Active substanceFluconazoleFluconazole
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  • Dosage form: & nbspcapsules
    Composition:
    1 capsule contains:
    Active substance: fluconazole 50 mg and 150 mg.
    Auxiliary substances: corn starch (C * Pharm. 03406), silicon dioxide colloid (aerosil), magnesium stearate, microcrystalline cellulose;
    Structure of the capsule of hard gelatin №3 \ titanium dioxide, dye quinoline yellow, dye sunset yellow, gelatin;
    Structure of the capsule of hard gelatin №0 \ titanium Dioxide, indigocarmine, iron oxide, yellow oxide, gelatin.

    Description:
    Dosage 50 mg:
    hard gelatin capsules number 3, body - yellow, cap - yellow, contents of capsules - a mixture of granules and powder white or almost white. Presence of lumps is allowed.
    Dosage of 150 mg:
    hard gelatin capsules № 0, body - blue, cap - blue, contents of capsules - a mixture of granules and powder of white or almost white color. Presence of lumps is allowed.

    Pharmacotherapeutic group:Antifungal agent.
    ATX: & nbsp

    J.02.A.C   Triazole derivatives

    J.02.A.C.01   Fluconazole

    Pharmacodynamics:
    Antifungal agent, has a highly specific effect, inhibiting the activity of enzymes of fungi, dependent on cytochrome P450. It blocks the conversion of lanosterol of fungal cells to ergosterol; increases the permeability of the cell membrane, disrupts its growth and replication.
    Fluconazole, being highly selective for cytochrome P450 fungi, practically does not inhibit these enzymes in the human body (in comparison with itraconazole, clotrimazole, econazole and ketoconazole less inhibits oxidative processes dependent on cytochrome P450 in human liver microsomes).Does not have antiadrogenic activity.
    It is active in opportunistic mycoses, including those caused by Candida spp. (including generalized forms of candidiasis on the background of immunodepression), Cryptococcus neoformans and Coccidioides immitis (including meningitis and encephalitis), Microsporum spp. and
    Trichophyton spp; with endemic mycoses caused by Blastomyces dermatidis, Histoplasma capsulatum (including immunosuppression).

    Pharmacokinetics:
    After oral administration fluconazole well absorbed, food intake does not affect the rate of absorption fluconazole a, its bioavailability is 90%.
    Time of maximum concentration after ingestion, fasting 150 mg of the drug
    0.5-1.5 hours and is 90% of the concentration in the plasma with intravenous administration at a dose of 2.5-3.5 mg / l. The half-life of fluconazole is 30 hours. The connection with plasma proteins
    11-12%. The concentration in the plasma is 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 greater than the usual daily dose, allows one to reach a concentration level corresponding to 90% of the equilibrium concentration by the second day.
    Fluconazole well penetrates into all body fluids.The concentration of the active substance in breast milk, articular fluid, saliva, sputum and peritoneal fluid is similar to that in blood plasma. Constant values ​​in the vaginal secretion are reached 8 hours after ingestion and are held at this level for at least 24 hours. Fluconazole well penetrates into the cerebrospinal fluid (CSF), with fungal meningitis, the concentration in the CSF is about 85% of its plasma level. In the fluid, epidermis and stratum corneum (selective accumulation), concentrations exceeding serum levels are achieved. After ingestion of 150 mg on day 7, the concentration in the stratum corneum is 23.4 μg / g, and 1 week after the second dose, 7.1 μg / g; concentration in the nails after 4 months of application at a dose of 150 mg once a week - 4.05 μg / g in healthy and 1.8 μg / g in the affected nails. The volume of distribution approximates the total water content in the body.
    It is an inhibitor of the isoenzyme CYP2C9 in the liver. It is excreted mainly by the kidneys (80% - unchanged, 11% - in the form of metabolites). The clearance of fluconazole is proportional to the creatinine clearance. Metabolites of fluconazole in peripheral blood were not detected.
    The pharmacokinetics of fluconazole significantly depend on the functional state of the kidneys, and there is an inverse relationship between the half-life and the clearance of creatinine. After hemodialysis for 3 hours the concentration of fluconazole in plasma is reduced by 50%.

    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 maternity (including those with AIDS, during transplantation bodies); the drug can be used to prevent cryptococcal infection in AIDS patients;
    -generative 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;
    -candidosis of mucous membranes, incl. oral cavity and pharynx (incl.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;
    -prophylaxis of fungal infections in patients with malignant neoplasms that are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy;
    - mikozy skin, including mycosis of the feet, body, inguinal area; pityriasis (multicolored) lichen, onychomycosis; candidiasis of the skin;
    - Deep endemic mycoses, including coccidiomycosis and histoplasmosis, in patients with normal immunity.

