Producer: LLC Pharm Start Ukraine
Code of automatic telephone exchange: J02AC02
Release form: Firm dosage forms. Capsules.
General characteristics. Structure:
Active agent: итраконазол 100 mg.
Pharmacodynamics. Sporagal - synthetic antifungal drug of group of triazoles with a wide range of antifungal action. The mechanism of action of Sporagal same, as at other drugs of a class of azoles. It suppresses formation of ergosterol of cell walls of a mushroom, exerting impact to a nalanosterindimetilaz - the enzyme dependent on R-450 cytochrome. Trichophyton spp are sensitive to drug., Microsporum spp., Epidermophyton floccosum, Candidaspp. (Including S. albicans), Cryptococcus neoformans, Aspergillus spp., Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp., Cladosporium spp., Blastomyces dermatidis and some иншимикро organisms.
Pharmacokinetics. Maksimalnabiodostupnist Sporagala is marked out at administration of drug right after food. After a single dose of drug the maximum concentration of an itrakonazol in a blood plasma is reached in 3 - 4 hours. At prolonged use stable concentration of an itrakonazol in plasma is reached in 1 - 2 weeks from an initiation of treatment and in 3 - 4 h after reception of the last dose of drug makes 0,4 mkg/ml - at reception 100 mgitrakonazola of 1 times a day; 1,1 mkg/ml - at reception of 200 mg of drug of 1 times a day; 2,0 mkg/ml - at reception of 200 mg 2 times a day. 99,8% of active agent contact proteins of plasma. Itrakonazol is distributed in different body tissues, and concentration in lungs, kidneys, a liver, bones, a stomach, a spleen, skeletal muscles by 2 - 3 times exceeds concentration of an itrakonazol in a blood plasma. Concentration of an itrakonazol in the fabrics containing a keratin, especially in skin by 4 times exceeds concentration in a blood plasma. Therapeutic concentration of an itrakonazol in skin remains within 2 - 4 weeks after the termination of a 4 weeks course of treatment. Therapeutic concentration of an itrakonazol in a keratin of nails is reached in 1 week after an initiation of treatment and remains at least within 6 months after end of a 3-month course of treatment. Itrakonazol gets also in grease and stalemate (in smaller quantity) skin glands. Drug is metabolized in a liver with formation of a large number of derivatives, one of which - гидроксиитраконазол - attracts antifungal action almost at the level of an itrakonazol and has the final period to a floor of removal of 1 - 1,5 days. About 35% of a dose of drug are removed with urine in the form of metabolites within 1 week, less than 0,03% are brought out of them in not changed look. With a stake in not changed look about 3 - 18% of a dose of drug are removed. At patients with a renal and liver failure, and also at some patients with immunosuppression (AIDS, a neutropenia, organ transplantation) bioavailability of an itrakonazol can decrease.
Indications to use:
• treatment of the mycoses caused by activators, sensitive to drug:
• vulvovaginal candidiasis;
• mycoses of skin, oral cavity, eye (in particular dermatomycosis, chromophytosis, fungal keratitis, candidosis stomatitis);
• the onychomycoses caused by dermatophytes and/or barmy mushrooms;
• system mycoses: system aspergillosis, candidiasis, cryptococcosis (including cryptococcal meningitis), histoplasmosis, sporotrichosis, paracoccidioidosis, zymonematosis.
