Active substanceFluconazoleFluconazole
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  • Dosage form: & nbspcapsules
    Composition:
    50 mg: Active substance: fluconazole 50 mg; Excipients: lactose monohydrate, talc, silicon dioxide colloid, sodium carboxymethyl starch; Composition of the empty capsule: water, methyl parahydroxybenzoate (methylparaben), propyl parahydroxybenzoate (propylparaben), gelatin, sodium lauryl sulfate; dyes: carmoizine (azorubin), brilliant blue, quinoline yellow, titanium dioxide.
    100 mg: Active substance: fluconazole 100 mg; Excipients: lactose monohydrate, talc, silicon dioxide colloid, sodium carboxymethyl starch; Composition of an empty capsule: water, gelatin, sodium lauryl sulfate, bronopol, povidone; dyes: brilliant blue, quinoline yellow, titanium dioxide, sunset yellow.
    150 mg: Active substance: fluconazole 150 mg; Excipients: lactose monohydrate, talc, silicon dioxide colloid, sodium carboxymethyl starch, magnesium stearate; Composition of the empty capsule: water, methyl parahydroxybenzoate (methylparaben), propyl-parahydroxybenzoate (propylparaben), gelatin, sodium lauryl sulfate; dyes: brilliant blue, titanium dioxide.
    200 mg: Active substance: fluconazole 200 mg; Excipients: lactose monohydrate, talc, silicon dioxide colloid, sodium carboxymethyl starch; Composition of the empty capsule: water, methyl parahydroxybenzoate (methylparaben), propyl parahydroxybenzoate (propylparaben), gelatin, sodium lauryl sulfate; dyes: brilliant blue, crimson [Ponso 4R], sunset yellow sun, titanium dioxide, floxin B.

    Description:
    Capsules 50 mg: Hard gelatin capsules No. 2 with a gray lid and a white body, with the inscription "SYSCAN 50" and a monogram of the logo (square emblem) on the capsule shell. The contents of the capsules are white or almost white powder.
    Capsules 100 mg: Hard gelatin capsules No. 2 with a green lid and a white body, with the inscription "SYSCAN 100" and a monogram of the logo (square emblem) on the capsule shell. The contents of the capsules are white or almost white powder.
    Capsules 150 mg:. Hard gelatin capsules No. 0 with a blue lid and a white body with the inscription "SYSCAN 150" and a monogram of the logo (square emblem) on the shell of the capsule. The contents of the capsules are white or almost white powder.
    Capsules 200 mg: Hard gelatin capsules No. 0 with a black lid and orange casing, with the inscription "SYSCAN 200" and a monogram of the logo (square emblem) on the shell of the capsule. The contents of the capsules are white or almost white powder.

    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 potent selective inhibitor of the fungal enzyme 14-a-demethylase.The drug prevents the transition of lanosterol to ergosterol, the main component of cell membranes of fungi.
    The drug is effective in opportunistic mycoses, including those caused by Candida spp. (Candida albicans, Candida tropicalis), Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Also shown is the activity of fluconazole on models of endemic mycoses, including infections caused by Blastomyces dermatidis, Coccidioides immitis and Histoplasma capsulatum. However, Blastomyces dermatidis, Coccidioides immitis and Histoplasma capsulatum to fluconazole are less sensitive than to other azoles.

