Ketokonazol of levers. candles 0,4 No. 5
Producer: CJSC Lekhim-Kharkiv Ukraine
Code of automatic telephone exchange: G01A F11
Release form: Firm dosage forms. Suppositories vaginal.
General characteristics. Structure:
International and chemical names: ketoconazole; tsis-1-atsetil-4-[4-[[2-(2,4 dichlorophenyl)-2-(1H-imidazole-1-илметил) - 1,3-dioxolane-4-silt] metoks] phenyl] piperazin; main physical and chemical properties: suppositories of white or almost white color, cigar-shaped form; existence of a plaque on the surface of suppository is allowed.
structure: 1 suppository contains a ketokonazol – 0,4 g;
excipients: solid fat.
Pharmacological properties:
Pharmacodynamics. Antifungal broad-spectrum agent – derivative an imidazoldioksolana. The mechanism of pharmacological properties is caused by ability to have the damaging effect on a cellular membrane of mushrooms as a result of ergosterol biosynthesis oppression. It leads to braking of processes of cellular respiration of mushrooms, disturbance of their transformation in micellar forms, to suppression of capture of purines, disturbance of biosynthesis of phospholipids in a cellular membrane. High concentration of a ketokonazol have fungicidal effect. Resistance to a ketokonazol does not develop.
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. At intravaginalny use small amounts of a ketokonazol come to a system blood stream. The maximum concentration in a blood plasma at women after intravaginalny use of 400 mg of a ketokonazol fluctuates in limits
0-20,7 ng/ml.
Indications to use:
Acute and chronic mycosis of a vagina; prevention of fungal infections of a vagina at the lowered resistance of an organism and against the background of treatment by the antibacterial agents and other drugs breaking normal microflora of a vagina.
Route of administration and doses:
Intravaginalno, deeply, in a dorsal decubitus, on 1 suppository a day within 3-5 days. If necessary the course is repeated before the absolute clinical recovery confirmed with laboratory researches.
Features of use:
With care to apply at pregnant women, when breastfeeding. Experience of use of drug for treatment of children and teenagers is absent.
Before use of drug it is necessary to wash up hands. It is necessary to avoid contact of suppository with products from latex (contraceptive diaphragms, condoms).
Side effects:
Local allergic reactions (itch, burning) are possible. In rare instances – nausea, dizziness.
Interaction with other medicines:
Increases concentration in plasma of cyclosporine, indirect anticoagulants, Methylprednisolonum. Rifampicin, an isoniazid reduce concentration of a ketokonazol in plasma at simultaneous use.
Contraindications:
Individual hypersensitivity to drug components.
Overdose:
Cases of overdose are not revealed.
Storage conditions:
In the place protected from light at a temperature from +8ºС to +15ºС.
Period of validity - 2 years.
Issue conditions:
According to the recipe
Packaging:
On 5 suppositories in a blister strip packaging, on 1 or 2 blister strip packagings in a pack cardboard.