Route of administration and doses:
Drug is appointed inside, right after food, swallow of capsules entirely. At vulvovaginal кандидозипрепарат appoint 2 capsules 2 times a day within 1 day or on 2 capsules of 1 times a day within 3 days. At chronic retsidivuyuchomugribkovy a vulvovaginitis - on 1 capsule 2 times a day within 6 - 7 days, then during 3 - 6 menstrual cycles on 1 capsule in the first day of a cycle. At visivkopodibnomu herpes - 2 capsules of 1 times a day within 7 days. At dermatomycoses - 1 capsule of 1 times a day within 15 days. In case of defeat of the high-keratinized sites (such as skin of brushes and feet) conduct an additional course of treatment within 15 days, applying such a drug dose. At oral cavity candidiasis - 1 capsule of 1 times a day within 15 days. At a fungal keratitis - 2 capsules of 1 times a day within 21 days. At onikhomikozi - 2 capsules a day within 3 months or carry out repeated courses of treatment by method pulse therapy, appointing drug on 2 capsules 2 times a day during 1tizhnya with the following breaks: at damage of nails standing (irrespective of whether nails on hands are affected) conduct 3 courses of treatment: 1 weeks of administration of drug, then 3 weeks break. At damage of nails only on hands conduct 2 courses of treatment: 1 weeks of administration of drug, 3 weeks - a break. At a system aspergilyozipreparat appoint 2 capsules of 1 times a day within 5 months, if necessary the dose of drug is raised to 2 capsules by 2 times a day. At a system candidiasis - 1 - 2 capsules of 1 times a day during from 3 weeks to 7 months, if necessary raise a dose of drug to 2 capsules 2 times a day. At a system cryptococcosis (without symptoms of meningitis) - 2 capsules of 1 times a day; for a maintenance therapy drug is appointed on 2 capsules of 1 times a day from 2 months to 1 year. To Prikriptokovy meningitis - on 2 capsules 2 times a day. At histoplasmosis - from 2 capsules of 1 times a day to 2 capsules 2 times a day within 8 months. At a sporotrichosis - 1 capsule of 1 times a day within 3 months. At a paracoccidioidosis - 1 capsule of 1 times a day within 6 months. At chromomycosis - 1 - 2 capsules of 1 times a day within 6 months. At a blastoma to a goat - from 1 capsule of 1 times a day to 2 capsules 2 times a day within 6 months. For some patients with immunity disturbances (AIDS, organ transplantation, a neutropenia) increase in a dose of drug can be required.
Features of use:
During pregnancy drug is appointed only at system mycoses if the expected effect of therapy exceeds risk of undesirable influence on a fruit. Women of childbearing age during treatment by drug are recommended to apply effective contraceptive remedies. During feeding a breast drug is appointed only when the expected effect of treatment exceeds risk of possible undesirable influence on the child. To patients with the increased level of transaminases in blood drug is appointed only in cases if the expected effect of therapy exceeds possible action rizikgepatotoksichno; use of drug is admissible if values of indicators of ALAT and ASAT exceeds the upper bound of norm no more than twice. At cirrhosis or a renal failure drug is used under control of level of an itrakonazol in plasma; in case of need adjust doses. The functional condition of a liver is necessary cotton wool control if the course of treatment lasts more than 1 month and also if at the patient accepting drug the vinikayeanoreksiya, nausea, vomiting, increased fatigue, an abdominal pain or is marked dark color of urine. At identification of abnormal liver functions drug is cancelled. At the peripheral neuropathy caused by administration of drug it is also necessary to cancel drug. Clinical data are still not enough to recommend drug for broad use in pediatric practice.
Dyspepsia, nausea, abdominal pain, lock, транзиторнепидвищення activities of transaminases in blood, in some cases at prolonged treatment - hepatitis (accurate relationship of cause and effect is not established with administration of drug ), a headache, dizziness, peripheral neuropathy, allergic reactions (a skin itch, a small tortoiseshell, ангио neurotic hypostasis, Stephens-Johnson's syndrome); a dysmenorrhea, in some cases at prolonged treatment the alopecia, a hypopotassemia, hypostases are possible.
Interaction with other medicines:
The concomitant use in a terfenadin, an astemizola, a tsizaprida, midazolam is not recommended from the Dispute by the Gaul to an abotriazolam. It is necessary to be careful at co-administration of indirect anticoagulants, cyclosporine A, digoxin, blockers of calcium channels of group of dihydropyridine, and also quinidine and Vincristinum which metabolism is carried out with the participation of enzymes like cytochrome 450-3A as strengthening of effects and/or increase in time of effect of these medicines is possible. A concomitant use of the drugs inducing fermental systems of a liver (rifampicin, Phenytoinum, etc.)., Significantly reduces Sporagal's bioavailability. Antiacid drugs accept not earlier, than in 2 hours after Sporagal's reception. At a concomitant use of Sporagal with a zidovudine, ethinylestradiol abonoretisterony considerable interaction is noted.
Hypersensitivity to drug or its components.
There are no messages on cases of overdose of drug.
To store in the place, unavailable to children, at a temperature from 15 to 25 °C.
According to the recipe
Капс. 100 mg, No. 10, No. 30.