Clotrimazole medicine for what. Use during pregnancy and lactation. Repeated treatment with Clotrimazole is prescribed by a doctor

Clotrimazole is a widely used synthetic antifungal drug for external use.

pharmachologic effect

The active substance Clotrimazole has an antifungal effect against:

• Candidaalbicans;
• Malasseziafurfur;
• Cryptococcus neoformans;
• Coccidioidesimmitis;
• Trichophyton;
• Blastomyces dermatitidis;
• Sporothrix schenckii;
• epidermophyton;
• microsporum;
• Aspergillus.

According to the instructions, Clotrimazole has a very high penetrating power and also exhibits antitrichomonas, antibacterial (gram-positive microorganisms, in particular, staphylococci, streptococci, and less pronounced corynebacteria) and antiamebic (cysts of pathogenic negleria) action.

Release form

Clotrimazole is produced in various dosage forms:

• White biconvex homogeneous, in the form of a parallelepiped with rounded edges vaginal tablets Clotrimazole (Clotrimazole suppositories), containing 100 mg of the active substance - clotrimazole. 6 pieces in a blister;
• white homogeneous antifungal ointment Clotrimazole for external use. 1 g of ointment contains 10 mg of active ingredient. In tubes of 30 g;
• 1% cream Clotrimazole, applied externally, in tubes of 20 g;
• 2% cream Clotrimazole vaginal, in tubes of 50 g;
• 1% solution for external use in orange bottles, 15 ml and 30 ml.

Indications for use Clotrimazole

According to the instructions, Clotrimazole is used for fungal diseases of the skin, mucous membranes, mycoses. skin folds and stop:

• Epidermophytosis;
• Erythrasma;
• Dermatomycosis;
• Genital infections and superinfections (vulvovaginal candidiasis, trichomoniasis);
• Candidiasis;
• Superficial candidiasis caused by various types of fungi sensitive to clotrimazole;
• Dermatophytosis;
• stomatitis;
• Mycoses, complicated secondary pyoderma;
• Pityriasis versicolor;
• Microsporia.

Candles Clotrimazole ( vaginal tablets Clotrimazole) is used for sanitation birth canal before childbirth, as well as to prevent infection before operations on the genitals.

Contraindications

Clotrimazole has a small list of contraindications.

The drug is not used for hypersensitivity to clotrimazole or other components of the drug, as well as in the first trimester of pregnancy.

In the second or third trimesters of pregnancy and during lactation, Clotrimazole tablets are used with caution strictly according to indications.

Instructions for use Clotrimazole

Clotrimazole vaginal tablets are usually injected into the vagina in the evening, as deep as possible in the supine position. To do this, use the applicator included in the package. The course is - 1 candle Clotrimazole daily for 6 days.

Re-treatment Clotrimazole is prescribed by a doctor.

With candidal vulvitis or candidal balanitis, suppositories are used simultaneously with Clotrimazole cream, which is applied externally several times a day to the affected areas for one to two weeks. With trichomoniasis, it is recommended to combine the use of Clotrimazole suppositories with chemotherapeutic medicines inside (metronidazole).

Clotrimazole ointment for external use is applied to clean, affected areas of the skin. thin layer several times a day, gently rubbing. The duration of treatment depends on the location, severity of the disease and the effectiveness of therapy:

• Dermatomycosis is treated for at least a month;
• Pityriasis versicolor - up to three weeks;
• Fungal diseases of the skin of the legs - therapy is continued for at least two weeks after the symptoms have passed.

Clotrimazole cream can also be used to treat these diseases.

After applying Clotrimazole ointment, sealing dressings should not be applied.

Side effects

With external use of Clotrimazole ointment, edema may occur, as well as burning, peeling or skin irritation, itching, erythematous rashes, paresthesia, blistering or urticaria.

When using Clotrimazole suppositories, burning, itching, swelling of the mucous membrane are possible. Also, sometimes when using Clotrimazole suppositories, according to the instructions, vaginal discharge appears, urination becomes more frequent, intercurrent cystitis occurs, and pain during intercourse and a burning sensation in the partner's penis may also occur.

