Ketazol

General characteristics. Structure:

Active agent - кетоконазол 200 mg.

Excipients: lactoses monohydrate, cellulose microcrystallic, povidone (polyvinylpirrolidone), sodium of starch glikolit, silicon dioxide colloid (аэросид), magnesium stearate.

Pharmacological properties:

Pharmacokinetics. At intake it is well soaked up (especially in acid medium of a stomach). Ketokonazol is well dissolved in lipids that promotes high bioavailability (75-90%). Cmax is reached in plasma of 3,5 mg/ml in 2 hours after a single dose in 200 mg of drug during food. Contacts proteins of plasma (albuminous fraction) makes 99%. An insignificant part of drug gets into cerebrospinal fluid and urine. Ketokonazol is metabolized in a liver, way oxidation and splitting of imadazolny and piperazinovy rings, oxidizing O-dealkylation and an aromatic hydroxylation. Removal from plasma two-phase: within the first 10 hours the elimination half-life (Т½) makes 2 hours, and in the subsequent-8 hours. 13% - with urine are allocated in an invariable look and in the form of inactive metabolites, generally with bile, and.

Pharmacodynamics. Ketazol has antifungal, fungistatic, fungicidal effect. Slows down synthesis of ergosterol, the triglycerides and phospholipids necessary for synthesis of a cellular membrane of fungi (fungi lose colony-forming).

It is active concerning dermafit, yeast (Candida, Pityrosporum, Torulopsis, Cryptococcus), dimorphous fungi and the highest mushrooms (eumitset). Are less sensitive to action of a ketokonazol of Aspergillus spp., Sporothrix schenckii some Dermatiaceae, Mucor spp. and other phycomycetes, except for Enomophthorales.

Indications to use:

- the damages of skin, hair and nails caused by dermatophytes and/or yeast (a dermatophytosis, an onychomycosis, a candidosis paronychia, multi-colored deprive, a folliculitis, a trichophytosis);

- бластомицетоз oral cavity and digestive tract (DT);

- the seborrheal dermatitis caused by Pityrosporum ovale;

- system mycoses (candidiasis, паракокцидиомикоз, histoplasmosis, кокцидиомикоз, zymonematosis);

- vaginal candidiasis (acute and chronic recuring), dermatomycosis of smooth skin, inguinal epidermophitia, chromophytosis;

- mycoses at patients with an immunodeficiency (prevention).

Ketazol is applied when these infections it is impossible to treat locally owing to their localization, wide circulation and deep damage of skin.

Route of administration and doses:

Due to a hepatotoxic Ketazol is recommended to apply only when other antifungal drugs are not effective.

Accept inside once a day during food.

Adults. At dermatomycoses – on 200 mg (1 tablet) once a day within 2-8 weeks. At onychomycoses and chronic candidiases – on 200 mg ((1 tablet) to full (with mycologic control) recovery (4-6 weeks). At gastrointestinal tract diseases and urinogenital system – on 1-2 tablets a day within 2 weeks, then on 1 tablet a day to an absolute recovery (4-6 weeks). At system mycoses appoint in the first 2 weeks 2 tablets a day, then on 1 tablet a day within several months.

Preventively appoint on 1 tablet a day, duration of treatment depends on a current of a basic disease.

For children over 6 years, with the body weight of 20-40 kg, the daily dose makes 100 mg (½ tablets).

When using a ketokonazol for treatment of mycoses of eyes appoint 200 mg (1 tablet) a day.

Features of use:

Ketazol is recommended to appoint only when the expected advantage perevyshat potential risk, accepting availability of other antifungal drugs in attention.

Before an initiation of treatment it is necessary to exclude an acute and chronic disease of a liver. At oral administration it is regularly necessary to control a pattern of peripheral blood, a functional condition of a liver and kidneys. In case of the subjective and objective symptoms testimonial of possible development of hepatitis, it is necessary to cancel administration of drug immediately.

If applied glucocorticosteroids to treatment of skin defeats, then кетоконазол it is necessary to appoint not earlier than in 2 weeks.

