What are the primary uses of Clotrimazole 10mg troche. How does Clotrimazole work to treat yeast infections. What are the common side effects of Clotrimazole 10mg troche. How should Clotrimazole be taken for optimal effectiveness. What precautions should be taken when using Clotrimazole 10mg troche.

Understanding Clotrimazole: An Antifungal Medication

Clotrimazole is an antifungal medication belonging to the azole class of drugs. It is primarily used to treat and prevent yeast infections of the mouth and throat in adults and children over three years old. The medication is available in the form of a 10mg troche (lozenge) that dissolves slowly in the mouth, providing localized treatment.

As an azole antifungal, Clotrimazole works by inhibiting the growth of fungi, particularly Candida species, which are responsible for most oral yeast infections. It does this by interfering with the fungal cell membrane synthesis, ultimately leading to the death of the fungal cells.

Key Points About Clotrimazole 10mg Troche

• It is specifically designed for oral use
• Not absorbed through the stomach, so it won’t treat fungal infections elsewhere in the body
• Typically prescribed for oropharyngeal candidiasis (oral thrush)
• Can be used both for treatment and prophylaxis in immunocompromised patients

Indications and Uses of Clotrimazole 10mg Troche

Clotrimazole 10mg troche is primarily indicated for the treatment and prevention of oral thrush. Oral thrush is a fungal infection caused by an overgrowth of Candida species in the mouth and throat. It can affect people of all ages but is more common in infants, elderly individuals, and those with weakened immune systems.

Treatment of Oral Thrush

For the treatment of confirmed oral thrush, Clotrimazole 10mg troche is typically prescribed to be taken five times a day for 14 days. It’s important to note that the infection should be confirmed through a KOH smear or other culture methods before starting treatment.

Prophylaxis for High-Risk Patients

In addition to its treatment role, Clotrimazole 10mg troche is also used prophylactically to reduce the incidence of oral thrush in immunocompromised patients. This includes individuals undergoing chemotherapy, radiotherapy, or steroid therapy for conditions such as leukemia, solid tumors, or after renal transplantation.

For prophylaxis, the typical dosage is 10mg taken orally three times a day. This regimen is usually continued for the duration of chemotherapy or until steroid doses are reduced to maintenance levels.

Proper Administration of Clotrimazole 10mg Troche

To ensure the maximum effectiveness of Clotrimazole 10mg troche, it’s crucial to administer it correctly. Here are the key points to remember:

1. Allow the troche to dissolve slowly in your mouth
2. Do not chew the troche
3. Take as directed by your healthcare provider, typically 3-5 times per day
4. If you miss a dose, take it as soon as you remember, unless it’s almost time for your next dose
5. Never double up on doses

Is it safe to take Clotrimazole 10mg troche long-term? While Clotrimazole can be effective for prophylaxis in immunocompromised patients, the safety and efficacy of prolonged treatment doses have not been established. It’s generally recommended to limit treatment to short-term use when possible. Always follow your healthcare provider’s instructions regarding the duration of use.

Side Effects and Precautions of Clotrimazole 10mg Troche

Like all medications, Clotrimazole 10mg troche can cause side effects, although not everyone experiences them. It’s important to be aware of potential adverse reactions and take necessary precautions.

Common Side Effects

While the medication insert doesn’t specify common side effects, typical reactions to oral antifungal medications may include:

• Nausea or stomach discomfort
• Changes in taste sensation
• Dry mouth
• Mild burning or irritation in the mouth

Serious Side Effects

Though rare, serious side effects can occur. Seek immediate medical attention if you experience signs of an allergic reaction, such as:

• Hives
• Difficulty breathing
• Swelling of the face, lips, tongue, or throat

Precautions and Contraindications

Before using Clotrimazole 10mg troche, inform your healthcare provider if you:

• Are allergic to Clotrimazole or any other medications
• Have a history of liver disease
• Are pregnant or breastfeeding
• Are taking any other medications, including over-the-counter drugs and herbal supplements

Can Clotrimazole 10mg troche be used during pregnancy? While the medication insert doesn’t provide specific guidance for use during pregnancy, it’s crucial to inform your healthcare provider if you are pregnant or planning to become pregnant. They can assess the potential risks and benefits of using Clotrimazole in your specific situation.

Drug Interactions and Considerations

Clotrimazole 10mg troche is not absorbed through the stomach, which minimizes the risk of systemic drug interactions. However, it’s still important to inform your healthcare provider about all medications you’re taking to ensure there are no potential local interactions or contraindications.

While systemic interactions are unlikely, certain medications or conditions might affect the effectiveness of Clotrimazole or increase the risk of side effects. These could include:

• Other antifungal medications
• Medications that affect liver function
• Immunosuppressant drugs

How does Clotrimazole 10mg troche interact with the immune system? Clotrimazole primarily works locally in the mouth and throat, so it doesn’t have a significant impact on the overall immune system. However, in immunocompromised patients, it plays a crucial role in preventing opportunistic fungal infections that could otherwise take advantage of a weakened immune response.

Storage and Handling of Clotrimazole 10mg Troche

Proper storage and handling of Clotrimazole 10mg troche are essential to maintain its effectiveness and safety. Here are the key points to remember:

• Store at room temperature away from moisture and heat
• Avoid freezing the medication
• Keep out of reach of children
• Do not share your medication with others
• Use only for the prescribed indication

What is the shelf life of Clotrimazole 10mg troche? The exact shelf life can vary depending on the manufacturer and storage conditions. Always check the expiration date on the packaging and do not use the medication if it has expired. If you have any doubts about the quality or effectiveness of your medication, consult your pharmacist or healthcare provider.

