Antifungal Clotrimazole ointment: methods of use. Clotrimazole ointment for the treatment of thrush and other mycoses. What is clotrimazole ointment used for?

Clotrimazole is a drug for external and local use with antifungal, antibacterial, antiprotozoal and trichomonacid action.

Release form and composition

Clotrimazole is available in the following forms:

• Vaginal tablets - white, with a smooth surface, biconvex, oblong, rounded at one end, flat at the other (1, 3 or 6 pieces in blisters, in a cardboard pack 1 blister complete with an applicator);
• Cream for external use – a homogeneous white mass (20 g in aluminum tubes, 1 tube in a cardboard box);
• Ointment for external use – homogeneous, white or almost white (30 g in aluminum tubes, 1 tube in a cardboard box);
• Gel for external use – homogeneous, transparent, colorless, with the aroma of sage, air bubbles are allowed (20 and 40 g in aluminum tubes, 1 tube in a cardboard pack);
• Vaginal suppositories - cylindrical-conical, white or white with a yellowish tint, the presence of an air rod on the cut is allowed (6 pieces in contour strip packs, 1 pack in a cardboard pack);
• Solution for external use (15 ml in bottles with a dropper, 1 bottle in a cardboard box).

Active ingredient: clotrimazole:

• 1 suppository – 100 mg;
• 1 g of cream, ointment and gel – 10 mg;
• 1 tablet – 100, 200 or 500 mg;
• 1 ml of solution – 10 mg.

Auxiliary components:

• Tablet: potato starch, lactose monohydrate, magnesium stearate, sodium lauryl sulfate, sodium bicarbonate, adipic acid, colloidal silicon dioxide;
• Cream: cetostearyl alcohol, benzyl alcohol, polysorbate 60, octyldodecanol, sorbitan stearate, synthetic spermaceti, water;
• Ointment: propylene glycol, polyethylene oxide 400, polyethylene oxide 1500, methylparaben, nipagin;
• Gel: rectified 96% ethyl alcohol, propylene glycol, macrogol 400, carbomer, glycerol, sage essential extract;
• Suppositories: semi-synthetic glycerides;
• Solution: anhydrous ethanol, isopropyl myristinate.

Indications for use

Clotrimazole in the form of vaginal tablets and suppositories is prescribed to women and teenage girls (after the onset of sexual activity) for the following diseases:

• Infections of the genital organs that are caused by fungi of the genus Candida, including infections caused by nystatin-resistant strains;
• Vaginitis and vulvovaginitis caused by fungi of the genus Candida;
• Genital superinfections caused by microorganisms sensitive to clotrimazole;
• Sanitation of the birth canal in pregnant women before childbirth.

The drug in dosage forms for external use (cream, ointment, gel and solution) is used to treat fungal infections of the skin and mucous membranes caused by mold and yeast-like fungi, dermatophytes and other pathogens sensitive to clotrimazole:

• Mycoses of the trunk, feet, hands and skin folds;
• Pityriasis versicolor, erythrasma;
• Superficial candidiasis, candidal vulvitis and balanitis;
• Fungal infections of the outer ear;
• Paronychia;
• Mycoses complicated by pyoderma.

Contraindications

The drug in any form is contraindicated in the first trimester of pregnancy and in case of hypersensitivity to clotrimazole or auxiliary components.

Vaginal tablets and suppositories are not prescribed during the menstrual period and for children under 12 years of age.

Clotrimazole should be used with caution during breastfeeding.

Directions for use and dosage

Suppositories and tablets are intended for local intravaginal use.

Suppositories are inserted into the vagina with the patient lying on her back, as deep as possible. The drug is used daily in the evening for 6 days. Single dose – 1 suppository (100 mg). A repeat course is possible after consultation with a specialist.

Vaginal tablets are recommended to be used 2 times a day for 3 days (1 piece per dose) or 1 time per day for 6-7 days (1 piece per dose), preferably in the evening, before bedtime. Complete dissolution of the tablets is possible only with normal humidity of the vaginal mucosa. If the vaginal mucosa is dry, undissolved parts of vaginal tablets may be released, so the tablet should be inserted as deep into the vagina as possible.

If necessary, the course of treatment can be repeated, but it should be borne in mind that recurrent infections may indicate diseases such as HIV infection or diabetes mellitus. If symptoms occur again within 2 months, consult a doctor.

If the vulva and adjacent areas are simultaneously infected, you should resort to external treatment using a cream.

To sanitize the birth canal, Clotrimazole is prescribed once, 1 tablet immediately before childbirth.

The drug in the form of cream, ointment and solution is intended for external use. Clotrimazole cream and ointment are applied to the affected areas of the skin 2-3 times a day, lightly rubbing. On the feet, the cream or ointment should be applied between the toes.

To avoid relapses, treatment must be continued for at least two more weeks after all symptoms of the disease have disappeared.

