Clotrimazolum ointment

General characteristics. Structure:

Active ingredient: 10 mg of Clotrimazolum on 1 g

Excipients: a macrogoal cetostearyl ether, cetostearyl alcohol, paraffin white soft, oil mineral, propylene glycol, chlorcresol, sodium hydrophosphate a dihydrate, fragrance (Creamatest P3078), the water purified.

Antifungal means for topical administration for the treatment of infections of skin and mucous membranes caused by fungal activators.

Pharmacological properties:

Pharmacodynamics. Clotrimazolum suppresses growth and division of microorganisms and, depending on concentration, can have fungistatic or fungicidal effect. The mechanism of action of Clotrimazolum is connected with change of permeability of cellular membranes due to influence on synthesis of ergosterol and linkng with phospholipids of a cell wall of mushrooms. Clotrimazolum suppresses protein synthesis, fats, DNA, polysaccharides, damages nucleic acids in cells of mushrooms and accelerates potassium removal. Also it can suppress activity of oxidatic and peroksidantny enzymes and biosynthesis of triglycerides and phospholipids in cells of mushrooms. In higher concentration Clotrimazolum causes damage of cellular membranes on the mechanisms which are not depending on synthesis of sterol. Clotrimazolum prevents transformation Candida albicans blastospor in invasive forms of a mycelium. Change of activity of a cellular membrane leads to death of cells, and this process depends on contact of drug with microbes.

Clotrimazolum is characterized by a wide range of antifungal and antibacterial activity. It is active in the relation: dermatophytes (Epidermophyton floccosum, Microsporum canis, Trichophyton mentagrophytes, Trichophyton rubrum), yeast (Candida spp., Cryptococcus neoformans), dimorphous mushrooms (Coccidioides immitis, Histoplasma capsulatum, Paracoccidioides brasiliensis), elementary (Trichomonas vaginalis).

Also Clotrimazolum is active concerning some gram-positive bacteria.

In vitro Clotrimazolum is characterized by a wide range of fungistatic and fungicidal activity. It influences a mycelium of dermatophytes (Trichophyton, Microsporum, Epidermophyton) similar to griseofulvin, its action on the budding drozhzhepodobny mushrooms (Candida) is similar to effect of polyenes (Amphotericinum In and nystatin).

In concentration less than 1 mkg/ml Clotrimazolum suppresses development of the majority of strains of the disease-producing mushrooms relating to Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis.

In concentration of 3 mkg/ml Clotrimazolum suppresses development of the majority of other bacteria: Pityrosporum orbiculare, Aspergillus fumigatus, sorts Candida, including Candida albicans, some strains of Staphylococcus aureus, Streptococcus pyogenes, and also some strains of Proteus vulgaris and Salmonella. Clotrimazolum is active concerning Sporothrix, Cryptococcus, Cephalosporium, Fusarium.

In concentration more than 100 mkg/ml it is effective concerning Trichomonas vaginalis.

The mushrooms steady against Clotrimazolum meet extremely seldom; there are Candida guilliermondii given only on separate strains.

It was not reported about development of stability in mushrooms, sensitive to Clotrimazolum, after a passage of Candida albicans and Trichophyton mentagrophytes. Cases of development of resistance to Clotrimazolum in strains of Candida albicans steady against half-yen antibiotics owing to a chemical mutation are not described.

Pharmacokinetics. Clotrimazolum after use on skin is soaked up in quantity not exceeding 1%, but gets into a rogovy layer of epidermis and there collects. In insignificant degree it is soaked up from mucous membranes (to 3%). The absorbed drug is metabolized in a liver and removed by kidneys; half-life makes 3-5 hours.

Indications to use:

Fungus diseases of skin, mycoses of skin folds, feet; the chromophytosis, an erythrasma, superficial candidiases caused by dermatophytes, barmy (including the sort Candida), the mold and other mushrooms and activators sensitive to Clotrimazolum; the mycoses complicated by a secondary pyoderma.

Route of administration and doses:

Outwardly. Put with a thin layer 2-3 times a day on previously cleared (using soap with neutral value рН) and dry affected areas of skin and carefully rub. Duration of treatment depends on disease severity, localization of pathological changes and efficiency of therapy.

Treatment of dermatomycoses is carried out by not less than 4 weeks, a chromophytosis of-1-3 weeks.

At fungus diseases of skin of legs therapy is recommended to be continued within not less than 2 weeks after elimination of symptoms of a disease.

Features of use:

Prevention of spread of an urogenital infection requires simultaneous treatment of sexual partners. At trichomoniasis for more successful treatment together with Clotrimazolum it is necessary to appoint other medicines possessing systemic action (for example, metronidazole inside).

Vaginal tablets are not recommended to be applied during periods.
In case of an unforeseen route of administration of drug the following symptoms - anorexia, nausea, vomiting, a gastralgia, an abnormal liver function, seldom drowsiness, hallucinations, a pollakiuria, skin allergic reactions are (orally) possible. In a verse situations it is necessary to accept absorbent carbon and to see a doctor.

At a razvivitiya of allergic reactions or irritations, treatment it is necessary to stop and pick up other therapy.

At a dermatomycosis of feet use of solution after each washing of feet is recommended.
Putting drug on skin in eyes is not recommended.

If in 4 weeks from an initiation of treatment clinical improvement is noted, it is necessary to confirm the diagnosis microbiological and to exclude other cause of illness.

Does not influence the speed of reactions at an uparvleniya by vehicles and other mechanisms.

Drug is contraindicated to children.

It is contraindicated in 1 trimester of pregnancy, and in 2 and 3 trimesters harm advantage on an organism of mother and a fruit is applied after the analysis of a ratio.

Side effects:

In certain cases there can be local reactions - burning, a pricking, reddening, sometimes development of a dieback, allergic reaction. In case of development of any unusual reactions, it is necessary to suspend treatment by this drug.

 

Interaction with other medicines:

Reduces action of local half-yen antibiotics (Amphotericinum, nystatin, натамицин, etc.).

Propyl ether of para-hydroxybenzoic acid in high concentration strengthens antifungal action of Clotrimazolum, dexamethasone — reduces.

At simultaneous use with nystatin activity of Clotrimazolum can decrease.

Contraindications:

Hypersensitivity to Clotrimazolum, the I trimester of pregnancy, children's age.

Overdose:

Due to the low absorption of drug at topical administration the overdose is improbable.

Storage conditions:

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

Issue conditions:

Without recipe

Packaging:

On 20 g of ointment in aluminum tubas on 1 tuba in a cardboard box.