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One capsule of means Sporagal includes 100 mg of an itrakonazol.
Additional substances: sucrose, polyethyleneglycol 20000, acrylate copolymer, gidroksipropilmetiltsellyuloz.
Structure of a capsule: titanium dioxide, gelatin, indigotin.
Solid blue gelatinous capsules, contain yellowish spherical granules inside. 10 capsules in the blister — three or one blister in a pack from paper.
Pharmacodynamics and pharmacokinetics
Derivative triazole, possessing a broad spectrum of activity concerning fungi. Slows down biosynthesis of ergosterol of walls of a cell of a fungus, providing thereby antifungal effect.
Research demonstrate what itrakonazol blocks growth of a large number of types of fungi, disease-producing for the person. Treat those:
- dermatophytes of the sort Microsporum, Trichophyton and Epidermophyton floccosum;
- yeast of the sort Pityrosporum, Trichosporon, Geotrichum, Candida (including C.кrusei, C.glabrata, S. albicans) and Cryptococcus neoformans;
- fungi of the sort Aspergillus, Fonsecaea, Histoplasma, Cladosporium, Sporothrix schenckii, Paracoccidioides brasiliensis, Blastomyces dermatidis, Pseudallescheria boydii, Coccidiodes immitis, Penicillium marneffei and other versions.
Candida krusei, glabrata and tropicalis are the least susceptible types of Candida, and a number of isolates show nonsensitivity to an itrakonazol at all.
The main groups of fungi which are not suppressed itrakonazoly: Zygomycetes of the sort Rhizopus, Rhizomucor, Mucor, Absidia, and also fungi of the sort Fusarium, Scopulariopsis and Scedosporium ptoliferans.
It is actively soaked up after oral administration. The maximum level of an itrakonazol in blood comes 2-4 hours later. Bioavailability reaches 55%. The greatest bioavailability of an itrakonazol is registered at intake directly after the use of high-calorific food.
Reacts with blood proteins to 99,7%. Itrakonazol shows also expressed tropnost to fats. Only about 0,3% of a dose in blood circulate in an untied look. It is distributed in different bodies and body tissues. Contents in kidneys, bones, lungs, a liver, a stomach, skeletal muscles, a spleen is 2-3 times more than the content in blood, and concentration in the fabrics including a keratin (for example, in skin), concentration in blood are four times higher.
It is metabolized in a liver with allocation of a large number of derivatives, but only one of them (gidroksiitrakonazol) renders antifungal effect at the level, comparable with itrakonazoly. Content in blood of an active metabolite is twice higher, than an itrakonazola.
CYP3A4 – the main enzyme which participates in transformation of active agent. About 34% of an itrakonazol in the form of inactive metabolites are allocated with kidneys and 54% — intestines. In an invariable look kidneys bring about 0,03%, and intestines in an invariable look evacuate 3-17% of the accepted dose. The elimination half-life reaches 40 hours.
Persons with insufficiency have functions of kidneys and a liver, and also at a number of patients with immunosuppression (a neutropenia, AIDS, organ transplantation) bioavailability can decrease.
Indications to use
The mycoses provoked by activators, sensitive to drug:
- dermatological and ophthalmologic diseases of the fungal nature – a dermatomycosis, a fungal keratitis, a chromophytosis;
- vulvovaginal candidiasis;
- oral candidiasis;
- system mycoses — system candidiasis, a cryptococcosis, a system aspergillosis, cryptococcal meningitis (to persons with the weakened immunity at a cryptococcosis of a nervous system means is appointed only in case of absence of effect of treatment other antifungal drugs);
- the onychomycoses provoked by yeast or dermatophytes;
- paracoccidioidosis, sporotrichosis, histoplasmosis, zymonematosis and other rare system mycoses.
Hypersensitivity to drug components.
Simultaneous treatment by the following medicines:
- the reductase HMG-CoA blockers which are metabolized thanks to CYP3A4 (Lovastatin, Atorvastatin, Simvastatin);
- the CYP3A4 substrates increasing QT interval – Bepridil, Astemizol, tsizaprid, Dofetilida, Mizolastin, Quinidine, Pimozidum and others;
- Triazolam and midazolam for intake;
- ergot alkaloids;
Use of drug is contraindicated to patients with ventricular dysfunction, including heart failure of congestive character (except treatment according to vital indications).
Dermatological, digestive and hepatic reactions were the most frequent undesirable reactions when using an itrakonazol.