    Contraindications:
    -hypersensitivity to the drug (including other azole antifungal drugs in history),
    - simultaneous reception of terfenadine (against the background of a constant intake of fluconazole at a dose of 400 mg / day or more) or astemizole, as well as other drugs that extend the QT interval,
    We are looking forward to seeing you in 4-lane.

    E-mail:
    : пÐμÑ ‡ ÐμÐ½Ð¾Ñ ‡ нР° Ñ Ð¸ / иР»Ð¸ Ð¿Ð¾Ñ ‡ ÐμÑ ‡ нР° Ñ Ð½ÐμÐ'Ð¾Ñ Ñ,Ð ° Ñ,Ð¾Ñ ‡ Ð½Ð¾Ñ Ñ,ÑŒ, Ð¿Ð¾Ñ Ð²Ð» ÐμнР¸Ðμ Ñ Ñ <пи нР° Ñ "онÐμ Ð¿Ñ € имÐμнÐμÐ½Ð¸Ñ Ñ" Ð »ÑƒÐºÐ¾Ð½Ð ° Ð · ол Ð ° у пР° Ñ † иÐμнÑ,ов Ñ Ð¿ We would like to inform you that we are pleased to offer our customers a full range of products and services. ¸Ð ± ÐºÐ¾Ð²Ñ <ми Ð¸Ð½Ñ "ÐμÐºÑ † Ð¸Ñ Ð¼Ð¸, оÐ'Ð½Ð¾Ð²Ñ € ÐμмÐμÐ½Ð½Ñ <й Ð¿Ñ € иÐμм поÑ,ÐμÐ½Ñ † иР° л ьно гÐμпР° Ñ,оÑ,Ð¾ÐºÑ Ð¸Ñ ‡ Ð½Ñ <Ñ ... Ð »ÐμкР° Ñ € Ñ Ñ,вÐμÐ½Ð½Ñ <Ñ ... Ñ Ñ € ÐμÐ'Ñ Ñ,в, поÑ,ÐμÐ½Ñ † иР° Ð »Sewing and dyeing of sour cream ° кÑ,Ð¾Ñ € Ð ° ми Ñ € Ð¸Ñ ÐºÐ ° (Ð¾Ñ € гР° Ð½Ð¸Ñ ‡ ÐμÑ ÐºÐ¸Ðμ Ð · Ð ° Ð ± оР»ÐμвР° Ð½Ð¸Ñ Ñ ÐμÑ € Ð'Ñ † Ð °, нР° Ñ € уÑÐμÐ½Ð¸Ñ Ñ Ð »ÐμкÑ,Ñ € ол иÑ,ного Ð ± Ð ° Ð »Ð ° Ð½Ñ Ð °, оÐ'Ð½Ð¾Ð²Ñ € ÐμмÐμÐ½Ð½Ñ <й Ð¿Ñ € иÐμм Ð »ÐμкР° Ñ € Ñ Ñ,вÐμÐ½Ð½Ñ <Ñ ... Ñ Ñ € ÐμÐ'Ñ Ñ,в, Ð²Ñ <Ð · Ñ <вР° ÑŽÑ ‰ Ð¸Ñ ... Ð ° Ñ € иÑ,мии), Read more.

    Call of Duty:

    ÐŸÑ € имÐμнÐμниÐμ Ð¿Ñ € ÐμпР° Ñ € Ð ° Ñ,Ð ° у Ð ± ÐμÑ € ÐμмÐμÐ½Ð½Ñ <Ñ ... - нÐμ Ñ † ÐμÐ »ÐμÑ Ð¾Ð¾Ð ± Ñ € Ð ° Ð · но, Ð · Ð ° Ð¸Ñ ÐºÐ »ÑŽÑ ‡ ÐμниÐμм Ñ,Ñ Ð¶Ðμл Ñ <Ñ ... иР»Ð¸ ÑƒÐ³Ñ € ожР° ÑŽÑ ‰ Ð¸Ñ ... жиР· ни Ñ ​​"Ð¾Ñ € м Ð³Ñ € иР± ÐºÐ¾Ð²Ñ <Ñ ... инÑ" ÐμÐºÑ † ий, когÐ'Ð ° поÑ,ÐμÐ½Ñ † иР° Ð »ÑŒÐ½Ð ° Ñ Ð¿Ð¾Ð» ьР· Ð ° оÑ, Ñ € имÐμнÐμÐ½Ð¸Ñ Ñ "л уконР° Ð · оР»Ð ° Ð'л Ñ Ð¼Ð ° Ñ,ÐμÑ € и Ð · нР° Ñ ‡ иР»Ñ,Ðμл Welcome, welcome, welcome. ÐºÐ¾Ð½Ñ † ÐμнÑ,Ñ € Ð ° Ñ † Ð¸Ñ Ñ "л уконР° Ð · оР»Ð ° в Ð³Ñ € уÐ'ном мол окÐμ и в пР»Ð ° Ð · мÐμ оÐ'и нР° ковР°, Ð¿Ñ € имÐμÐ½Ñ Ñ,ÑŒ Ð¿Ñ € ÐμпР° Ñ € Ð ° Ñ,Ð ° в пÐμÑ € иоÐ' Ð »Ð ° кÑ,Ð ° Ñ † Handle - Handle