According to reviews frequent use clotrimazole cream may occur headache and gastralgia.

Storage conditions

Clotrimazole is available without a prescription.

Sincerely,

Self-medication can be harmful to your health.
It is necessary to consult a doctor, and also read the instructions before use.

Clotrimazole cream: instructions for use

Compound

1 g of cream contains:

active ingredient: kpotrimazole 0.01 g

excipients: benzyl alcohol, cetasteryl alcohol,

octyldodecanol, polysorbate 60, sorbitan stearate, synthetic cetaceum (ester cetyl wax), purified water.

Description

Homogeneous mass of white.

pharmachologic effect

Kpotrimazole is a broad-spectrum antifungal agent for topical use. The antimycotic effect of the active active substance (imidazole derivative) is associated with a violation of the synthesis of ergosterol, which is part of cell membrane fungi, which changes the permeability of the membrane and causes subsequent cell lysis. In small concentrations, it acts fungistatically, and in large concentrations, it acts fungicidal, and not only on proliferating cells. In fungicidal concentrations, it interacts with mitochondrial and peroxidase enzymes, resulting in an increase in the concentration of hydrogen peroxide to a toxic level, which also contributes to the destruction of fungal cells. Effective against dermatophytes, yeast-like and mold fungi, as well as the pathogen versicolor Pityriasis versicolor (Malazessia furfur) and the causative agent of erythrasma. It has an antimicrobial effect against gram-positive (staphylococci, streptococci) and gram-negative bacteria (Bacteroides, Gardnerella vaginalis), as well as against Trichomonas vaginalis.

Pharmacokinetics

Kpotrimazole is poorly absorbed through the skin and mucous membranes and has practically no systemic effect. The concentration in the deep layers of the epidermis is higher than the minimum inhibitory concentration for dermatophytes.

When applied externally, the concentration of clotrimazole in the epidermis is higher than in the dermis and subcutaneous tissue.

Indications for use

Fungal diseases of the skin, mycoses of skin folds, feet;

Pityriasis versicolor, erythrasma, superficial candidiasis caused by dermatophytes, yeasts (including the genus Candida), molds and other fungi and pathogens sensitive to clotrimazole;

Mycoses complicated by secondary pyoderma.

Contraindications

Hypersensitivity to clotrimazole or excipients, I trimester of pregnancy.

With caution - lactation.

Pregnancy and lactation

With clinical and experimental studies It has not been established that the use of the drug during pregnancy or during lactation has bad influence on the health of a woman or a fetus (child). However, the question of the advisability of prescribing the drug should be decided individually after consulting a doctor.

Applying the drug directly to the lactating mammary gland contraindicated.

Dosage and administration

Outwardly. The cream is applied in a thin layer 2-3 times a day on previously cleansed (using soap with a neutral pH value) and dry affected areas of the skin and rubbed gently.

The duration of treatment depends on the severity of the disease, localization pathological changes and effectiveness of therapy.

Treatment of dermatomycosis is carried out for at least 4 weeks, pityriasis versicolor- 1-3 weeks.

In case of fungal diseases of the skin of the legs, it is recommended to continue therapy for at least 2 weeks after the symptoms of the disease have disappeared.

Side effect

Itching, burning, tingling at the site of application of the cream, the appearance of erythema, blisters, swelling, irritation and peeling of the skin. Allergic reactions (itching, urticaria).

Overdose

The use of the cream in higher doses does not cause any reactions and conditions that are life-threatening.

Interaction with other drugs

Amphotericin B, nystatin, natamycin reduce the effectiveness of clotrimazole with simultaneous use.

When applying the cream negative interactions with other means are not known and should not be expected, tk. the resorption capacity of clotrimazole is very low.

