About all

Clotrimazole tablet side effects: Clotrimazole Lozenge: MedlinePlus Drug Information

Содержание

Clotrimazole Lozenge: MedlinePlus Drug Information


pronounced as (kloe trim’ a zole)

To use the sharing features on this page, please enable JavaScript.

  • Why is this medication prescribed?
  • How should this medicine be used?
  • Other uses for this medicine
  • What special precautions should I follow?
  • What special dietary instructions should I follow?
  • What should I do if I forget a dose?
  • What side effects can this medication cause?
  • What should I know about storage and disposal of this medication?
  • In case of emergency/overdose
  • What other information should I know?
  • Brand names

Clotrimazole lozenges are used to treat yeast infections of the mouth in adults and children 3 years of age and older. It can also be used to prevent yeast infections of the mouth in people at risk of these infections who are receiving certain treatments. Clotrimazole is in a class of antifungal medications called imidazoles. It works by stopping the growth of fungi that cause infection.

Clotrimazole comes as a lozenge to slowly dissolve in the mouth. For the treatment of yeast infections, it is usually used five times a day for 14 days. For the prevention of yeast infections, it is usually used three times a day. The length of your treatment for prevention depends on your condition. Use clotrimazole lozenges at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Use clotrimazole exactly as directed. Do not use more or less of it or use it more often than prescribed by your doctor.

To use the lozenge, place it in your mouth and allow it to slowly dissolve. Do not chew, crush, or swallow clotrimazole lozenges. It should take about 30 minutes to dissolve.

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

Before using clotrimazole lozenges,

  • tell your doctor and pharmacist if you are allergic to clotrimazole, any other medications, or any of the ingredients in clotrimazole lozenges. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.
  • tell your doctor if you have or have ever had liver disease.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while using clotrimazole lozenges, call your doctor.

Unless your doctor tells you otherwise, continue your normal diet.

Use the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not use a double dose to make up for a missed one.

Clotrimazole may cause side effects.

Tell your doctor if any of these symptoms are severe or do not go away:

  • nausea
  • vomiting
  • unpleasant mouth sensations
  • itching

Clotrimazole may cause other side effects. Call your doctor if you have any unusual problems while using this medication.

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Do not freeze.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.

  • Mycelex®

This branded product is no longer on the market. Generic alternatives may be available.

Last Revised – 11/15/2018

Browse Drugs and Medicines

Clotrimazole Topical: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

Clotrimazole is used to treat skin infections such as athlete’s foot, jock itch, ringworm, and other fungal skin infections (candidiasis). This medication is also used to treat a skin condition known as pityriasis (tinea versicolor), a fungal infection that causes a lightening or darkening of the skin of the neck, chest, arms, or legs. Clotrimazole is an azole antifungal that works by preventing the growth of fungus.

How to use Clotrimazole Solution, Non-

Use this medication on the skin only. Clean and thoroughly dry the area to be treated. Apply this medication to the affected skin, usually twice a day or as directed by your doctor. Dosage and length of treatment depends on the type of infection being treated. Do not apply this more often than prescribed. Your condition will not clear faster, but side effects may be increased.

Apply enough medication to cover the affected area and some of the surrounding skin. After applying this medication, wash your hands. Do not wrap, cover or bandage the area unless directed to do so by your doctor.

Do not apply this medication in the eyes, nose, mouth, or vagina.

Use this medication regularly in order to get the most benefit from it. Remember to use it at the same times each day.

Continue to use this medication until the full prescribed amount is finished, even if symptoms disappear after starting clotrimazole. Stopping the medication too early may allow the fungus to continue to grow, which may result in a relapse of the infection.

Inform your doctor if your condition lasts after 4 weeks of treatment or gets worse at any time.

Side Effects

Burning, stinging, swelling, irritation, redness, pimple-like bumps, tenderness, or flaking of the treated skin may occur. If any of these effects last or get worse, notify your doctor or pharmacist promptly.

If your doctor has directed you to use this medication, remember that your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: blistering, oozing, open sores.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before using clotrimazole, tell your doctor or pharmacist if you are allergic to it; or to other azole antifungals such as econazole, ketoconazole, or miconazole; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history.

This medication should be used only if clearly needed during pregnancy. Discuss the risks and benefits with your doctor.