- Invasions and reactions of infectious character: infections of upper respiratory ways.
- Reactions from a hemopoiesis: thrombocytopenia, neutropenia, leukopenia.
- Metabolic frustration: hypopotassemia, gipertriglitseridemiya, hypocalcemia.
- Reactions from immunity: Quincke's disease, serum disease, anaphylactic, allergic and anaphylactoid reactions.
- Reactions from nervous activity: paresthesias, headache, hypesthesia, peripheral neuropathy, dizziness.
- Reactions from touch bodies: diplopia, sight opacification, hearing loss, vision disorder, sonitus.
- Reactions from blood circulation: heart failure of congestive character.
- Reactions from breath: sinusitis, rhinitis, short wind, fluid lungs.
- Reactions from digestion: dyspepsia, abdominal pains, vomiting, nausea, lock, diarrhea, dysgeusia, swelling, pancreatitis, temporary increase of content of transaminases of a liver, hepatotoxic reactions, hepatitis.
- Reactions from skin: photosensitivity, alopecia, itch, urticaria, rash, multiformny erythema, acute exanthematous generalized pustulez, epidermal toxic necrolysis, leykotsitoklastichesky vasculitis, exfoliative dermatitis.
- Reactions from a musculoskeletal system: muscle and joints pains.
- Reactions from the urinogenital sphere: urine incontience, dysmenorrhea, pollakiuria, erectile dysfunction.
General reactions: hypostases, fever.
Application instruction (Way and dosage)
The instruction on Sporagal orders to accept drug orally. It is necessary to use capsules directly after reception of food for ensuring the best absorption of drug Sporagal. The application instruction also recommends to swallow of capsules entirely.
At treatment of vulvovaginal candidiasis appoint twice a day on 200 mg of means within one days or 200 mg of times a day within 3 days.
At dermatological and ophthalmologic defeats (dermatomycoses, a chromophytosis) appoint 200 mg of means of times a day for a week.
At defeat of the keratinized skin sites (feet and hands) treatment of 200 mg of medicine twice a day for a week is offered.
At treatment of oral candidiases appoint within 2 weeks to accept 100 mg of times a day. At patients with a neutropenia or AIDS it is recommended to increase a dosage to 200 mg of times a day keeping the two-week duration of treatment.
At a fungal keratitis accept 200 mg of times a day within 3 weeks.
The onychomycoses caused by barmy mushrooms or dermatophytes treat by method of repeated courses pulse therapy.
One course includes reception of 2 capsules twice a day for one week. For therapy of damages of nails of fingers of brushes it is recommended to conduct 2 courses of such therapy. For therapy of damages of nails of fingers of feet – 3 courses. The break between courses makes usually 3 weeks. Results are shown after completion of therapy in process of growth of nails.
Evacuation of an itrakonazol from skin and nails longer than evacuation from blood therefore optimum clinical effects are reached 2-3 weeks later after the end of therapy of skin infections and 7-9 months later after the end of therapy of onychomycoses. Duration of therapy of systemic lesions has to be adjusted, considering clinical results.
At therapy of candidiasis appoint 100-200 mg of times a day for 3-30 weeks.
At therapy of an aspergillosis accept 200 mg of means of times a day for 2-5 months.
At a cryptococcosis without existence of meningitis appoint 200 mg of times a day for 2-12 months. At cryptococcal meningitis the dosage is doubled keeping treatment terms.
At a sporotrichosis accept 100 mg of times a day for 3 months.
At histoplasmosis 1-2 times a day for 8 months recommend reception of 200 mg of drug.
At chromomycosis recommend reception of 100-200 mg of times a day for 6 months.
At a paracoccidioidosis accept 100 mg of times a day for 6 months, however for patients with AIDS of a similar dosage can be insufficiently.
At a zymonematosis it is possible to recommend reception of 100 mg of times a day to 200 mg twice a day for 6 months.
There are no confirmed messages on overdose episodes.
At inadvertent overdose consults to wash out a stomach (if from the moment of reception passed no more than an hour), to accept enterosorbents. Is not removed by means of a dialysis. There is no selection antidote.
The medicines reducing acidity reduce absorption of an itrakonazol.
Simultaneous use of the drugs stimulating hepatic fermental systems (Rifabutin, Rifampicin, Phenytoinum), significantly lowers bioavailability of an itrakonazol. At combined use with the Isoniazid, Phenobarbital, Carbamazepine, extract of a St. John's Wort we expect the same effect.