Application features

It is not recommended to apply the drug to the skin in the eye area. In patients with liver failure should be checked periodically functional state liver. If signs of hypersensitivity or irritation appear, treatment is stopped. If there is no effect within 4 weeks, the diagnosis should be confirmed.

Precautionary measures

Release form

Antifungal agent for topical use from the group of imidazole derivatives.

White crystalline substance without smell. Practically insoluble in water, sparingly soluble in ether, very soluble in polyethylene glycol 400, ethanol and chloroform. Molecular mass 344,84.

Pharmacology

Violates the synthesis of ergosterol (the main structural component of the fungal cell membrane), changes the permeability of the fungal membrane, promotes the release of potassium, intracellular phosphorus compounds from the cell and the breakdown of cellular nucleic acids. Inhibits the synthesis of triglycerides and phospholipids. It reduces the activity of oxidative and peroxidase enzymes, as a result of which the intracellular concentration of hydrogen peroxide rises to a toxic level, which contributes to the destruction of cell organelles and leads to cell necrosis. Depending on the concentration, it exhibits a fungicidal or fungistatic effect. Inhibits blastospore transformation candida albicans into an invasive mycelial form.

Clotrimazole acts mainly on growing and dividing microorganisms. In vitro exhibits fungicidal and fungistatic activity against dermatomycetes (Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis), yeast-like fungi Candida spp.(including candida albicans). Active against the causative agent of multi-colored lichen - Pityrosporum orbiculare(Malassezia furfur).

Fungal strains with natural resistance to clotrimazole are rare. Primary resistance to clotrimazole has only been described for Candida guillermondii.

Effective against gram-positive bacteria - the causative agent of erythrasma Corynebacterium minutissimum, as well as Staphylococcus spp., Streptococcus spp., gram-negative bacteria Bacteroides, Gardnerella vaginalis. AT high concentrations active against Trichomonas vaginalis.

It is poorly absorbed through the skin and mucous membranes.

It accumulates in the stratum corneum of the epidermis, the concentration in the deep layers of the epidermis is higher than the MIC for dermatomycetes. When applied to the nails, it is found in keratin.

With intravaginal administration, 3-10% of the dose is absorbed.

In the liver, it is rapidly biotransformed to inactive metabolites and excreted in the faeces. Absorbed clotrimazole induces the activity of microsomal liver enzymes, which leads to an acceleration of its catabolism.

High concentrations in vaginal secretions and low concentrations remain in the blood for 48-72 hours.

Carcinogenicity, mutagenicity, effect on fertility

There was no evidence of carcinogenicity of clotrimazole in a study in rats given it orally for 18 months. Long-term studies in animals to evaluate the potential carcinogenicity of clotrimazole when administered intravaginally have not been conducted.

A study of mutagenicity in Chinese hamsters, which received 5 doses of clotrimazole at 100 mg/kg orally, did not reveal a mutagenic effect - structural changes during metaphase in spermatophore chromosomes.

Pregnancy. In studies in pregnant rats with intravaginal doses of clotrimazole up to 100 mg / kg, no adverse effects on the fetus were found. However, daily oral intake clotrimazole at doses of 50 to 120 mg/kg resulted in embryotoxicity in rats and mice (possibly secondary to maternal toxicity). So, in mice, when taking clotrimazole in doses 120 times higher than usual dose in humans, in the period from 9 weeks before mating to the end of feeding, a violation of mating, a decrease in the number of viable cubs, and a decrease in the survival rate of offspring from birth to the end of feeding were recorded. At doses up to 60 times the usual human dose, no adverse effects were observed. In rats at doses 50 times the usual human dose, clotrimazole, at a similar time period of observation, caused a slight decrease in the number of pups in the offspring and a decrease in their survival. No teratogenic effect was found in mice, rabbits and rats when taking clotrimazole orally at doses up to 200, 180 and 100 mg/kg, respectively.