    Pharmacokinetics:
    After oral administration fluconazole well absorbed, its bio availability is 90%. The maximum concentration (Cmax) after ingestion, fasting 150 mg of the drug is 90% of the concentration in the plasma with intravenous 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 maximum after 0.5-1.5 h (TCam) after administration. The concentration in the plasma is in direct proportion to the dose. 90% level of equilibrium concentration is achieved by 4-5 days of treatment with the drug (once taken once a day). The use of a dose on the first day, which is 2 times greater than the usual daily dose, makes it possible to achieve a plasma concentration of fluconazole equal to 90% of the equilibrium concentration value by the second day.The apparent volume of distribution approximates the total volume of water in the body. Binding to plasma proteins is low-11-12%.
    Fluconazole well penetrates into all body fluids, including cerebrospinal fluid. The concentration of the drug in saliva and sputum is similar to that in plasma. In patients with fungal meningitis, the fluconazole content in the cerebrospinal fluid reaches 80% of its plasma value.
    In the stratum corneum, epidermis, dermis and fluids, high concentrations are reached that exceed serum levels.
    Less than 5% of fluconazole is metabolized on first passage through the liver. The half-life (T1 / 2) of fluconazole is about 30 hours. Prolonged IVg allows the use of a single dose of the drug for the treatment of vaginal candidiasis and ensures the drug is taken once a day for other indications. Fluconazole is excreted mainly by the kidneys; approximately 80% of the administered dose is excreted by the kidneys 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 those with AIDS, organ transplantation ); the drug can be used to prevent 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 performed in patients with malignant neoplasms, in intensive care units, in patients undergoing cytostatic or immunosuppressive therapy, and in the presence of other factors predisposing to the development of candidiasis;
    • Candidiasis of mucous membranes, incl. oral cavity and pharynx (including atrophic candidiasis of the oral cavity, associated with the wearing of dentures), esophagus, non-invasive bronchopulmonary candidiasis, candiduria, candidiasis of the skin; prevention of recurrence of oropharyngeal candidiasis in AIDS patients;
    • genital candidiasis: vaginal candidiasis (acute and chronic recurrent), preventive use to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes a year); candidiasis balanitis, the 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;
    • mycosis of the skin, including mycosis of the feet, trunk, inguinal region; pityriasis lichen, onychomycosis; candidiasis of the skin;
    • Deep endemic mycoses, including coccidiomycosis and histoplasmosis in patients with normal immunity.

    Contraindications:
    Hypersensitivity to fluconazole, other components of the drug or to other azole compounds; simultaneous reception of terfenadine (against the background of a constant intake of fluconazole at a dose of 400 mg per day or more), cisapride or astemizole and other drugs that extend the QT interval and increase the risk of severe rhythm disturbances; lactose intolerance; deficiency of lactase; glucose-galactose malabsorption; lactation period; Children under 3 years old (for this dosage form).

    Carefully:
    Precautions: hepatic and / or renal failure, occurrence of rash on the background of fluconazole in patients with superficial fungal infection and invazivny- E / systemic fungal infections, simultaneous terfenadine and fluconazole less than 400 mg per day, potentially proaritmogennoe status in patients with multiple risk factors (organic heart diseases, electrolyte balance disorders, simultaneous intake of drugs that cause arrhythmias), pregnancy; patients with intolerance to acetylsalicylic acid, pregnancy.

    Pregnancy and lactation:
    The use of the drug in pregnant women is inappropriate, except for severe or life-threatening forms of fungal infections, if the expected effect for the mother 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. The daily dose depends on the nature and severity of the fungal infection.
    Adults with cryptococcal meningitis and cryptococcal infections at other sites on the first day is usually administered 400 mg and the treatment is then continued at a dose of 200 mg 1 time per day.Depending on the answer, the dose can be increased to 400 mg once a day. The duration of treatment for cryptococcal infections depends on the clinical efficacy, confirmed by mycological examination. The recommended duration of treatment for the initial treatment of cryptococcal meningitis is 10-12 weeks after a negative result of a microbiological study of a sample of cerebrospinal fluid.
    To prevent the recurrence of cryptococcal meningitis in AIDS patients, after completion of the full course of primary therapy, fluconazole prescribe a dose of 200 mg per day for a long period of time.
    When candidemia, disseminated candidiasis and other invasive candidiasis infections in the first day, the dose is usually 400 mg, and then - 200 mg per day. With insufficient clinical efficacy, the dose of the drug can be increased to 400 mg per day; with severe systemic candidiasis - it is possible to increase the dose to 800 mg per day. The duration of therapy depends on clinical effectiveness; treatment should be continued at least 2 weeks after receiving negative blood cultures or after the disappearance of the symptoms of the disease.
    With oropharyngeal candidiasis, the drug is usually prescribed 50-100 mg once a day; the duration of treatment is 7-14 days. If necessary, in patients with a marked decrease in immunity, treatment may be longer (3 weeks).
    In atrophic candidiasis of the oral cavity associated with the wearing of dentures, fluconazole is usually prescribed 50 mg once a day for 14 days in combination with antiseptic agents for prosthesis treatment.
    With other localizations of candidiasis (with the exception of genital candidiasis), for example, with esophagitis, noninvasive bronchopulmonary disease, candiduria, candidiasis of the skin and mucous membranes, etc., the effective dose is usually 50-100 mg per day with a treatment duration of 14-30 days; with severe candidiasis of the mucous membranes - 100-200 mg per day. 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, Ciskan® is taken once inside at a 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 spp., Ciskan® is administered orally once a day at a dose of 150 mg per day.
    For the prevention of candidiasis, the recommended dose is 50-400 mg once a 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 once daily. Ciskan® is prescribed a few days before the expected appearance of neutropenia; after increasing the number of neutrophils more than 1000 / mm3 treatment is continued for another 7 days.
    . With skin mycoses (including candidiasis), including mycosis of the feet, skin of the inguinal area, the recommended dose is 150 mg once a week or 50 mg once a day. Duration of therapy in usual cases is 2-4 weeks, however, with foot mycoses, longer therapy (up to 6 weeks) may be required.
    With pityriasis 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; an alternative treatment regimen is to administer 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). To re-grow the nails on the fingers and toes, it normally 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 to 400 mg per day for up to 2 years. The duration of therapy is determined individually; it can be 11-24 months with coccidioidosis 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 per day.
    In candidiasis of mucous membranes, the recommended dose of fluconazole is 3 mg / kg per day. On the first day, a shock dose of 6 mg / kg can be administered to achieve equilibrium concentrations more quickly.
    For treatment of generalized candidiasis or cryptococcal infection, the recommended dose is 6-12 mg / kg per 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 per day, depending on the severity and duration of preservation of induced neutropenia. The maximum daily dose for children is 12 mg / kg.
    Dosing for patients with renal insufficiency
    Fluconazole is excreted mainly by the kidneys in unchanged form. With a single admission, a dose change is not required.
    Adult patients with impaired renal function with a repeated prescription of the drug should first be prescribed 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 or a usual dose of 1 every 2 days is applied. Patients regularly on dialysis, a single dose of the drug is used after each session of hemodialysis.
    Children with impaired renal function the daily dose should be reduced (in the same proportion as in adults), in accordance with the severity of renal failure.
    In elderly patients in the absence of violations of kidney function should follow the usual dosage regimen.

