Clotrimazolum

General characteristics. Structure:

Active ingredient: 100 mg of Clotrimazolum

Excipients: lactoses monohydrate, potato starch, adipic acid, Natrii hydrocarbonas, magnesium stearate, silicon dioxide colloid, sodium lauryl sulfate.

It is applied in gynecology at the genital infections caused by barmy mushrooms of the sort Candida i Trichomonas vaginalis.

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. Pharmacokinetic researches of Clotrimazolum at intravaginalny use showed that absorption makes 3-10% of the entered dose. In a liver Clotrimazolum is metabolized to pharmacological inactive metabolites, in this regard its concentration in a blood plasma at intravaginalny introduction in a dosage of 500 mg makes less than 10 ng/ml, confirming the fact that Clotrimazolum at intravaginalny introduction does not result in significant system effects or side effects.

Clotrimazolum is generally metabolized in a liver to the metabolites removed through kidneys and intestines.

Indications to use:

The genital infections caused by barmy mushrooms of the sort Candida and/or Trichomonas vaginalis (a candidosis vulvovaginitis, trichomoniasis).

Route of administration and doses:

For intravaginalny use. Appoint on 1 таб. 2 times/days within 3 days or on 1 таб. For 1 times/days within 6-7 days, it is desirable before going to bed.

In the absence of effect within 3 days it is necessary to confirm the diagnosis.

If symptoms remain more than 7 days, observation of the doctor is necessary.

Treatment can be repeated if necessary, however recurrent infections can testify to the cornerstone pathology, including a diabetes mellitus or HIV infection.

If symptoms arise repeatedly within 2 months, the patient has to consult with the doctor.

In case of simultaneous infection of a vulva and adjacent sites outside treatment with cream use is necessary.

Full dissolution of vaginal tablets requires normal humidity mucous vaginas. At women with dryness mucous vaginas not dissolved parts of a tablet can be allocated outside. For prevention of it it is necessary to enter a tablet whenever possible more deeply into a vagina before going to bed.

Treatment during periods is not recommended because of risk of a vymyvananiye of a tablet, it needs to be completed to periods.

For sanitation of patrimonial ways once 1 tablet just before childbirth.

For children over 12 years a route of administration same, as well as at adults.

The drug Tablet Clotrimazolum vaginal is not recommended to be used to children 12 years are younger.

The repeated course of therapy is possible according to medical indications.

Features of use:

In case of purpose of drug of the pregnant woman, she needs to be warned that at introduction of vulval tablets it is impossible to use an applicator. Not to apply vulval tablets during periods. Prevention of reinfection requires simultaneous treatment of both sexual partners. For successful treatment of patients from trichomoniasis together with Clotrimazolum appoint other medicines which have systemic action, for example, metronidazole internally.

Use of Clotrimazolum does not influence speed of response at control of motor transport or work with other mechanisms.

Do not apply to children up to 12 years.

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: allergic reactions (urticaria, faints, arterial hypotension, asthma).

From a GIT: abdominal pain.

From generative organs and a mammary gland: it is unknown - discomfort in a vulva and a vagina, a hyperemia and hypostasis of a mucous membrane of a vagina, allocation from a vagina, burning, a peeling, irritation, an itch, pain in a small pelvis, a burning sensation in a penis at the sexual partner, pain during sexual intercourse, rash. At emergence of these symptoms therapy by Clotrimazolum needs to be stopped.

From a nervous system: headache.

From kidneys and urinary tract: the speeded-up urination, intercurrent cystitis.

Interaction with other medicines:

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

The accompanying use of Clotrimazolum vaginalno and a takrolimusa (FK-506; the immunosuppressant) can orally lead to increase in concentration of a takrolimus in plasma. It is necessary to watch carefully patients concerning symptoms of overdose of a takrolimus with measurement of concentration of drug in case of need.

Amphotericinum In, nystatin, натамицин reduce efficiency of Clotrimazolum at their simultaneous use.

Contraindications:

— hypersensitivity to Clotrimazolum or other components of drug;

— age up to 12 years;

— periods period.

With care

At the first case of a mycotic vulvovaginitis it is necessary to consult with the doctor.

At identification of any of the listed below factors before purpose of the vaginal tablets Clotrimazolum it is necessary to consult with the doctor:

— more than two episodes of a mycotic vulvovaginitis in the previous 6 months;

— existence in the anamnesis of diseases, sexually transmitted, or contact with the partner having a disease, sexually transmitted;

— the proved or alleged pregnancy;

— the age is more senior than 60 years;

— existence in the anamnesis of hypersensitivity to imidazoles or other antifungal drugs for vaginal use.

Overdose:

Use of Clotrimazolum in the raised doses does not cause any reactions and states which would threaten life. Due to the low absorption of drug the overdose is improbable. At hypersensitivity and overdose allergic reactions are possible.

At identification of symptoms of overdose, use of drug is stopped and appoint a symptomatic treatment.

Storage conditions:

To store in the place, dry, unavailable to children, at a temperature not above 25 degrees Celsius.

Issue conditions:

According to the recipe

Packaging:

On 6 vaginal tablets in the blister. On 1 blister in cardboard packaging together the applicator.