AIDS patients;
    • genital candidiasis: vaginal Candidiasis (acute and chronic recurrent), prophylactic use to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes a year); Candidiasis balanitis;
    • prevention of fungal infections in patients with malignant neoplasms who are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy;
    • mycosis of the skin, including mycosis of the feet, the body, the groin area; pityriasis lichen; onychomycosis; candidiasis of the skin;
    • Deep endemic mycoses, including coccidiomycosis, paracoccidiomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.

    Contraindications:
    • simultaneous administration of cisapride, terfenadine, astemizole and other drugs that extend the QT interval.
    • hypersensitivity to the drug or a similar structure of azole compounds.
    • pregnancy, lactation period, children's age (up to 3 years) for this dosage form.

    Carefully:
    Hepatic insufficiency, the appearance of rash against the background of fluconazole in patients with superficial fungal infection. infection and invasive / systemic fungal infections, potentially pro-rhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte balance disorders, simultaneous use of medications that cause arrhythmias).

    Pregnancy and lactation:
    The use of the drug in pregnant women is not advisable, except for severe or life-threatening forms of fungal infections, if the expected effect exceeds the possible risk to the fetus.
    Fluconazole is found in breast milk in the same concentration as in plasma, so its use during lactation is not recommended.

    Dosing and Administration:
    Inside.
    In cryptococcal meningitis and cryptococcal infections of other locations, 400 mg are usually prescribed on the first day, and then continue treatment at a dose of 200-400 mg once / day.Duration. treatment for cryptococcal infections depends on the clinical efficacy, confirmed by mycological examination; in cryptococcal meningitis, it usually lasts at least 6-8 weeks. To prevent the recurrence of cryptococcal meningitis in AIDS patients, after completing the full course of primary treatment, fluconazole prescribe at a dose of 200 mg / day for a long period of time.
    With candidemia, disseminated candidiasis and other invasive candidiasis infections, the dose is usually 400 mg on the first day, and then on 200 mg. With insufficient clinical effectiveness, the dose of the drug can be increased to 400 mg / day. The duration of therapy depends on clinical effectiveness.
    With oropharyngeal candidiasis, the drug is usually prescribed at 50-100 mg 1 time / day; the duration of treatment is 7-14 days. If necessary, in patients with marked, decreased immunity, treatment may be longer.
    With atrophic candidiasis of the oral cavity, associated with the wearing of dentures, fluconazole usually prescribed 50 mg 1 time / day for 14 days in combination with local antiseptic agents for prosthesis treatment.
    For other candidiasis localizations (with the exception of genital candidiasis), for example, with esophagitis, non-invasive bronchopulmonary disease, candiduria, candidiasis of the skin and mucous membranes, etc., the effective dose is usually 50-100 mg / day with a treatment duration of 14-30 days . To prevent the recurrence of oropharyngeal candidiasis in AIDS patients after completing the full course of primary therapy, the drug can be prescribed 150 mg once a week.
    With vaginal candidiasis fluconazole taken once inside the dose of 150 mg. To reduce the frequency of recurrences of vaginal candidiasis, the drug can be used at a dose of 150 mg once a month. The duration of therapy is determined individually; it varies from 4 to 12 months. Some patients may need more frequent use.
    With balanitis caused by Candida, fluconazole appoint a single dose of 150 mg orally.
    For the prevention of candidiasis, the recommended dose of fluconazole is 50-400 mg 1 time / day, depending on the degree of risk of fungal infection. If there is a high risk of generalized infection, for example, in patients with expected severe or persistent neutropenia, the recommended dose is 400 mg 1 time / day. Fluconazole appoint a few days before the expected appearance of neutropenia; after increasing the number of neutrophils more than 1000 / mm 3, treatment is continued for another 7 days.
    With mycosis of the skin, including mycosis of the feet, skin of the inguinal area, and candidiasis: from the skin, the recommended dose is 150 mg once a week or 50 mg 1 time / day. The duration of therapy in usual cases is 2-4 weeks, however, with foot mycoses may require longer therapy (up to 6 weeks).
    With pityriasis, the recommended dose is 300 mg once a week for 2 weeks. Some patients require a third dose of 300 mg per week, while in some cases it is sufficient to receive 300-400 mg once daily. An alternative treatment regimen is the use of the drug at 50 mg once a day for 2-4 weeks.
    With onychomycosis, the recommended dose is 150 mg once a week. Treatment should continue until the replacement of the infected nail (growth of uninfected nail). For the repeated growth of nails on the fingers and toes normally it takes 3-6 months and 6-12 months, respectively.
    With deep endemic mycoses, it may be necessary to use the drug at a dose of 200-400 mg / day for up to 2 years.The duration of therapy is determined individually; it can be 11-24 months with coccidiomycosis; 2-17 months with paracoccidiomycosis; 1-16 months with sporotrichosis and 3-17 months with histoplasmosis.
    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 that would exceed that of adults. The drug is used daily 1 time / day.
    In mucosal candidiasis, the recommended dose of fluconazole is 3 mg / kg / day. The first day can be: a shock dose of 6 mg / kg is prescribed in order to achieve a more rapid equilibrium equilibrium concentration.
    For treatment of generalized candidiasis or 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 children with reduced immunity, where the risk of infection is associated with neutropenia, resulting from cytotoxic chemotherapy or radiation therapy, the drug is prescribed at 3-12 mg / kg / day, depending on the severity and duration of preservation of induced neutropenia.
    In children with impaired renal function, the daily dose of the drug should be reduced (in the same proportional relationship as in adults), according to the degree of renal insufficiency.
    In elderly patients in the absence of violations of kidney function should follow the usual dosage regimen. Patients with renal insufficiency (creatinine clearance less than 50 ml / min) dosage regimen should be adjusted as indicated below.
    Use of the drug in patients with impaired renal function.
    Fluconazole is excreted mainly with urine in unchanged form. With a single admission, a dose change is not required. When re-administering the drug, patients with impaired renal function should first introduce a shock dose of 50 mg to 400 mg. If the creatinine clearance (CK) is more than 50 ml / min, the usual dose of the drug (100% of the recommended dose) is used. With SC from 11 to 50 ml / min, a dose equal to 50% of the recommended dose is applied. Patients regularly on dialysis, one dose of the drug is used after each session of hemodialysis.
    Side effects:
    From the side of the digestive system: a change in taste, nausea, vomiting, diarrhea,flatulence, abdominal pain, rarely - a violation of liver function (hyperbilirubinemia, increased activity of alanine aminotransferases, aspartate aminotransferases, increased activity of alkaline phosphatase).
    From the nervous system: headache, rarely - convulsions, dizziness.
    On the part of the organs of hematopoiesis: rarely - leukopenia, thrombocytopenia, neutropenia, agranulocytosis.
    On the part of the cardiovascular system: an increase in the duration of the Q-T interval, fibrillation / flutter of the ventricles.
    Allergic reactions: skin rash, rarely - malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions.
    Other: rarely - a violation of kidney function. Alopecia, hypercholesterolemia, hypertriglyceridemia, hypokalemia.