The duration of therapy depends on the severity and location of the infection, as well as the effectiveness of treatment:

• Erythrasma – 2-4 weeks;
• Pityriasis versicolor – 1-3 weeks;
• Dermatomycosis – 3-4 weeks;
• Candidiasis balanitis and vulvitis – 1-2 weeks

The duration of treatment is also influenced by the individual characteristics of the patient, however, it is not recommended to use Clotrimazole for less than 3 weeks.

A solution of a few drops is applied in a thin layer to dry, cleansed affected areas and surrounding skin 2 times a day and rubbed in thoroughly. After disappearing acute symptoms Treatment is continued on average for about a month.

Clotrimazole gel is used both intravaginally (100-500 mg for 1-6 days) and externally (2-3 times a day for 2-4 weeks). During processing oral cavity The gel is used 1-2 times a day for no more than 7 days.

If there is no therapeutic effect within 3 days, it is necessary to confirm the diagnosis, and if symptoms of the disease persist for more than 7 days, treatment should be carried out under the supervision of a doctor.

Side effects

When using Clotrimazole, allergic reactions (urticaria, itching) are possible.

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

With local intravaginal use: burning, itching, vaginal discharge, swelling and hyperemia of the mucous membrane, intercurrent cystitis, frequent urination, pain during sexual intercourse, in the partner - a burning sensation in the penis.

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

special instructions

It is necessary to avoid contact medicine on the mucous membrane of the eyes, and do not use Clotrimazole on skin areas with open wounds. After applying the ointment, cream or gel, do not apply sealed dressings.

In order to prevent re-infection, simultaneous treatment of both sexual partners is recommended. For trichomoniasis, systemic chemotherapeutic agents (metronidazole orally) should be prescribed together with Clotrimazole.

In patients with impaired liver function, it is necessary to periodically monitor its functional state.

If signs of hypersensitivity or irritation appear, treatment should be discontinued.

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

Drug interactions

Simultaneous use with contraceptives containing latex is not recommended, as they may be damaged and, consequently, reduce effectiveness. It is necessary to use alternative methods of contraception for at least five days after intravaginal use of Clotrimazole.

The effectiveness of the drug is reduced when administered simultaneously with nystatin, natamycin and amphotericin B.

When dexamethasone is prescribed in high doses, the antifungal effect of clotrimazole is reduced.

When oral tacrolimus is co-administered with vaginal clotrimazole, an increase in plasma tacrolimus concentrations is possible.

When using Clotrimazole in the form of ointment and cream, cases of negative interactions with other drugs have not been recorded and they should not be expected, since the resorption capacity of the drug is very low.

Terms and conditions of storage

Store in a place protected from light, at a temperature of no more than 20-25 °C. Keep away from children. Do not freeze.

The shelf life of the solution and ointment is 2 years, other dosage forms are 3 years.

Sage essential extract.

Compound cream 1%: clotrimazole at a concentration of 10 mg/g, cetostearyl and benzyl alcohols, polysorbate 60, synthetic spermaceti, octyldodecanol, sorbitan stearate, water.

Compound ointments 1%: clotrimazole at a concentration of 10 mg/g, polyethylene oxides 400 and 1500, propylene glycol, methylparaben, nipagin.

Compound solution 1%: clotrimazole at a concentration of 10 mg/ml (calculated on dry matter), polyethylene glycol 400, propylene glycol, ethanol 96%.

Compound candles: one suppository contains 100 mg of active substance and base in the volume necessary to obtain a suppository weighing 2 g. Clotrimazole suppositories contain semi-synthetic glycerides as a base.

Compound tablets: 100, 200 or 500 mg clotrimazole, lactose monohydrate, potato starch, adipic acid, sodium bicarbonate, colloidal silicon dioxide, sodium lauryl sulfate.

Release form

• gel 1% (pack of 20 and 40 g);
• cream 1% (tubes 15, 20, 30 and 50 g);
• ointment 1% (tubes 15, 20, 30 and 40 g);
• 1% solution (15 ml bottles);
• vaginal suppositories 0.1 g (package No. 6);
• vaginal tablets 0.1, 0.2 or 0.5 g (packaging No. 1, No. 3, No. 6; tablets are equipped with an applicator).

Tablets and vaginal suppositories Clotrimazole has an ATC code different from other dosage forms of the drug - G01AF02.

Clotrimazole can also be produced in the form of granules, powder for external use, or spray.

The drug is intended for local (including intravaginal) and external use; tablets for oral administration are not available.

pharmachologic effect

Antimycotic.

Pharmacodynamics and pharmacokinetics

Clotrimazole is a derivative imidazole .

In vitro shows high activity against the most pathogenic fungi , which can cause serious infectious complications, namely:

• dermatophytes (Microsporum sp., Epidermophyton floccosum, Trichophyton sp.);
• yeast-like fungi (Cryptococcus neoformans, Candida sp.);
• dimorphic fungi (Histoplasma capsulatum, Paracoccidicides brasiliensis, Coccidiodes immitis).

The mechanism of action of clotrimazole is based on its ability to block the synthesis of proteins, nucleic acids and ergosterol, which is necessary for the construction of cell membranes of fungi. As a result, the cell membranes of the fungi are damaged and the cells die.

