Clotrimazolum cream

General characteristics. Structure:

Cream for external use of 1% in the form of homogeneous mass of white color.

Active ingredient: Clotrimazolum of 1 g

Excipients: benzyl alcohol - 1 g, cetostearyl alcohol - 11.5 g, octyllauryl alcohol - 10 g, polysorbate of 60 - 1.5 g, sorbitan stearate - 2 g, spermaceti synthetic - 3 g, water - 71 g.

Pharmacological properties:

Clotrimazolum suppresses growth and division of microorganisms and, depending on concentration, can render fungistatic (detaining and stopping growth of cells of mushrooms) or fungicidal (leading to death of mushrooms) action. Clotrimazolum oppresses synthesis of ergosterol and contacts phospholipids of a cellular membrane of a mushroom that leads to change of permeability of membranes of cells.

In higher concentration Clotrimazolum causes damage of cellular membranes on the mechanisms which are not depending on synthesis of sterol.

Clotrimazolum also breaks processes of life activity in a mushroom cell, suppressing formation of the components necessary for creation of the vital cellular structures (proteins, fats, DNA, polysaccharides), damages nucleic acids and increases potassium removal.

Finally impact of Clotrimazolum on fungal cells leads to their death.

Clotrimazolum is characterized by a wide range of antifungal and antibacterial activity: 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 it is active concerning some gram-positive bacteria.

When studying efficiency of Clotrimazolum in vitro out of a human body (in vitro) the wide range of its fungistatic and fungicidal activity is revealed. It influences a mycelium of dermatophytes (Trichophyton, Microsporum, Epidermophyton) similar to griseofulvin, and its action on the budding 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. Absorption and distribution

Pharmacokinetic researches showed that Clotrimazolum is practically not soaked up in a system blood stream when putting drug on the unimpaired or inflamed sites of skin. Concentration of Clotrimazolum in blood serum were below a detection limit (0.001 mkg/ml), confirming the fact that Clotrimazolum at external use does not result in clinically significant system effects or side effects.

Metabolism and removal

Clotrimazolum breaks up in a liver to the inactive substances removed from an organism through kidneys and intestines.

Indications to use:

For outside treatment of the fungus diseases of skin caused by dermatophytes, drozhzhepodobny mushrooms, mold mushrooms, and also the activators sensitive to Clotrimazolum:

— mycoses of feet, brushes, trunks, skin folds;

— candidosis vulvitis, candidosis balanitis;

— multi-colored deprive, an erythrasma;

— fungal infections of an outside ear.

Route of administration and doses:

For external use. Cream should be applied on affected areas of skin 2-3

For prevention of a recurrence treatment should be continued, at least, within two weeks after disappearance of all symptoms of an infection.

Cream should be applied on pure dry sites of the affected skin (which is washed up by soap with a neutral rn), cream should be applied on feet between fingers.

Duration of treatment depends on disease severity, its localization, efficiency of treatment.

Treatment duration: dermatomycoses - 3-4 weeks; an erythrasma - 2-4 weeks; multi-colored deprive - 1-3 weeks; a candidosis vulvitis and a balanitis - 1-2 weeks.

Duration of treatment can change according to specific features, but treatment duration is not recommended less than 3 weeks. For prevention of a recurrence of an infection it is necessary to continue use of drug within 1-2 weeks after disappearance of all symptoms of a disease. If after 7 days of treatment there does not occur improvement of symptomatology, it is necessary to consult with the doctor.

Features of use:

It is necessary to avoid hit of cream on a mucous membrane of eyes. Not to swallow.

All infected areas it is necessary to treat at the same time.

Cetostearyl alcohol which can cause local skin reactions is a part of the drug Clotrimazolum (for example, contact dermatitis).

At emergence of symptoms of hypersensitivity or irritation treatment is stopped.

Data of laboratory researches demonstrate that use of the contraceptives containing latex can cause their damage at combined use with Clotrimazolum. Therefore, efficiency of such contraceptives can decrease. Patients should recommend use of alternative methods of contraception during, at least, 5 days after use of Clotrimazolum.

Influence on ability to driving of motor transport and to control of mechanisms

It was not reported about influence of Clotrimazolum on ability to manage vehicles and mechanisms.

Side effects:

The undesirable phenomena given below are listed according to defeat of bodies and systems of bodies and occurrence frequency. Frequency of occurrence is defined as follows: very often (≥1/10), it is frequent (≥1/100 and <1/10), infrequently (≥1/1000 and <1/100), is rare (≥1/10 000 and <1/1 000), is very rare (<1/10 000, including separate cases), it is unknown (frequency cannot be estimated according to the data which are available currently). Categories of frequency were created on the basis of post-registration observation.

From immune system: it is unknown - the allergic reaction (which is shown urticaria, a faint, arterial hypotension, an asthma).

From skin and hypodermic fabrics: it is unknown - rash, an itch, bubble rashes, a peeling, pain or discomfort, hypostasis, burning, irritation.

Interaction with other medicines:

It was not studied.

Contraindications:

— hypersensitivity to Clotrimazolum or other components of drug.

 

Drug CLOTRIMAZOLUM use cream at pregnancy and feeding by a breast

Use of the drug Clotrimazolum at pregnancy is allowed only if, according to the doctor, the potential advantage of use of cream for mother exceeds possible risk of a fruit.

In the conducted epidemiological researches the undesirable phenomena concerning pregnancy or health of a fruit are not revealed at drug Clotrimazolum use.

Use of the drug Clotrimazolum for women during breastfeeding is allowed only if, according to the doctor, the potential advantage of use of cream for mother exceeds possible risk for the child.

Fertility

Data are not available.

Overdose:

Symptoms: at accidental administration of drug emergence of dizziness, nausea, vomiting is inside possible.

Treatment: at accidental reception of cream inside it is necessary to carry out a symptomatic treatment. At external use of drug the overdose is improbable.

Storage conditions:

Drug follows in the place, unavailable to children, at a temperature not above 25 °C. Not to freeze. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

20 g - aluminum (1) - packs cardboard.