    Repeatable:
    Come on.
    Ð'Ð · Ñ € Ð¾Ñ Ð »Ñ <м и Ð'ÐμÑ,Ñ Ð¼ Ñ Ñ,Ð ° Ñ € ÑÐμ 15 л ÐμÑ, (мР° Ñ Ñ Ð¾Ð¹ Ñ,ÐμÐ »Ð ° Ð ± ол ÐμÐμ 50 кг) Ð¿Ñ € и ÐºÑ € ипÑ,ококковом мÐμнингиÑ,Ðμ и ÐºÑ € ипÑ,Ð¾ÐºÐ¾ÐºÐºÐ¾Ð²Ñ <Ñ ... Ð¸Ð½Ñ "ÐμÐºÑ † Ð¸Ñ Ñ ... Ð'Ñ € ÑƒÐ³Ð¸Ñ ... Ð »Ð¾ÐºÐ ° л иР· Ð ° Ñ † ий в пÐμÑ € Ð²Ñ <й Ð'Ðμнь оР± Ñ <Ñ ‡ но нР° Ð · нР° Ñ ‡ Ð ° ÑŽÑ, 400 мг (8 кР° Ð¿Ñ ÑƒÐ »Ð¿Ð¾ 50 мг), Ð ° Ð · Ð ° Ñ,Ðμм Ð¿Ñ € оÐ'ол жР° ÑŽÑ, Ð »ÐμÑ ‡ Lovely couple of 200 pieces (4 кР° Ð¿Ñ ÑƒÐ »Ñ <по 50 мг) - 400 мг (8 кР° Ð¿Ñ ÑƒÐ» по 50 мг) 1 Ñ € Ð ° Ð · в Ñ ÑƒÑ,ки.The duration of treatment for cryptococcal infections depends on the clinical efficacy, confirmed by mycological examination; when cryptococcal meningitis treatment course should be at least 6-8 weeks.
    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 (4 capsules of 50 mg) per day for a long period of time.
    When candidemia, disseminated candidiasis and other invasive candidiasis infections on the first day of the dose is 400 mg (8 capsules of 50 mg), and then - 200 mg (4 capsules of 50 mg) per day. With insufficient clinical effectiveness, the dose of the drug can be increased to 400 mg (8 capsules 50 mg) per day. The duration of therapy depends on clinical effectiveness.
    With oropharyngeal candidiasis, the drug is usually prescribed for 150 mg 1 time / day; the duration of treatment is 7-14 days. If necessary, in patients with a marked decrease in immunity, treatment may be longer.
    To prevent the recurrence of oropharyngeal candidiasis in AIDS patients after completing the full course of primary therapy - 150 mg once a week.
    With atrophic oral candidiasis associated with the wearing of dentures, 50 mg once a day for 14 days in combination with local antiseptic medicines to treat the prosthesis.
    In 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 150 mg / day with a treatment duration of 14-30 days.
    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. Duration of therapy from 4 to 12 months. Some patients may need more frequent use.
    With balanitis caused by Candida, fluconazole is administered intravenously at a dose of 150 mg / 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. For the prevention of candidiasis in patients with malignant neoplasms the recommended dose of fluconazole is 150-400 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 / day. Fluconazole appoint a few days before the expected appearance of neutropenia. After increasing the number of neutrophils more than 1 thousand / μl treatment is continued for another 7 days.
    With mycosis of the skin, including mycosis of the feet, skin of the inguinal region, and skin candidiasis, the recommended dose is 150 mg once a week or 50 mg once a day, the dosage regimen depends on the clinical mycological effect. 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 lichen - 300 mg (2 capsules of 150 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 One-time intake of 300-400 mg; an alternative treatment regimen is to apply 50 mg once a day for 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 the nails on the fingers and toes 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 mg (4 capsules of 50 mg) - 400 mg (8 capsules 50 mg) per day for up to 2 years. The duration of therapy is determined individually: it can be
    11-24 months. with coccidioidomycosis and 3-17 months. with histoplasmosis.
    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. Fluconazole is excreted mainly with urine in unchanged form. In chronic renal failure, a "shock" dose of 50-400 mg is initially administered. 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 50% of the recommended dose or usual dose is applied once in 2 days.
    Patients with impaired renal function fluconazole is introduced according to the following scheme:

    Creatine Clearance

    Interval / daily dose

    > 40 ml / min

    24 hours (normal dosing regimen)

    21-40 ml / min

    48 hours (1 time in 2 days) or half the usual daily dose (1 time in 24 hours)

    10-20 ml / min

    72 hours (1 every 3 days) or a third of the usual daily dose (1/3 in 24 hours)

    Patients regularly on dialysis, one dose of the drug is used after each session of hemodialysis.