At low concentrations, clotrimazole has a fungistatic effect. If the dose exceeds 20 mcg/ml, the drug has a fungicidal effect, and not only on proliferating cells.

When used in high doses, it helps to increase the concentration of hydrogen peroxide in the fungal cell to a toxic value and, as a result, destroys the fungal cells

When applied topically, the drug is absorbed epidermis . The highest concentration of a substance is determined in reticuloderm . It is also able to penetrate the keratin of nails.

Clotrimazole enters the systemic circulation in very small quantities. Metabolized in the liver to inactive substances that are excreted from the body in feces and urine.

When administered intravaginally, 5 to 10% of clotrimazole is absorbed. The absorbed substance is metabolized in the liver. Metabolic products are excreted in bile.

Indications for use: what is Clotrimazole ointment, cream, gel, suppositories and tablets for?

What do Clotrimazole ointment, gel, cream and solution help with?

The drug is prescribed for treatment fungal skin infections which are caused mold and yeast fungi , dermatophytes and other pathogens sensitive to clotrimazole.

They are also used as remedies depriving caused by Malassezia furfur, And erythrasmas (causative agent - Corynebacterium minutissimum).

Clotrimazole ointment, cream, gel and solution help: from nail fungus ( , fungal paronychia ), trichophytosis , dermatophytosis , fungal erosion and diaper rash, candidiasis , , , ringworm , complicated secondary pyoderma mycoses .

Indications for the use of ointment, gel, cream and solution include infectious diseases, pathogens that are resistant to and a number of other antifungal agents.

For treatment pityriasis rosea the drug is not suitable because this disease is most likely to have viral or infectious-allergic origin , and can also be the body’s response to a severe shock or nervous breakdown. Clotrimazole is effective in fungal infections .

The use of Clotrimazole ointment, gel and cream with Clotrimazole in gynecology is indicated:

• for treatment and prevention ;
• for prevention repeated fungal infections of the female reproductive system , which develop during long-term treatment with antibiotics or against the background of immunodeficiency states.

Also, solution, gel, cream and ointment in gynecology are used to sanitize the genital tract before delivery.

Candles - what are they for?

Indications for the use of vaginal suppositories are vaginal candidiasis And genital superinfections , provoked by microorganisms sensitive to clotrimazole. The drug is prescribed to women and, after the onset of sexual activity, to teenage girls.

What are Clotrimazole tablets for?

Clotrimazole tablets are used to treat blastomycotic infections of the vulva And vagina . In particular, the drug is prescribed for vaginitis caused by fungi of the genus Candida (including diseases caused by resistant to nystatin strains) caused by other pathogens sensitive to clotrimazole superinfections of the genital organs , for sanitization of the genital tract before delivery.

Contraindications

Contraindication: hypersensitivity.

Side effects

Allergic reactions.

When applied to the skin, the following side effects are possible:

• burning;
• edema;
• the appearance of blisters;
• skin irritation;
• tingling sensation
• peeling.

Local use for urogenital mycoses may be accompanied by burning, itching, swelling and hyperemia of the mucous membrane, intercurrent cystitis , the appearance of vaginal discharge, increased urination, pain during sexual intercourse.

When applied topically mycoses of the oral cavity Redness of the mucous membrane, tingling and burning sensation at the site of application of the drug, and irritation may be observed.

Instructions for use of Clotrimazole: Clotrimazole for women and men

Clotrimazole ointment: instructions for use. How to apply Clotrimazole ointment for men?

Before applying Clotrimazole ointment (Acri or other manufacturers), the affected areas of the body are first washed with soapy water and dried thoroughly.

The drug is applied to the affected areas (covering small areas of healthy skin around the lesion) in a thin layer from 1 to 3 r./day. and rub lightly.

For 1 treatment of an area the size of a palm, a 5-mm strip of ointment is sufficient.

Regardless of what pathogen causes the disease, treatment after relief of subjective symptoms is recommended to continue for another 2 weeks.

At dermatomycosis the course of treatment lasts from 3 to 4, with erythrasma — from 2 to 4, with - from 1 to 3 weeks.

If there is no clinical improvement after 4 weeks of regular use of the drug, the patient is sent for a repeat microbiological study and the treatment regimen is reviewed.

Using ointment for thrush in women, it helps block the spread of fungal cells and, when higher doses are prescribed, ensures their complete destruction. For therapeutic purposes, Clotrimazole from thrush use 2 times a day, rubbing the ointment into the affected areas of the perineum.

For men, method of use: thrush and others (candidal balanoposthitis , urogenital candidiasis ) the same as for women.

The ointment is applied to the foreskin and glans penis and gently rubbed into the skin and mucous membrane. Frequency of applications - 2 times/day.

The drug is poorly absorbed into the skin, and its active substance is characterized by the ability to gradually accumulate in the upper layer of the skin. Thanks to these properties, Clotrimazole ointment is highly effective in thrush in men and women.