    Overdose:
    Symptoms: hallucinations, paranoid behavior.
    Treatment: symptomatic, gastric lavage, forced diuresis. Hemodialysis for 3 hours; reduces the plasma concentration by approximately 50%.

    Interaction:
    With the use of fluconazole with warfarin, prothrombin time increases (on average by 12%).In this regard, it is recommended to carefully monitor the prothrombin time in patients receiving the drug in combination with coumarinic-anticoagulants.
    Fluconazole increases the plasma half-life of oral hypoglycemic agents - sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide, tolbugamid) in healthy people. The combined use of fluconazole and oral hypoglycemic agents in diabetic patients is permissible, but the doctor should keep in mind the possibility of developing hypoglycemia. The simultaneous use of fluconazole and phenytoin can lead to an increase in the concentration of phenytoin in the plasma to a clinically significant degree. Therefore, when it is necessary to jointly use these drugs, it is necessary to monitor the concentrations of phenytoin with correction of its dose in order to maintain the drug level within the therapeutic interval.
    The combination with rifampicin leads to a 25% reduction in AUC and a 20% decrease in the half-life of fluconazole from the plasma. Therefore, patients receiving concomitantly rifampicin, it is advisable to increase the dose of fluconazole.
    It is recommended to monitor the concentration of cyclosporine in the blood in patients receiving fluconazole, since with the use of fluconazole and cyclosporine in patients with kidney transplant, the administration of fluconazole at a dose of 200 mg / day leads to a slow increase in the concentration of cyclosporine in the plasma.
    Patients who receive high doses of theophylline or who are likely to develop theophylline intoxication,. should be monitored for the early detection of symptoms of a theophylline overdose, as taking fluconazole leads to a decrease in the average clearance rate of theophylline from the plasma.
    With the simultaneous use of fluconazole and cisapride, cases of unwanted reactions from the heart, including paroxysms of ventricular tachycardia (torsades de points), are described.
    There have been reports of an interaction between fluconazole and rifabutin, accompanied by an increase in serum levels of the latter. With the simultaneous use of fluconazole and rifabutin, cases of uveitis are described. It is necessary to carefully observe patients who simultaneously receive rifabutin and fluconazole.
    In patients,who receive a combination of fluconazole and zidovudine, an increase in the concentration of zidovudine is observed, which is caused by a decrease in the conversion of the latter into its main metabolite, so you should expect an increase in the side effects of zidovudine.
    Special instructions:
    In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, incl. with a lethal outcome, mainly in patients with serious concomitant diseases. In the case of hepatotoxic effects associated with fluconazole, there was no apparent dependence on the total daily dose, duration. therapy, sex and age of the patient. The hepatotoxic effect of fluconazole was usually reversible; signs of it disappeared after discontinuation of therapy. If there are clinical signs of liver damage that may be associated with fluconazole, the drug should be discontinued.
    Patients with AIDS are more likely to develop severe skin reactions with many drugs. In those cases when a rash develops in patients with superficial fungal infection and it is regarded as definitely associated with fluconazole, the drug should be discontinued.When rashes appear in patients with invasive / systemic fungal infections, they should be carefully monitored and canceled fluconazole when there are bullous changes or erythema multiforme. Caution should be exercised while taking fluconazole with rifabutin, tacrolimus, or other drugs metabolized by the cytochrome P450 system.

    Form release / dosage:Capsules 50 mg, 150 mg, 200 mg.
    Packaging:
    Capsules 50 mg:
    4 capsules in a strip from AL / AL. 1 strip with instructions for use in a cardboard box. 5 cardboard packs in a cardboard box.
    Capsules 150 mg:
    1 capsule in a strip from AL / AL. 1, 2 or 3 strips together with instructions for use in a cardboard bundle. 5 cardboard packs in a cardboard box.
    Capsules 200 mg:
    4 capsules in a strip from AL / AL. 1 strip with instructions for use in a cardboard box. 5 cardboard boxes in a cardboard box.

    Storage conditions:
    At a temperature of no higher than 25 ° C.
    Keep out of the reach of children.

    Shelf life:
    3 years.
    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:Without recipe
    Registration number:П N013634 / 01
    Date of registration:16.10.2008
    The owner of the registration certificate:Cipla Ltd.Cipla Ltd. India
    Manufacturer: & nbsp
    Cipla Ltd India
    Information update date: & nbsp16.10.2015
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