Potential blockers of CYP3A4 enzyme (Sakvinavir, Indinavir, Erythromycin, Ritonavir, Klaritromitsin) can increase bioavailability of an itrakonazol.
Itrakonazol is capable to suppress transformation of the means which are metabolized enzymes of the CYP3A4 type that can lead to strengthening or lengthening of their effects, including undesirable reactions.
After completion of therapy the level of an itrakonazol in blood decrease slowly. It needs to be considered at an assessment of overwhelming effect of active agent on a metabolism of means which are applied jointly.
It is necessary to be careful at combined use with blockers of channels of calcium in connection with increase in risk of heart failure of congestive character. Also blockers of channels of calcium can provoke negative inotropic effect which is capable to strengthen identical action of an itrakonazol.
Drugs when which using it is necessary to control their concentration in blood action or undesirable effects (at combined use with itrakonazoly the dose of stated below drugs if necessary is recommended to be reduced):
- peroral coagulants;
- protease inhibitors;
- some antineoplastic means – Busulfan, Dotsetaksel, alkaloids of a pink periwinkle, Trimetreksat;
- blockers of channels of calcium which are metabolized by CYP3A4 enzyme;
- some immunosuppressive means – Takrolimus, Cyclosporine, Sirolimus;
- some glucocorticoids – Flutikazona, Dexamethasone, Budesonid, Methylprednisolonum;
- drugs, the importance of interaction with which becomes clear – Tsilostazol, Carbamazepine, Buspiron, Alfentanil, Disopyramidum, Alprazolam, Midazolam, Brotiozolam, Rifabutin, Galofantrin, Fentanyl, Ebastin, Repaglinid and Reboksetin.
Terms of sale
According to the recipe.
To store at a temperature not above 25 °C. To protect from children.
Period of validity
Itrakonazol shows negative inotropic effect. There are messages on congestive heart failure which is connected with Sporagal's use. Episodes of heart failure at a dose of 400 mg a day were more frequent, than when using a smaller day dose. Drug should not be used to patients with heart failure of congestive character or with existence of this disease in the anamnesis, except cases when the probable advantage exceeds possible risk.
Joint reception of blockers of channels of calcium and itrakonazol can stimulate negative inotropic effect, also the last can brake an exchange of blockers of channels of calcium therefore it is necessary to observe extra care at their simultaneous use because of increase of risk of development of heart failure of congestive type.
When using an itrakonazol the heavy hepatotoxic extremely seldom develops, up to acute lethal insufficiency of function of a liver. Generally similar cases were observed at persons with a liver disease which had other serious diseases or used gepatotoksichny means. It is necessary to exercise control of work of a liver when using drug.
To patients with the active disease of a liver increased by the level of transaminases or with manifestations of a hepatotoxic from reception of other means, it is necessary to appoint drug only in emergency cases. In a similar situation monitoring of level of enzymes of a liver is necessary.
When lowering acidity absorption of medicine worsens. The patients using at the same time antiacid drugs have to observe a two-hour break between receptions. The patient with an achlorhydria, AIDS or the accepting H2 inhibitors and blockers of a proton pomp, it is recommended to accept itrakonazol with carbonated drink.
Drug should not be accepted to elderly patients, except situations when the expected advantage is higher than potential risk.
It is necessary to be careful when using drug at persons with disturbances of work of kidneys. Decrease in bioavailability of active agent at oral administration at persons with a renal failure or the weakened immunity is not excluded. In a similar case it is necessary to consider a question of change of a dose.
For the patients with AIDS passing therapy concerning system mycoses and belonging to risk group of emergence of recurrence it is necessary to consider the possibility of purpose of a maintenance therapy.
Due to the pharmacokinetic features itrakonazol does not consult to accept for primary treatment of the medical emergencies provoked by fungal infections of system character.
At emergence of symptoms of the peripheral neuropathy connected with administration of drug, Sporagal it is necessary to cancel.
Drug should be accepted 2 weeks later after the end of treatment by CYP3A4 activators (Rifabutin, Rifampicin, Phenytoinum, Phenobarbital, St. John's Wort extract, Carbamazepine). Sporagal's use along with these drugs can cause lowering of a dose of an itrakonazol in blood and, therefore, to inefficiency of treatment.
Patients with intolerance of fructose or deficit of sucrose-isomaltose should avoid reception of this drug.
Coincidence on the ATH code of the 4th level:
The most known analogs of Sporagal are listed below: Itrungar, Orungal, Sporaksol, Funit, Eszol.
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