Clotrimazole cream: instructions for use

The cream is intended for topical use. At thrush And other fungal diseases it is applied to the affected parts twice or thrice during the day and lightly rubbed.

The duration of the course depends on the indications for use and ranges from 1-2 (with candidal balanitis/vulvitis ) up to 3-4 weeks (with dermatomycosis ).

To prevent relapse of the disease, it is very important not to stop treatment for another 2 weeks after the subjective symptoms of infection disappear. If there is no improvement after 4 weeks of therapy, the patient should consult a doctor.

Vaginal cream Clotrimazole is administered into the vagina in portions of 5 grams 1 time per day. within 3 days.

Instructions for the solution

Before applying Clotrimazole, the skin should be washed with warm soapy water (especially the areas between the fingers) and dried well. The affected areas are treated 2-3 times a day. The amount of solution should be sufficient for uniform application to the entire affected surface.

If the skin of the feet is affected, liquid Clotrimazole solution must be applied after each wash.

The solution is the most preferred dosage form for onychomycosis . This is due to the fact that it has the best penetrating properties.

At fungal infections of the oral cavity the affected areas of the mucous membrane are treated with a cotton swab or swab, onto which drops are first applied (10 to 20 drops are enough to treat each ear). Frequency of procedures - 3-4 rubles/day.

After applying Clotrimazole, you should refrain from eating and drinking for an hour.

Clotrimazole drops are also effective in onomycosis caused by yeast fungi. Drops are administered into the ear using turundas: a twisted cotton ball is moistened in the solution and 3-4 times a day. Place it in the ear canal for 5-10 minutes. Treatment lasts from 3 to 4 weeks.

Instructions for the gel

The peculiarity of this dosage form is that the gel is well distributed on the skin and is also well absorbed into it. This allows the drug to be used for treating hard-to-reach areas of the body.

The gel is used intravaginally in the same way as clotrimazole cream: 1 r./day. 5 grams each. The course of treatment is 3 days.

Clotrimazole vaginal tablets: instructions for use

In the absence of other prescriptions, Clotrimazole Acri tablets and synonymous drugs for thrush and others fungal infections of the genital organs apply:

• for 3 days, 1 tablet 2 times a day;
• for 6 days, 1 tablet 1 time per day.

How to administer Clotrimazole vaginal tablets? Before administration, the tablet is removed from the package and moistened with chilled boiled water. The drug should be administered in the “lying on your back” position with your knees bent.

In order for the tablet to completely dissolve and clotrimazole to work, a moist environment is required (in otherwise undissolved particles may spill out). Therefore, the tablet is inserted into the vagina as deeply as possible. It is optimal to carry out the procedure before bedtime.

Treatment must be stopped before menstruation begins. Menstrual flow will wash away the drug and it will not have the desired effect. During treatment with vaginal tablets, you should not use tampons, spermicides, intravaginal douching or any other vaginal products.

For sanitation of the genital tract Before delivery, the woman is given a single dose of 200 mg of clotrimazole.

At pregnancy the drug is contraindicated in the 1st trimester. For more later Clotrimazole does not have any adverse effects on fetal development, but the use of the applicator may be associated with certain risks.

Instructions for candles

Candles from thrush used intravaginally. The drug should be injected deep into the vagina, one dose daily for 6 days. A repeat course is possible after consulting a doctor.

Clotrimazole suppositories for thrush and others urogenital mycoses Do not use during menstrual bleeding. Treatment must be completed before it begins.

During pregnancy, the drug in this dosage form is used from the 2nd trimester and in situations where the expected benefit to the mother outweighs the possible risks to the fetus.

Reviews allow us to conclude that the drug quickly destroys fungal colonies and eliminates the unpleasant symptoms of mycoses. Its other advantages include low price and a large selection of dosage forms.

Overdose

When applied to the skin and intravaginally, there is no risk of acute intoxication, since clotrimazole enters the systemic circulation in very small quantities.

In case of accidental ingestion of Clotrimazole, nausea, anorexia, vomiting, gastralgia, and liver dysfunction are possible. In rare cases, pollakiuria, hallucinations, drowsiness, and allergic skin reactions are observed.

In this case, the patient is prescribed enterosorbents and symptomatic treatment. Gastric lavage is performed in situations where a life-threatening dose was taken within the previous hour, as well as in the presence of visible symptoms of an overdose (nausea, dizziness, vomiting).

Interaction

When used simultaneously with polyene antibiotics ( , , ) drugs mutually suppress each other's activity.

Terms of sale

Over the counter.

Storage conditions

Protect from moisture and light. Storage temperature should not exceed 25°C. Freezing of cream, gel, ointment or solution is not allowed.

Best before date

Suppositories, cream, solution, gel and vaginal tablets are suitable for use for 3 years after the date of issue. The shelf life for the ointment is 2 years.

special instructions

Avoid ingestion and contact with eyes.

For mycoses, all affected areas of the body should be treated simultaneously.