The use of the substance Clotrimazole

Fungal lesions of the skin and mucous membranes: ringworm, dermatophytosis, trichophytosis, epidermophytosis, microsporia, candidiasis, interdigital fungal erosion, fungal paronychia; mycoses complicated by secondary pyoderma; versicolor versicolor, erythrasma; candidal stomatitis; candidal vulvitis, vulvovaginitis, balanitis, trichomoniasis; for sanitation of the birth canal before childbirth.

Contraindications

Hypersensitivity.

Use during pregnancy and lactation

It should not be used in the first trimester of pregnancy (no adequate and well-controlled studies have been conducted). With intravaginal use in women in II and III trimesters pregnancy, no adverse effect on the fetus has been identified, however, the use of a vaginal applicator is undesirable.

With caution - during breastfeeding(it is not known whether clotrimazole penetrates into breast milk).

Side effects of the substance Clotrimazole

Allergic reactions (itching, urticaria).

At topical application on the skin: erythema, blistering, swelling, burning and tingling, irritation and peeling of the skin.

When applied topically to treat urogenital infections: itching, burning, hyperemia and swelling of the mucous membrane, vaginal discharge, frequent urination, intercurrent cystitis, burning sensation in the partner's penis, pain during intercourse.

When applied topically in the oral cavity: redness of the oral mucosa, burning sensation and tingling at the site of application, irritation.

Interaction

Reduces the activity (mutually) of polyene antibiotics (amphotericin B, nystatin, natamycin).

Overdose

In case of accidental ingestion of drugs inside, the following are possible: symptoms: anorexia, nausea, vomiting, gastralgia, liver dysfunction; rarely - drowsiness, hallucinations, pollakiuria, skin allergic reactions.

Treatment: taking activated charcoal, symptomatic therapy.

Routes of administration

locally.

Precautions of the substance Clotrimazole

Avoid getting drugs on the mucous membrane of the eyes. Avoid application on areas with violation of the integrity of the skin.

After applying the cream, do not use airtight bandages.

It is recommended to prevent reinfection simultaneous treatment sexual partner. Do not prescribe intravaginally during menstruation. With trichomoniasis, a combined intake with systemic chemotherapeutic agents (metronidazole orally) is recommended.

In patients with impaired liver function, its functional state should be periodically monitored.

The appearance of irritation or signs of hypersensitivity requires discontinuation of treatment.

If there is no clinical improvement within 4 weeks, a microbiological research to confirm the diagnosis and exclude another cause of the disease.

Interactions with other active substances

Trade names

Name:

Clotrimazole (Clotrimazole)

Pharmacological
action:

Clotrimazole is a topical antifungal drug from the group of imidazole derivatives.
In vitro has wide range action, covering almost all pathogenic fungi that cause infection in humans, namely:
- dermatophytes (Epidermophyton floccosum, Microsporum sp., Trichophyton sp.)
- blastomycoses and molds (Candida sp., Cryptococcus neofo Torulosis sp., Aspqrgillus sp., Cladosporium sp., Madurella sp.)
- dimorphic fungi (Blastomyces dermatitidis, Coccidioides immitis, Histoplasma capsulatum)
- as well as actinomycetes from the Nocardia family.
In small concentrations, the drug acts fungistatically, in large concentrations it is fungicidal.
The mechanism of action is inhibition of ergosterol synthesis, the main element of the structure cell wall in fungi, its absence causes significant changes in the structure and properties of the shell.
The increased permeability of the membrane leads to lysis of the fungal cell, which additionally facilitates the accumulation of 14 L methylsterols inside the cell, which are precursors in the synthesis of ergosterol.
In addition, clotrimazole inhibits the activity of peroxidases (including mitochondrial ones), which additionally facilitates the accumulation of hydrogen peroxide in the fungal cell, most likely participating in its destruction.
In addition to the antimycotic action, clotrimazole also exhibits the action of:
- antibacterial (covers gram-positive microorganisms, in particular, staphylococci and streptococci, to a lesser extent corynebacteria)
- antitrichomonas (Trichomonas vaginalis).
- anti-amoebic (Naegleria fowleri).