    Side effects:
    From the digestive system, loss of appetite, change in taste, nausea, vomiting, diarrhea, flatulence, abdominal pain, rarely - increased activity of "liver" enzymes, and liver dysfunction (jaundice, hyperbilirubinemia, increased alanine aminotransferase activity (ALT), aspartate aminotransferase (ACT) and alkaline phosphatase (APF), hepatitis, hepatocellular necrosis), incl. with a lethal outcome.
    From the nervous system: headache, dizziness, rarely - convulsions.
    On the part of the organs of hematopoiesis: rarely - agranulocytosis, neutropenia. Patients with severe fungal infections may have hematologic changes (leukopenia and thrombocytopenia).
    From the cardiovascular system: an increase in the duration of the QT interval on an electrocardiogram (ECG), flicker / flutter of the ventricles.
    Allergic reactions: skin rash, multiforme exudative erythema (incl.Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), bronchial asthma (more often with acetylsalicylic acid intolerance), anaphylactoid reactions (including angioedema, face swelling, urticaria, skin itching).
    Other: rarely - renal dysfunction, alopecia, hypercholesterolemia, hypertriglyceridemia, hypokalemia.

    Overdose:
    Symptoms: nausea, vomiting, diarrhea, in severe cases, convulsions, hallucinations, paranoid behavior may occur.
    Treatment: symptomatic, gastric lavage; t. to. fluconazole excreted by the kidneys it is recommended forced diuresis. Hemodialysis within 3 hours reduces the concentration in the plasma by 2 times.