The use of vaginal tablets, unless otherwise advised by a doctor, is contraindicated in the presence of any of the following symptoms:

• acyclic vaginal bleeding ;
• bloody discharge or pathological bleeding from the vagina, uterine hemorrhages;
• dysuria ;
• lower abdominal pain;
• open sores, blisters, or sores of the vagina or vulva;
• any unpleasant symptoms that are associated with the use of Clotrimazole (irritation, redness, burning, swelling, etc.);
• chills or fever with a temperature above 38°C;
• nausea and/or vomiting;
• vaginal discharge with an unpleasant odor;
• pain in the shoulder or back.

To prevent reinfection, treatment is prescribed to both partners simultaneously. The optimal dosage form for men is cream.

At in addition to the drug, chemotherapeutic agents are prescribed for systemic treatment ( inside).

Which is better, Clotrimazole ointment or cream?

The choice in favor of one or another dosage form is made depending on the indications. Clotrimazole ointment for women and men is prescribed for diseases that are accompanied by increased dryness and flaking of the skin.

As a rule, these are mycoses of the skin caused by dermatophytes ( trichophytosis , microsporia ), erythrasma , pityriasis versicolor , individual cases

Candide is a synonym for Clotrimazole. The basis of both drugs is the same substance, so there are no fundamental differences between them.

Clotrimazole or Pimafucin - which is better?

Main component — antimycotic antibiotic nitamicin . Sensitivity to the drug is predominantly molds and yeasts (including childbirth Penicillium, Candida, Cephalosporium, Aspergillus And Fusarium).

Less sensitive to Pimafucin are Pseudoallescheria boydii And dermatophytes . That is, in situations where the cause of the disease is fungi of the genus Epidermophyton, Trichophyton or Microsporum, the choice should be made in favor of the drug Clotrimazole.

The use of Clotrimazole is less often accompanied by hypersensitivity reactions. Moreover, it is less common than Pimafucin , provokes imbalances in the microflora of the genital organs.

Clotrimazole for children

There is no experience with the use of solution, ointment, gel and cream 1% in children.

Tablets are used from 12 years of age, provided the patient has menarche .

Candles are not prescribed to children.

Clotrimazole during pregnancy and lactation

Cream, gel, ointment, solution, suppositories and vag. tablets during pregnancy can be used from the 2nd trimester.

Strictly controlled studies regarding the safety of use during pregnancy; therefore, Clotrimazole is not prescribed in the 1st trimester.

Clinical studies regarding the effect of the drug on were not carried out in women; no adverse effects were identified in animal experiments.

Clotrimazole tablets and suppositories during pregnancy (in the 2nd and 3rd trimesters) do not have a negative effect on the fetus, but using the applicator can be dangerous.

When breastfeeding, the drug is used with caution, since it is unknown whether it passes into milk.

Being one of the most effective antifungal drugs, Clotrimazole is prescribed for complex treatment various skin infections that are caused by overgrowth of Corynebacterium minutissimum and Malassezia furfur. Having a simple method of administration and a significant content of active substance in the composition of the drug, Clotrimazole is well tolerated by patients even with high sensitivity and has a small number of contraindications for use.

In the article we will review the instructions for use, price, analogs of Clotrimazole and reviews of doctors and patients about it.

Features of the drug

The greatest impact of this medicinal product has an effect in the development of diseases caused by molds, yeasts, as well as dermatophytes and other pathogens that are sensitive to the effects of clotrimazole, the active substance of the drug.

To see what the drug Clotrimazole is, watch the video below:

Composition of Clotrimazole

The main active ingredient is clotrimazole, of which 1 g of the product contains 10 mg (meaning 100% dry matter). Auxiliary components include the following:

• polyethylene glycol cetostearyl ether;
• propylene glycol;
• cetostearyl alcohol;
• polyethylene glycol 400;
• proxanol 268.

Externally, the drug is an ointment that is white in color, has a uniform consistency, and has a slight specific medicinal odor.

Dosage forms

The drug is offered for sale in the form of aluminum tubes with bouchons having inner covering varnish that is approved for use. The tube with a leaflet describing the composition and method of use is contained in a cardboard package.

Clotrimazole is also sold in the following forms:

• vaginal tablets having appearance parallelepiped with slightly rounded corners. They contain 100 mg of active substance. There are 6 pieces in the blister;
• ointment (cream), having a white color and uniform consistency, for external use. The active substance in the ointment is 10 mg per 1 g of ointment. The ointment is packaged in tubes of 30 g, 20 g. Vaginal cream 2% is offered in tubes of 50 g;
• solution, also used for outdoor use. The solution (1%) is packaged in bottles orange color and their volume can be 15 or 30 ml.

The cost of the drug may vary: vaginal pharmacies offer tablets at prices ranging from 35 to 60 rubles. A solution of various volumes costs from 96 to 123 rubles per bottle, and ointment, also depending on the volume of the tube, costs 180-215 rubles.

pharmachologic effect

A special feature of Clotrimazole is its rapid penetration into the upper layer of the epidermis and the immediate onset of action on yeast fungi. At the same time, the rate of reproduction of fungi is sharply limited, the possibility for their further spread is reduced, and improvements in the condition of the skin appear.