    Side effects:
    From the digestive system: loss of appetite, changes in taste, abdominal pain, vomiting, nausea, diarrhea, flatulence, abdominal pain, rarely - liver dysfunction (jaundice, hepatitis, gepatonekroz, hyperbilirubinemia, increased alanine aminotransferase activity, aspartate aminotransferase, increased alkaline phosphatase , hepatocel Lular necrosis), incl. heavy.
    From the nervous system: headache, dizziness, excessive fatigue, rarely - convulsions.
    From the hemopoiesis: rarely - leucopenia, thrombocytopenia (bleeding, petechiae), neutropenia, agranulocytosis.
    Allergic reactions: skin rash, rarely - erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions (including angioneurotic edema, swelling of the face, hives, itchy skin) .
    From the cardiovascular system: an increase in the duration of the QT interval, flicker / flutter of the ventricles.
    Other: rarely - a violation of kidney function, alopecia, hypercholesterolemia, hypertriglyceridemia, hypokalemia.

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

    Interaction:
    When using 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 coumarin anticoagulants.
    Fluconazole increases the half-life of plasma from oral hypoglycemic agents - sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide, tolbutamide) in healthy people. Joint use of fluconazole and oral hypoglycemic agents in diabetic patients is allowed, 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, if a joint use of these drugs is necessary,
    monitor the concentration of phenytoin with correction of its dose in order to maintain the drug concentration within the therapeutic interval.
    Combination with rifampicin leads to a decrease in the area under the concentration-time curve (AUC) by 25% and a shortening of the half-life of fluconazole from the plasma by 20%. Therefore, it is advisable to increase the dose of fluconazole to patients receiving rifampicin simultaneously.
    It is recommended to monitor the concentration of cyclosporine in the blood in patients receiving fluconazole, because with the use of fluconazole and cyclosporine in patients with kidney transplantation, the use 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 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, terfenadine and cisapride, cases of unwanted reactions from the heart, including paroxysms of ventricular tachycardia (torsades des points), have been described.
    Simultaneous use of fluconazole and hydrochlorothiazide can lead to an increase in the concentration of fluconazole in blood plasma by 40%.
    There are reports of the interaction of fluconazole and rifabutin, accompanied by an increase in the serum concentration of the latter. With simultaneous application of fluconazole and rifampumbin, cases of uveitis are described. It is necessary to carefully observe patients who simultaneously receive rifabutin and fluconazole.
    In patients receiving 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 the side effects of zidovudine should be expected to increase.
    Increases the concentration of midazolam, which increases the risk of developing psychomotor effects (more pronounced when fluconazole is administered orally than intravenously).
    Increases the concentration of tacrolimus, in connection with which, the risk of nephrotoxic action increases.

    Special instructions:
    Treatment should continue until the appearance of clinical-hematologic remission. Premature termination of treatment leads to relapse.
    In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, in tons: h. with Fatal outcome, mainly in patients with serious concomitant diseases. In the case of hepatotoxic effects associated with fluconazole, there was no apparent dependence on total daily dose, duration of therapy, sex and age of the patient. The hepatotoxic effect of fluconazole was usually reversible; signs of it disappeared after discontinuation of therapy. When there are clinical signs of liver damage that can be associated with flnonazole, the drug should be discarded.
    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.
    Care should be taken when taking fluconazole simultaneously with cisapride, rifabutin, or other drugs metabolized by the cytochrome P450 system.

    Form release / dosage:
    Capsules 50 mg and 150 mg.

    Packaging:
    For 7 capsules with a dosage of 50 mg or 1 capsule with a dosage of 150 mg in a contiguous cell pack of Polyvinylchloride Film AND aluminum foil printed lacquered.
    For 1, 2 contour packs of 7 capsules or 1 contour pack of 1 capsule with instructions for use are placed in a pack of cardboard.

    Storage conditions:
    In a dry, protected from light place 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 expiration date.

    Terms of leave from pharmacies:Without recipe
    Registration number:P N002942 / 01
    Date of registration:14.08.2008
    The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia
    Information update date: & nbsp16.10.2015
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