With care women should appoint more senior than 50 years.

Ketokonazol can suppress metabolism of the medicines split by some liver enzymes of system of P450 cytochrome, especially from the CYP3A group. At a concomitant use with such drugs there can be strengthening or prolongation of their action and the possible undesirable side reactions (USR). In such cases it is necessary behind their levels in plasma, undesirable side reactions.

At a concomitant use with alcohol there can be a Disulfiramum-like reaction which is characterized by erubescence, rash, hypostases, nausea and a headache.

At patients with reduced acidity of a gastric juice Ketazol's absorption decreases. The patients receiving antacids have to accept these drugs not earlier than in 2 hours after Ketazol's reception.

During treatment by drug Ketazol at patients with adrenal insufficiency, and also at prolonged use is recommended to control function of adrenal glands.

Sick AIDS and to the persons receiving anti-secretory drugs (antagonists histamine H2 receptors or inhibitors of the protonew pump), recommends to wash down Ketazol's tablets with drinks Pepsi Cola or Coca-Cola.

Fungal meningitis it is not necessary to treat drug Ketazol as it badly gets through a blood-brain barrier.

Ketazol gets into breast milk, in this regard it is not recommended to appoint during breastfeeding.

Considering side effects of drug it is necessary to be careful when driving and other potentially dangerous mechanisms.

Side effects:

- loss of appetite, abdominal pains, nausea, vomiting, diarrhea;

- changes of indicators of level of transaminases, toxic damage of a liver, including jaundice, hepatitis, a necrosis and cirrhosis, a liver failure;

- headache, dizziness, sleeplessness, paresthesias, reversible increase in intracranial pressure;

- gynecomastia, decrease in a libido, disturbance of a menstrual cycle, impotence, oligospermatism;

- rash, a skin itch, a small tortoiseshell, an anaphylaxis (including a Quincke's disease and an acute anaphylaxis).

Seldom:

- photophobia;

- alopecia;

- arthralgia;

- insufficiency of bark of adrenal glands;

- fever;

- thrombocytopenia;

- hyperemia, irritations and itch of a mucous membrane of a vagina.

Interaction with other medicines:

At simultaneous use with rifampicin, an isoniazid rifabutiny, not Virapinum and fenintoiny notes decrease in concentration of a ketokonazol in a blood plasma.

At a concomitant use with the drug (ритонавир) increasing bioavailability of a ketokonazol it is necessary to reduce a dose of the last.

Joint reception of following groups of drugs with Ketazol has to be carefully analyzed and in need of their dose has to be reduced:

- anticoagulants peroral;

- HIV protease inhibitors (индинавир, саквинавир);

- some antineoplastic drugs (иматиниб and эрлотиниб, dotsetakset and бисульфан, alkaloids of the Periwinkle pink);

- the blockers of "slow calcium channels" of a dihydropyridinic row split by CYP3A4 enzyme (verapamil);

- some immunosuppressive means (cyclosporine, токролимус, сиролимус);

- аторвастатин, glucocorticoids, digoxin, alfentanil, to alprazola, brotiozolam, буспирон, carbamazepine, циклотазол, эбастин, fentanyl, to midozala for intravenous use, кветиапин, ребоксетин, репаглинад, рифабутин, sildenafit, солифенацин, тольтерадин, триметрексат.

With oral contraceptives, with the low content of hormones, breakthrough bleedings can cause simultaneous use.

Contraindications:

- hypersensitivity to drug components;

- abnormal liver functions;

- pregnancy and period of a lactation;

- children's age up to 18 years;

- a concomitant use with astemizoly, tsizapridy, terfanidiny, domperidony, midazolam, statines (simvastat and ловастатин), ergot alkaloids (dihydroergotamine, ergometrine or эргоновин, ergotamine and methylergometrine or метилэргоновин), everolimusy.

Overdose:

Overdose cases are not described by drug.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 25 °C.

 

To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging from a film polyvinyl chloride or import and a foil aluminum or import. 1 blister strip packaging together with the approved instruction on a medical use in the state and Russian languages is placed in a pack from a cardboard.