Pharmacodynamics

Clotrimazole, penetrating the skin within 30-45 minutes after its application, destroys the cell membranes of fungi, preventing the absorption of nutrients from environment. Without a negative effect on the composition of the blood, the drug penetrates into all layers of the epidermis and has a detrimental effect on the colonies of Corynebacterium minutissimum and Malassezia furfur.

Pharmacokinetics

Due to the rapid rate of absorption of the active substance of the drug into the skin, the fastest possible effect on the cause of the disease occurs: the skin is cleansed, its surface is smoothed and functions are restored.

The breakdown products of the drug are eliminated by the kidneys. Negative effects on the body when the product is absorbed in the absence hypersensitivity skin to the components of Clotrimazole was not detected.

The active substance can penetrate the tissues of the placenta and enter the fetus; for this reason, careful administration of Clotrimazole is required during pregnancy or when pregnancy is suspected. The drug can be used by pregnant women in cases where its benefit exceeds the probable Negative consequences for the fetus. When breastfeeding, Clotrimazole is prescribed as needed; Before feeding, the mammary glands should be thoroughly wiped to avoid the drug entering the newborn’s body.

What, besides fungus, does Clotrimazole help with, this video will tell you:

Indications

Clotrimazole is prescribed for many lesions of the upper layer of skin. Due to the high activity of the active substance, it has a rapid effect on the foci of infection and a noticeable improvement in the condition of the skin within 1.5-2 weeks from the start of use of the product.

The drug is prescribed in the presence of the following diseases and conditions:

• skin infections that are caused by mold, yeast and other fungi, as well as dermatophytes and other types of pathogens;
• diseases that arise in the layers of the skin under the influence of excessively active reproduction of Corynebacterium minutissimum (erythrasma) and Malassezia furfur (variegated);
• for the treatment of inflammation;
• during treatment.

Usually the drug is recommended by a dermatologist, who, when drawing up a treatment regimen, takes into account the general condition of the body, the presence of hypersensitivity to the components of the drug, however, Clotrimazole is sold in pharmacies without the need to present a prescription, which allows it to be used independently in the presence of severe skin lesions. In this case, it is mandatory to carefully study the attached instructions.

Instructions

Before using the antifungal drug in question, you should thoroughly clean the surface of the affected skin using soap and plenty of water. The pH value should be neutral. After this, dry the skin and apply ointment (cream) to the affected areas, which is distributed evenly over it. The amount of ointment depends on the area of ​​the lesion.

After application, the ointment should be lightly rubbed in: this will allow it to be absorbed faster and increase the effect of the active substance. The first signs of improvement in skin condition usually begin to appear after 1.5-2 weeks from the start of treatment. Also, the final effect depends on the degree of skin damage and its sensitivity to the active substance.

After the first signs of improvement appear, it is recommended to continue using the drug for another two weeks to consolidate the effect.

Depending on the type of disease, the duration of treatment is prescribed:

• for lichen versicolor, the ointment is used for 1-3 weeks;
• for dermatomycosis of various origins - 3-4 weeks;
• When treating erythrasma, 2.5-4 weeks of using Clotrimazole is usually sufficient.

If a pronounced improvement in the condition of the skin has not occurred after 4 weeks of continuous use of the drug, you should inform your dermatologist about this and make adjustments to the proposed treatment regimen.

In the presence of liver or kidney dysfunction, the dose of the drug used does not change.

Contraindications

• Excessive sensitivity to the active substance of the drug or to its other components should be considered a contraindication to the use of Clotrimazole.
• Some caution should also be exercised when prescribing the drug during pregnancy and breastfeeding.

Side effects

The most common side effects when using Clotrimazole usually include:

special instructions

Pregnancy and breastfeeding are special cases in which special caution should be exercised when prescribing Clotrimazole. If there is greater benefit for the pregnant woman than the negative effect of the drug on the fetus, Clotrimazole can be prescribed, but it should be constantly monitored by a doctor.

Interaction with other drugs

Enhancing the antifungal effect of increased concentrations of propyl ester of hydroxybenzoic acid allows the use of these substances together without reducing the effect. However, Clotrimazole reduces the degree of exposure to nystatin, amphotericin, and natamycin.

When using Clotrimazole in significant concentrations on the affected areas of the skin, the degree of its effectiveness increases.

Antifungal drug for external use

Active substance

Release form, composition and packaging

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

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

20 g - aluminum tubes (1) - cardboard packs.

pharmachologic effect

Clotrimazole inhibits the growth and division of microorganisms and, depending on the concentration, can have a fungistatic (delaying and stopping the growth of fungal cells) or fungicidal (leading to the death of fungi) effect. Clotrimazole inhibits ergosterol synthesis and binds to phospholipids cell membrane fungus, which leads to changes in the permeability of cell membranes.

At higher concentrations, clotrimazole causes damage to cell membranes by mechanisms independent of sterol synthesis.