Indications for
application:

Genital infections caused by yeast fungi of the genus Candida and/or Trichomonas vaginalis(vulvovaginal candidiasis, trichomoniasis), genital superinfections caused by bacteria sensitive to clotrimazole.

special instructions
To prevent the spread of urogenital infection, simultaneous treatment of sexual partners is necessary. With trichomoniasis for more successful treatment together with clotrimazole, other medicines having systemic action(eg, metronidazole by mouth).
Vaginal tablets are not recommended for use during menstruation.
In the case of an unintended method of using the drug (orally), the following symptoms- anorexia, nausea, vomiting, gastralgia, liver dysfunction, rarely drowsiness, hallucinations, pollakiuria, allergic skin reactions. In these situations, it is necessary to take Activated carbon and see a doctor.

Mode of application:

locally, apply a thin layer on the affected areas of the skin and mucous membranes 2-4 times a day. The course of treatment is selected individually, usually at least 4 weeks; upon its completion (disappearance clinical manifestations) it is advisable to continue the use of the drug for another 14 days. The duration of therapy for erythrasma is 2-4 weeks, for lichen multi-colored - 1-3 weeks.

Before lubrication, the feet are washed warm water with soap, wipe thoroughly, especially between the fingers. In case of fungal diseases of the skin of the legs, it is recommended to continue treatment after reaching therapeutic effect within 2–3 weeks.

Locally in the oral cavity: 10-20 drops (0.5-1 ml) of topical solution are applied to the affected areas of the oral mucosa with a cotton swab / stick 3-4 times a day. Improvement usually occurs on the 3rd-5th day of treatment; treatment should be continued until the complete elimination of the clinical manifestations of the disease.

Locally for urogenital infections. With candidal vulvitis or balanitis, use 2-3 times a day for 1-2 weeks. For the treatment of trichomoniasis, vaginitis in adults and adolescents: vaginal tablets (500 mg once or 200 mg for 3 days or 100 mg for 6-7 days, 1 time per day, in the evening), or cream (full applicator) is administered as soon as possible deeper into the vagina 1 time per day (before going to bed). For sanitation of the birth canal, a single administration of the tablet is recommended.

With urethritis, an instillation of a 1% solution of clotrimazole into the urethra is also carried out for 6 days.

Precautions for the substance Clotrimazole:

Should avoid getting drugs on the mucous membrane of the eyes. Avoid application on areas with violation of the integrity of the skin.

After applying the cream, do not use airtight bandages.

For the prevention of reinfection, simultaneous treatment of the sexual partner is recommended. Do not prescribe intravaginally during menstruation. With trichomoniasis, a combined intake with systemic chemotherapeutic agents (metronidazole orally) is recommended.

In patients with impaired liver function, its functional state should be periodically monitored.

The appearance of irritation or signs of hypersensitivity requires discontinuation of treatment.

In the absence of clinical improvement within 4 weeks, a microbiological study should be performed to confirm the diagnosis and exclude another cause of the disease.

Side effects:

Allergic reactions (itching, urticaria).

When applied topically to the skin: erythema, blistering, swelling, burning and tingling, irritation and peeling of the skin.

When applied topically to treat urogenital infections: itching, burning, hyperemia and swelling of the mucous membrane, vaginal discharge, frequent urination, intercurrent cystitis, burning sensation in the partner's penis, pain during intercourse.

When applied topically in the oral cavity: redness of the oral mucosa, burning sensation and tingling at the site of application, irritation.

Contraindications:

Hypersensitivity or allergy to the components of the drug are a contraindication for the use of clotrimazole.

Interaction
other medicinal
by other means:

Clotrimazole may inhibit the action of other topical antifungal agents, especially polyene antibiotics(nystatin, natamycin).
Dexamethasone used in large doses, inhibits the antifungal action of clotrimazole. The antimycotic effect of clotrimazole is enhanced by high local concentrations of the propyl ester of p-hydroxybenzoic acid.