Ketokonazol таб. 0,2 No. 10

General characteristics. Structure:

International and chemical name: ketoconazole; tsis-1-atsetil-4-[4-[[2-(2,4 dichlorophenyl)-2-(1H-imidazole-1-илметил) - 1,3-dioxolane-4-silt] metoks] phenyl] piperazin.osnovny physical and chemical properties: tablets of white or almost white color with фаской.состав: one tablet contains a ketokonazol of 0,2 g; excipients: starch corn, lactose, silicon dioxide colloid, magnesium stearate, PVP low-molecular.

Pharmacological properties:

Pharmacodynamics. Antifungal broad-spectrum agent. Slows down synthesis of ergosterol, triglycerides and phospholipids that leads to disturbance of permeability of a cell wall and causes mikostatichesky effect. Has fungicidal and fungistatic activity concerning the activator multi-colored depriving of Pityrosporum orbiculare, activators of some dermatomycoses (Trichophyton spp., Epidermophyton floccosum, Microsporum spp.), causative agents of candidiasis (Candida spp.), and also causative agents of system mycoses (Cryptococcus spp.). It is active also concerning gram-positive cocci (Staphylococcus spp., Streptococcus spp.).

Pharmacokinetics. After intake drug is well soaked up. Absorption worsens at increase рН gastric contents. The maximum concentration in plasma is reached in 1–2 hours. Linkng with proteins of plasma makes 99%. Pharmacokinetic processes are presented by two-phase model: an elimination half-life of the first phase – 2 hours, the second phase – 8 hours. It is removed in an invariable look and in the form of inactive metabolites; in 4 days 70% of the accepted quantity are removed (57% – intestines and 13% – kidneys).

Indications to use:

Treatment and prevention of the mycoses caused by microorganisms, sensitive to drug: infections of mucous membranes of digestive tract; the expressed damages of skin, hair and nails (a dermatofitiya, an onychomycosis, multi-colored deprive also others); chronic recurrent vaginal candidiasis in the absence of effect of local therapy; system mycoses (candidiasis, паракокцидиомикоз, histoplasmosis, кокцидиомикоз, zymonematosis).
Prevention of fungal infections at the weakened patients, including at patients with an immunodeficiency.

Route of administration and doses:

Drug is used internally during food. To adults and children with body weight more than 30 kg are appointed on 200 mg (1 tablet) of 1 times a day. Duration of treatment makes: at dermatomycoses – about 4 weeks; at multi-colored herpes – 10 days; at candidiasis of skin and oral cavity – 2–3 weeks; at onychomycoses – 6–12 months (before clinical and mycologic improvement); at system mycoses – 1–2 months. In the absence of significant improvement of a state against the background of administration of drug in a dose of 200 mg a day, the daily dose is increased to 400 mg (2 tablets). For children with the body weight from 15 to 30 kg the daily dose makes 100 mg (1/2 tablets). At vaginal candidiasis the daily dose makes 400 mg; therapy duration – 5 days. For prevention of fungal infections appoint adult 400 mg a day, to children – 4–8 mg/kg a day.

Features of use:

With care drug is appointed to patients with diseases of a liver or allergic reactions to medicines in the anamnesis, with dysfunctions of adrenal glands; in need of performing long therapy by Ketokonazol with simultaneous use of hepatotoxic drugs.
Purpose of drug during pregnancy and in the period of a lactation perhaps only if the estimated advantage for mother exceeds potential risk for a fruit or the child.
At a concomitant use of antiacid drugs they should be accepted not earlier than in 2 hours after Ketokonazol's reception.
After disappearance of symptoms of a disease treatment is continued within several days. In case of lack of effect after 4 weeks of treatment it is necessary to verify the diagnosis. At drug use over 2 weeks it is regularly necessary to control a pattern of peripheral blood, indicators of function of a liver.

Side effects:

From the central and peripheral nervous system: seldom – a headache, dizziness, paresthesias, photophobia, reversible increase in intracranial pressure.
From the alimentary system: seldom – nausea, vomiting; very seldom – reversible increase in level of transaminases, hepatitis.
From system of a hemopoiesis: seldom – thrombocytopenia.
From a reproductive system: seldom (at prolonged use in high doses) – inhibition of formation of androgens, a gynecomastia, an oligospermatism, disturbance of a menstrual cycle.

Interaction with other medicines:

Ketokonazol is incompatible with terfenadiny, astemizoly, alcohol. Antacids, cholinolytics, H2 blockers considerably reduce its absorption. Rifampicin, an isoniazid, рифабутин, carbamazepine, Phenytoinum reduce its concentration in plasma. At simultaneous use with ketokonazoly increase in plasma of concentration of cyclosporine, indirect anticoagulants, HIV protease inhibitors (инданавир, саквинавир), some antineoplastic drugs (Vincristinum, дисульфан, dotsetakset), blockers of calcium channels (nifedipine, verapamil), and also digoxin, carbamazepine, a buspiron, alfentanil, a sildenafil, an alprazolam, midazolam, a rifabutin, Methylprednisolonum, a trimeksat in plasma is possible.

Contraindications:

Hypersensitivity to a ketokonazol. The expressed abnormal liver functions. Concomitant use of a terfenadin, astemizol, tsisaprid, triazolam, quinidine, Pimozidum, HMG-CoA reductase inhibitors (симвастатин, ловастатин).

Overdose:

At overdose of drug strengthening of side effects is possible. Treatment: gastric lavage, symptomatic therapy.

Storage conditions:

To store in the dry, protected from light place at a temperature from 15 °C to 25 °C. To store in the place, unavailable to children.

Period of validity – 3 years.

Issue conditions:

According to the recipe

Packaging:

No. 10 or No. 30 (3x10) in blister strip packagings.