Clotrimazole also disrupts the vital processes in the fungal cell, suppressing the formation of components necessary for the construction of vital cellular structures (proteins, fats, DNA, polysaccharides), damages nucleic acids and increases the excretion of potassium.

Ultimately, the effect of clotrimazole on fungal cells leads to their death.

Clotrimazole is characterized by a wide spectrum antifungal and antibacterial activity: dermatophytes (Epidermophyton floccosum, Microsporum canis, Trichophyton mentagrophytes, Trichophyton rubrum), yeast (Candida spp., Cryptococcus neoformans), dimorphic fungi (Coccidioides immitis, Histoplasma capsulatum, Paracoccidioides brasiliensis), protozoa (Trichomonas vaginalis).

He also active regarding some gram-positive bacteria.

When studying the effectiveness of clotrimazole in laboratory conditions outside the human body (in vitro), a wide range of its fungistatic and fungicidal activity was revealed. It acts on the mycelium of dermatophytes (Trichophyton, Microsporum, Epidermophyton) in a similar way to griseofulvin, and its effect on budding fungi (Candida) is similar to the effect of polyenes (amphotericin B and nystatin).

At concentrations less than 1 mcg/ml, clotrimazole inhibits the development of most strains of pathogenic fungi belonging to Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis.

At a concentration of 3 μg/ml, clotrimazole inhibits the development of most other bacteria: Pityrosporum orbiculare, Aspergillus fumigatus, the genus Candida, incl. Candida albicans, some strains of Staphylococcus aureus, Streptococcus pyogenes, as well as some strains of Proteus vulgaris and Salmonella. Clotrimazole is active against Sporothrix, Cryptococcus, Cephalosporium, Fusarium.

At concentrations greater than 100 μg/ml, it is effective against Trichomonas vaginalis.

Fungi resistant to clotrimazole are extremely rare; There is data only on individual strains of Candida guilliermondii.

The development of resistance in clotrimazole-sensitive fungi following passage of Candida albicans and Trichophyton mentagrophytes has not been reported. There have been no cases of the development of resistance to clotrimazole in Candida albicans strains resistant to polyene antibiotics due to a chemical mutation.

Pharmacokinetics

Suction and distribution

Pharmacokinetic studies have shown that clotrimazole is practically not absorbed into the systemic circulation when the drug is applied to intact or inflamed areas of the skin. Clotrimazole serum concentrations were below the detection limit (0.001 μg/ml), confirming that topical clotrimazole does not lead to clinically significant systemic effects or side effects.

Metabolism and excretion

Clotrimazole breaks down in the liver to inactive substances that are excreted from the body through the kidneys and intestines.

Indications

For external treatment of fungal infections caused by dermatophytes, yeast-like fungi, molds, as well as pathogens sensitive to clotrimazole:

• mycoses of the feet, hands, torso, skin folds;
• candidal vulvitis, candidal balanitis;
• lichen versicolor, erythrasma;
• fungal infections of the outer ear.

Contraindications

• hypersensitivity to clotrimazole or other components of the drug.

Dosage

For external use. The cream should be applied to the affected areas of the skin 2-3 times a day.

For relapse prevention Treatment should be continued for at least two weeks after all symptoms of infection have disappeared.

The cream should be applied to clean, dry areas of affected skin (washed with neutral pH soap), and on the feet the cream should be applied between the toes.

The duration of treatment depends on the severity of the disease, its location, and the effectiveness of treatment.

Duration of treatment: ringworm - 3-4 weeks; erythrasma - 2-4 weeks; pityriasis versicolor - 1-3 weeks; candidal vulvitis and balanitis - 1-2 weeks.

The duration of treatment may vary according to individual characteristics, but a treatment duration of less than 3 weeks is not recommended. To prevent recurrence of infection, use of the drug should be continued for 1-2 weeks after all symptoms of the disease disappear. If after 7 days of treatment there is no improvement in symptoms, you should consult your doctor.

Side effects

The adverse events presented below are listed according to the damage to organs and organ systems and the frequency of occurrence. The frequency of occurrence is defined as follows: very often (≥1/10), often (≥1/100 and< 1/10), нечасто (≥1/1000 и < 1/100), редко (≥1/10 000 и < 1/1 000), очень редко (< 1/10 000, включая отдельные случаи), неизвестно (частота не может быть оценена по имеющимся на настоящий момент данным). Категории частоты были сформированы на основании пострегистрационного наблюдения.

From the immune system: unknown - allergic reaction (manifested by urticaria, fainting, arterial hypotension, shortness of breath).

For the skin and subcutaneous tissues: unknown - rash, itching, blistering rashes, peeling, pain or discomfort, swelling, burning, irritation.

Overdose

Symptoms: If the drug is accidentally taken orally, nausea and vomiting may occur.

Treatment: In case of accidental ingestion of the cream, symptomatic treatment should be carried out. When using the drug externally, an overdose is unlikely.

Drug interactions

Not studied.

special instructions

Avoid contact of the cream with the mucous membrane of the eyes. Do not swallow.

All infected areas should be treated at the same time.