It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Does Clotrimazole Solution, Non- interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

This medicine may be harmful if swallowed. If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

Do not share this medication with others.

If your doctor has directed you to use this medication, use it for your current condition only. Do not use it later for another infection unless your doctor tells you to.

When treating pityriasis, this medication may not cause an immediate return to normal skin color. It may take several months after treatment is completed for your natural skin color to return.

If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Use your next dose at the regular time. Do not double the dose to catch up.

Different brands/strengths of this medication may have different storage requirements. Read the package labeling or ask your pharmacist for the storage requirements for the product you are using. Protect from light. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Images

clotrimazole 1 % topical solution

Color: clearShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical solution

Color: colorlessShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical solution

Color: colorlessShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical solution

Color: Shape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: Shape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical solution

Color: clearShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical solution

Color: colorlessShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical solution

Color: clearShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical cream

Color: whiteShape: Imprint:

This medicine is a clear, clear, solution

clotrimazole 1 % topical solution

Color: clearShape: Imprint:

This medicine is a clear, clear, solution

Next

Save up to 80% on your prescriptions.

Available coupons

Save up to 80% on your prescription with WebMDRx

Drug Survey

Are you currently using Clotrimazole Solution, Non-?

This survey is being conducted by the WebMD marketing sciences department.

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Clotrimazole – description of the substance, pharmacology, use, contraindications, formula

Contents

  • Structural formula

  • Russian name

  • English name

  • Latin name

  • chemical name

  • Gross formula

  • Pharmacological group of the substance Clotrimazole

  • Nosological classification

  • CAS code

  • pharmachologic effect

  • Characteristic

  • Pharmacology

  • The use of the substance Clotrimazole

  • Contraindications

  • Use during pregnancy and lactation

  • Side effects of the substance Clotrimazole

  • Interaction

  • Overdose

  • Dosage and administration

  • Precautionary measures

  • Trade names with the active substance Clotrimazole

Structural formula

Russian name

Clotrimazole

English name

Clotrimazole

Latin name

Clotrimazolum (born ) Clotrimazoli)

Chemical name

1-[(2-Chlorophenyl)diphenylmethyl]-1H-imidazole

Gross formula

C 22 H 17 ClN 2

9000 2 Pharmacological group of the substance Clotrimazole

Antifungals

Other synthetic antibacterial agents

Nosological classification

ICD-10 code list

  • A59. 0 Urogenital trichomoniasis

  • B35 Dermatophytosis

  • B36 Other superficial mycoses

  • B36.0 Lichen versicolor

  • B37. 0 Candidal stomatitis

  • B37.2 Skin and nail candidiasis

  • B37.3 Vulvar and vaginal candidiasis (N77.1*)

  • B37.4 Candidiasis of other urogenital sites

  • L08. 0 Pyoderma

  • L08.1 Erythrasma

  • N51.2 Balanitis in diseases classified elsewhere

  • N77.1 Vaginitis, vulvitis and vulvovaginitis in infectious and parasitic diseases classified elsewhere

  • O23. 9 Other and unspecified urinary tract infection in pregnancy

CAS code

23593-75-1

Pharmacological action

Pharmacological action

antibacterial , broad spectrum antifungal , antiprotozoal , trichomonacid .

Characteristics

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

Odorless white crystalline substance. Practically insoluble in water, sparingly soluble in ether, very soluble in polyethylene glycol 400, ethanol and chloroform. Molecular weight 344.84.

Pharmacology

It disrupts 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 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 the nails, it is found in keratin.

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

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

High concentrations in vaginal secretion and low concentrations in the blood persist for 48-72 hours

Carcinogenicity, mutagenicity, effects on fertility . Long-term studies in animals to evaluate the potential carcinogenicity of clotrimazole when administered intravaginally have not been conducted.

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

Pregnancy. In studies in pregnant rats, intravaginal doses of clotrimazole up to 100 mg/kg showed no adverse effect on the fetus. However, daily oral doses of 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 the usual dose in humans, in the period from 9 weeks to mating and until the end of feeding, mating disorders, 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 dose in humans, clotrimazole, with a similar observation period, caused a slight decrease in the number of pups in the offspring and a decrease in their survival. There was no teratogenic effect in mice, rabbits and rats when taking clotrimazole orally at doses up to 200, 180 and 100 mg/kg, respectively.