    Interaction:
    One-time administration of fluconazole in the treatment of vaginal candidiasis is not accompanied by significant interactions.
    When several or more doses of the drug are used simultaneously with other drugs, the following drug interactions are possible:
    The interaction of fluconazole with terfenadine, cisapride and astemizole can lead to an increase in the concentration of these drugs in the plasma, which in turn can cause prolongation of the QT interval and lead to serious disturbances of the heart rhythm.Fluconazole inhibits the enzymes of the P450 system in the liver, thereby reducing the metabolism of terfenadine, cisapride and astemizole. The simultaneous administration of fluconazole and these drugs is contraindicated.
    With the combined use of warfarin and fluconazole, lengthening of prothrombin time is noted. In this regard, it is necessary to monitor prothrombin time in patients simultaneously receiving fluconazole and indirect anticoagulants of the coumarin series. Fluconazole prolongs T'A of oral hypoglycemic drugs (derivatives of sulfo-
    nylurea). Patients with diabetes mellitus can simultaneously be prescribed fluconazole and derivatives of sulfonylureas, however, it is necessary to take into account the possible risk of developing hypoglycemia.
    It is necessary to take into account that with repeated simultaneous use of hydrochlorothiazide and fluconazole, the concentration of fluconazole in the plasma is increased.
    Rifampicin accelerates the metabolism of fluconazole. It is necessary to increase the dose of fluconazole accordingly during their simultaneous use.
    In patients who underwent renal transplantation, fluconazole can increase the concentration of cyclosporine in plasma. In this regard, it is recommended to monitor the concentration of cyclosporine in patients simultaneously receiving ciclosporin and fluconazole.
    Fluconazole increases the concentration of theophylline in plasma. In this regard, it is recommended to monitor the concentration of theophylline in patients simultaneously receiving theophylline and fluconazole.
    Fluconazole may increase plasma concentrations of indinavir and midazolam. With the simultaneous use of these drugs with fluconazole, their dose should be appropriately reduced.
    Clinical studies have shown that as a result of slowing the metabolism of zidovudine, its plasma concentration can be increased with simultaneous application with fluconazole. It is necessary to monitor patients who are simultaneously receiving both of these drugs, since in this case, the incidence of side effects of zidovudine may increase.
    Strengthens the pharmacological effects of rifabutin (with simultaneous application described cases of uveitis) and phenytoin in a clinically significant degree (with combined use requires monitoring the concentration of phenytoin in the plasma). Fluconazole increases serum concentrations of phenytoin. At simultaneous application it is necessary to control doses of phenytoin and accordingly to correct them.
    Increases the concentration of tacrolimus - the risk of nephrotoxicity.
    Doctors should take into account that interaction with other drugs has not been specifically studied, but it is possible.

    Special instructions:
    Treatment can be started in the absence of seeding results or other laboratory tests, but if appropriate, a correction of fungicidal therapy is recommended. Because the fluconazole is excreted mainly by the kidneys, caution should be exercised in patients with renal insufficiency. With long-term treatment with fluconazole, dosing should be performed taking into account the CK.
    Caution should be exercised when administering fluconazole to patients with impaired liver function. During treatment, it is necessary to regularly monitor the activity of "liver" enzymes and monitor the patient in order to identify possible toxic effects. When the activity of "liver" enzymes is increased, the doctor must weigh the benefits of the therapy and the risk of developing severe liver damage.The hepatotoxic effect of fluconazole is usually reversible: symptoms disappear after discontinuation of therapy.
    Patients with AIDS are more likely to develop severe skin reactions with many drugs. In those cases where the 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.
    It is necessary to monitor prothrombin time in patients simultaneously receiving fluconazole and indirect anticoagulants of the coumarin series.
    Treatment should continue until the appearance of clinical and microbiological remission. Premature termination of treatment leads to relapse.
    The azorubin dye (dosage 50 mg), which is part of the drug, can cause an allergic reaction, including bronchial asthma. Allergic reactions are more common in patients with intolerance to acetylsalicylic acid.

    Effect on the ability to drive transp. cf. and fur:
    the experience with fluconazole indicates that a disruption to the ability to drive and drive machinery associated with the use of the drug is unlikely.
    However, given that the drug may cause dizziness and convulsions, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions
    Form release / dosage:
    Capsules 50 mg, 100 mg, 150 mg and 200 mg:

    Packaging:
    Dosage 50 mg, 100 mg: 7 capsules in a blister of PVC film and aluminum foil. 1 blister together with instructions for use packed in a cardboard box.
    Dosage of 150 mg: 1 capsule in an aluminum foil strip. 1 strip along with instructions for use packed in a cardboard box.
    Dosage 200 mg: 4 capsules in a blister of PVC film and aluminum foil. 2 blisters together with instructions for use packed in a cardboard box.

    Storage conditions:
    At a temperature not higher than 30 ° C. Keep out of the reach of children.

    Shelf life:
    3 years.
    Do not use after expiry date.

    Terms of leave from pharmacies:Without recipe
    Registration number:П N013944 / 01
    Date of registration:06.05.2008
    The owner of the registration certificate:Torrent Pharmaceuticals Co., Ltd.Torrent Pharmaceuticals Co., Ltd. India
    Manufacturer: & nbsp
    Information update date: & nbsp18.10.2015
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