The drug Clotrimazole contains cetostearyl alcohol, which can cause local skin reactions (for example, contact reactions).

If symptoms of hypersensitivity or irritation appear, stop treatment.

Laboratory data indicate that the use of latex-containing contraceptives may cause contraceptive damage when used concomitantly with clotrimazole. Consequently, the effectiveness of such contraceptives may be reduced. Patients should be advised to use alternative methods for at least 5 days after using clotrimazole.

Impact on the ability to drive vehicles and operate machinery

The effect of clotrimazole on the ability to drive vehicles and machines has not been reported.

Pregnancy and lactation

The use of the drug Clotrimazole is allowed only if, in the opinion of the doctor, the potential benefit from using the cream for the mother outweighs the possible risk to the fetus.

Epidemiological studies have not revealed any adverse events related to pregnancy or fetal health when using the drug Clotrimazole.

The use of the drug Clotrimazole in women during breastfeeding is allowed only if, in the opinion of the doctor, the potential benefit of using the cream for the mother outweighs the possible risk for the child.

Fertility

No data available.

Conditions for dispensing from pharmacies

The drug is available without a prescription.

Storage conditions and periods

The drug should be kept out of the reach of children at a temperature not exceeding 25 °C. Do not freeze. Shelf life - 3 years.

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

White crystalline substance, odorless. Practically insoluble in water, sparingly soluble in ether, very soluble in polyethylene glycol 400, ethanol and chloroform. Molecular mass 344,84.

Pharmacology

pharmachologic effect- antibacterial, antiprotozoal, trichomonacid, antifungal wide range .

Disturbs the synthesis of ergosterol (the main structural component fungal cell membrane), changes the permeability of the fungal membrane, promotes the release of potassium and intracellular phosphorus compounds from the cell and the breakdown of cellular nucleic acids. Inhibits the synthesis of triglycerides and phospholipids. Reduces the activity of oxidative and peroxidase enzymes, as a result of which the intracellular concentration of hydrogen peroxide increases to a toxic level, which contributes to the destruction of cellular 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 lichen versicolor - Pityrosporum orbiculare(Malassezia furfur).

Fungal strains that are naturally resistant 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, and Staphylococcus spp., Streptococcus spp., gram-negative bacteria - Bacteroides, Gardnerella vaginalis. In high concentrations it is active against Trichomonas vaginalis.

Poorly absorbed through the skin and mucous membranes.

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 nails, it is found in keratin.

When administered intravaginally, 3-10% of the dose is absorbed.

In the liver it is quickly biotransformed to inactive metabolites and excreted in feces. 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 in blood persist for 48-72 hours.

Carcinogenicity, mutagenicity, effect on fertility

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

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

Pregnancy. In studies in pregnant rats, intravaginal administration of doses of clotrimazole up to 100 mg/kg did not reveal any adverse effects on the fetus. However, daily oral administration of clotrimazole at doses ranging from 50 to 120 mg/kg resulted in embryotoxicity in rats and mice (possibly secondary to maternal toxicity). Thus, in mice, when taking clotrimazole in doses 120 times higher than the usual dose in humans, in the period from 9 weeks before mating to the end of feeding, mating disruption, a decrease in the number of viable pups, 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 normal human dose, no adverse effects were observed. In rats, at doses 50 times higher than the usual human dose, clotrimazole, over a similar observation period, caused a slight decrease in the number of pups in the litter and a decrease in their survival. No teratogenic effects were detected in mice, rabbits and rats when clotrimazole was taken orally at doses up to 200, 180 and 100 mg/kg, respectively.

Use of the substance Clotrimazole

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

Contraindications

Hypersensitivity.

Use during pregnancy and breastfeeding

Should not be used in the first trimester of pregnancy (adequate and strictly controlled studies have not been conducted). When used intravaginally in women in the second and third trimesters of pregnancy, no adverse effects on the fetus were detected, but the use of a vaginal applicator is undesirable.

With caution - during breastfeeding (it is unknown whether clotrimazole penetrates into breast milk).

Side effects of the substance Clotrimazole

Allergic reactions (itching, urticaria).

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

When used topically for the treatment of 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 sexual intercourse.

When applied topically in the oral cavity: redness of the oral mucosa, burning and tingling sensation 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, the following are possible: symptoms: anorexia, nausea, vomiting, gastralgia, liver dysfunction; rarely - drowsiness, hallucinations, pollakiuria, allergic skin reactions.

Treatment: reception activated carbon, symptomatic therapy.

Routes of administration

Locally.

Precautions for the substance Clotrimazole

Avoid contact of the drug with the mucous membrane of the eyes. Avoid use in areas where the integrity of the skin is damaged.

After applying the cream, do not use sealed dressings.

To prevent reinfection, simultaneous treatment of the sexual partner is recommended. Do not prescribe intravaginally during menstruation. For trichomoniasis, combined use 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 study should be performed to confirm the diagnosis and exclude another cause of the disease.

Interactions with other active ingredients

Trade names

Name	The value of the Vyshkowski Index ®