Application of the substance Clotrimazole

Fungal infections 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; candidiasis stomatitis; candidal vulvitis, vulvovaginitis, balanitis, trichomoniasis; for sanitation of the birth canal before childbirth.

Contraindications

Hypersensitivity.

Use in pregnancy and lactation

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 the II and III trimesters of pregnancy, no adverse effects on the fetus have been identified, however, the use of a vaginal applicator is undesirable.

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

Side effects of the substance Clotrimazole

Allergic reactions (itching, urticaria).

When applied topically to the skin: erythema, blistering, swelling, burning and stinging, skin irritation and flaking.

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.

Topically applied in the mouth: 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 symptoms are possible: anorexia, nausea, vomiting, gastralgia, impaired liver function; rarely – drowsiness, hallucinations, pollakiuria, allergic skin reactions.

Treatment: activated charcoal, symptomatic therapy.

Dosage and Administration

Locally, is applied in a thin layer to 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 of clinical manifestations), it is advisable to continue using the drug for another 14 days. The duration of therapy for erythrasma is 2-4 weeks, for lichen multi-colored – 1-3 weeks.

Before greasing, wash the feet with warm water and soap, dry thoroughly, especially between the toes. In fungal diseases of the skin of the legs, it is recommended to continue treatment after achieving a therapeutic effect for 2-3 weeks.

Topical 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. For 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, once a 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 the rehabilitation of the birth canal, a single administration of the tablet is recommended.

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

Precautions

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

Do not use sealing dressings after applying the cream.

Simultaneous treatment of the sexual partner is recommended to prevent reinfection. 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, it is necessary to periodically monitor its functional state.

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

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

Trade names with active substance Clotrimazole

Reset filters

Lek. form
All lek. forms gel vaginal gel for external use cream cream vaginal cream for external use ointment for external use powder for external use solution for topical application solution for external use topical spray powder substance suppositories vaginal tablets vaginal

Dosage
All dosages 0. 1 g 1% 10 mg/g 10 mg/ml 100 mg 2% 200 mg 500 mg No dosage

Manufacturer
All manufacturers AKRIKHIN AO Aveksima Sibir OOO Agio Pharmaceuticals Ltd. Akrikhin OJSC Amoli Organics VERTEX JSC VERTEX ZAO GlaxoSmithKline Pharmaceuticals Glenmark Pharmaceuticals Ltd. Jintan Zhang Xing Medical Pharma Zelenaya Dubrava CJSC ZiO-Zdorovye Ivanovskaya Pharmaceutical Factory Kirov Pharmaceutical Company JSC Lock-Beta Pharmaceuticals (I) Pvt. Ltd Magistra K & K Medana Pharma JSC Merkle Micro Labs Limited Murom Instrument-Making Plant JSC (MPZ JSC) Murom Instrument-Making Plant Ozon OJSC Ozon Pharm LLC Sedate Healthcare Synthesis OJSC Troponwerke Tula Pharmaceutical Factory PharmVILAR LLC NPO PharmConcept LLC Pharma Wernigerode GmbH Pharmaprime Pharmaceutical Plant POLFARMA SA Medan Division in Seradz Pharmstandard-Leksredstva Hyperion Shreya Life Sciences Pvt. Ltd. Yangsu Yunyang Group Pharmaceutical Co.

Information for healthcare professionals only.
Are you a healthcare professional?

Clotrimazole – description of the substance, pharmacology, use, contraindications, formula

Contents

  • Structural formula

  • Russian name

  • English name

  • Latin name

  • chemical name

  • Gross formula

  • Pharmacological group of the substance Clotrimazole

  • Nosological classification

  • CAS code

  • pharmachologic effect

  • Characteristic

  • Pharmacology

  • The use of the substance Clotrimazole

  • Contraindications

  • Use during pregnancy and lactation

  • Side effects of the substance Clotrimazole

  • Interaction

  • Overdose

  • Dosage and administration

  • Precautionary measures

  • Trade names with the active substance Clotrimazole

Structural formula

Russian name

Clotrimazole

English name

Clotrimazole

Latin name

Clotrimazolum (born ) Clotrimazoli)

Chemical name

1-[(2-Chlorophenyl)diphenylmethyl]-1H-imidazole

Gross formula

C 22 H 17 ClN 2

9000 2 Pharmacological group of the substance Clotrimazole

Antifungals

Other synthetic antibacterial agents

Nosological classification

ICD-10 code list

  • A59. 0 Urogenital trichomoniasis

  • B35 Dermatophytosis

  • B36 Other superficial mycoses

  • B36.0 Lichen versicolor

  • B37. 0 Candidal stomatitis

  • B37.2 Skin and nail candidiasis

  • B37.3 Vulvar and vaginal candidiasis (N77.1*)

  • B37.4 Candidiasis of other urogenital sites

  • L08. 0 Pyoderma

  • L08.1 Erythrasma

  • N51.2 Balanitis in diseases classified elsewhere

  • N77.1 Vaginitis, vulvitis and vulvovaginitis in infectious and parasitic diseases classified elsewhere

  • O23. 9 Other and unspecified urinary tract infection in pregnancy

CAS code

23593-75-1

Pharmacological action

Pharmacological action

antibacterial , broad spectrum antifungal , antiprotozoal , trichomonacid .

Characteristics

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

Odorless white crystalline substance. Practically insoluble in water, sparingly soluble in ether, very soluble in polyethylene glycol 400, ethanol and chloroform. Molecular weight 344.84.

Pharmacology

It disrupts 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 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 the nails, it is found in keratin.

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

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

High concentrations in vaginal secretion and low concentrations in the blood persist for 48-72 hours

Carcinogenicity, mutagenicity, effects on fertility . Long-term studies in animals to evaluate the potential carcinogenicity of clotrimazole when administered intravaginally have not been conducted.

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

Pregnancy. In studies in pregnant rats, intravaginal doses of clotrimazole up to 100 mg/kg showed no adverse effect on the fetus. However, daily oral doses of 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 the usual dose in humans, in the period from 9 weeks to mating and until the end of feeding, mating disorders, 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 dose in humans, clotrimazole, with a similar observation period, caused a slight decrease in the number of pups in the offspring and a decrease in their survival. There was no teratogenic effect in mice, rabbits and rats when taking clotrimazole orally at doses up to 200, 180 and 100 mg/kg, respectively.

Application of the substance Clotrimazole

Fungal infections 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; candidiasis stomatitis; candidal vulvitis, vulvovaginitis, balanitis, trichomoniasis; for sanitation of the birth canal before childbirth.

Contraindications

Hypersensitivity.

Use in pregnancy and lactation

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 the II and III trimesters of pregnancy, no adverse effects on the fetus have been identified, however, the use of a vaginal applicator is undesirable.

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

Side effects of the substance Clotrimazole

Allergic reactions (itching, urticaria).

When applied topically to the skin: erythema, blistering, swelling, burning and stinging, skin irritation and flaking.

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.

Topically applied in the mouth: 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 symptoms are possible: anorexia, nausea, vomiting, gastralgia, impaired liver function; rarely – drowsiness, hallucinations, pollakiuria, allergic skin reactions.

Treatment: activated charcoal, symptomatic therapy.

Dosage and Administration

Locally, is applied in a thin layer to 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 of clinical manifestations), it is advisable to continue using the drug for another 14 days. The duration of therapy for erythrasma is 2-4 weeks, for lichen multi-colored – 1-3 weeks.

Before greasing, wash the feet with warm water and soap, dry thoroughly, especially between the toes. In fungal diseases of the skin of the legs, it is recommended to continue treatment after achieving a therapeutic effect for 2-3 weeks.

Topical 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. For 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, once a 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 the rehabilitation of the birth canal, a single administration of the tablet is recommended.

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

Precautions

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

Do not use sealing dressings after applying the cream.

Simultaneous treatment of the sexual partner is recommended to prevent reinfection. 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, it is necessary to periodically monitor its functional state.

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

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

Trade names with active substance Clotrimazole

Reset filters

Lek. form
All lek. forms gel vaginal gel for external use cream cream vaginal cream for external use ointment for external use powder for external use solution for topical application solution for external use topical spray powder substance suppositories vaginal tablets vaginal

Dosage
All dosages 0.