Monitoring and Follow-up During Clotrimazole Treatment

While using Clotrimazole 10mg troche, it’s important to monitor your condition and follow up with your healthcare provider as recommended. This may include:

1. Regular check-ups to assess the effectiveness of the treatment
2. Liver function tests, especially if you have a history of liver disease or are on long-term treatment
3. Reporting any persistent or worsening symptoms to your healthcare provider
4. Discussing any new medications or changes in your health status with your doctor

How long does it typically take for Clotrimazole 10mg troche to show effects? The response to treatment can vary among individuals. Some people may start to notice improvement in their symptoms within a few days of starting treatment. However, it’s important to complete the full course of treatment as prescribed, even if symptoms improve, to ensure the infection is fully cleared. If you don’t see improvement after a week of treatment, consult your healthcare provider.

Alternative Treatments and Complementary Approaches

While Clotrimazole 10mg troche is an effective treatment for oral thrush, there may be situations where alternative treatments are considered. These could include:

• Other antifungal medications such as nystatin or fluconazole
• Probiotics to help maintain a healthy balance of microorganisms in the mouth
• Dietary changes to reduce sugar intake, which can feed yeast growth
• Good oral hygiene practices to prevent recurrence of infections

Are there any natural alternatives to Clotrimazole for treating oral thrush? Some people may consider natural remedies like coconut oil, tea tree oil, or garlic for their antifungal properties. However, the effectiveness of these treatments for oral thrush is not well-established through scientific research. It’s important to consult with a healthcare provider before trying any alternative treatments, especially if you have a severe infection or are immunocompromised.

In conclusion, Clotrimazole 10mg troche is a valuable medication for treating and preventing oral yeast infections. By understanding its proper use, potential side effects, and necessary precautions, patients can maximize the benefits of this treatment while minimizing risks. Always consult with your healthcare provider for personalized advice and follow-up care during your treatment with Clotrimazole.

Clotrimazole Uses, Side Effects & Warnings

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Generic name: clotrimazole [ kloe-TRIM-a-zole ]
Brand name: Mycelex Troche
Dosage form: oral lozenge (10 mg)
Drug classes: Azole antifungals, Mouth and throat products

Medically reviewed by Drugs.com on Jun 13, 2023. Written by Cerner Multum.

What is clotrimazole?

Clotrimazole is used to treat and prevent yeast infections of the mouth and throat in adults and children older than 3 years.

The clotrimazole lozenge is not absorbed through your stomach. clotrimazole will not treat fungal infections in any other part of your body.

Clotrimazole may also be used for purposes not listed in this medication guide.

Warnings

Use only as directed. Tell your doctor if you use other medicines or have other medical conditions or allergies.

Before taking this medicine

You should not use clotrimazole if you are allergic to it.

Tell your doctor if you have ever had liver disease.

Tell your doctor if you are pregnant or breastfeeding.

How should I take clotrimazole?

Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.

Clotrimazole is usually given 3 to 5 times per day. Allow the lozenge to dissolve slowly in your mouth without chewing.

You may need liver function tests.

Store at room temperature away from moisture and heat. Avoid freezing.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking clotrimazole?

Follow your doctor’s instructions about any restrictions on food, beverages, or activity.

Clotrimazole side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Common side effects of clotrimazole may include:

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Clotrimazole dosing information

Usual Adult Dose for Oral Thrush:

Treatment: 10 mg orally 5 times a day for 14 days

Prophylaxis: 10 mg orally 3 times a day for the duration of chemotherapy OR until steroids are reduced to maintenance levels

Comment:
-Safety and efficacy of treatment doses given for a prolonged duration have not been established. Treatment should be limited to short-term use when possible.

Uses:
-Local treatment of oropharyngeal candidiasis that has been confirmed by a KOH smear of other culture before treatment.
-Prophylaxis to reduce the incidence of oropharyngeal candidiasis in patients who are immunocompromised (e.g., chemotherapy, radiotherapy, steroid therapy in the treatment of leukemia, solid tumors, or renal transplantation)

Usual Pediatric Dose for Oral Thrush:

3 years and older:
Treatment: 10 mg orally 5 times a day for 14 days

Prophylaxis: 10 mg orally 3 times a day for the duration of chemotherapy OR until steroids are reduced to maintenance levels

Comment:
-Safety and efficacy of treatment doses given for a prolonged duration have not been established. Treatment should be limited to short-term use when possible.

Uses:
-Local treatment of oropharyngeal candidiasis that has been confirmed by a KOH smear of other culture before treatment.
-Prophylaxis to reduce the incidence of oropharyngeal candidiasis in patients who are immunocompromised (e.g., chemotherapy, radiotherapy, steroid therapy in the treatment of leukemia, solid tumors, or renal transplantation)

What other drugs will affect clotrimazole?

Clotrimazole is not absorbed through your stomach and is not likely to be affected by other drugs you use. However, tell your doctor about all your current medicines, including prescription and over-the-counter medicines, vitamins, and herbal products.

Frequently asked questions

• What are the most common skin conditions? (with photos)

More about clotrimazole

• Check interactions
• Compare alternatives
• Reviews (42)
• Drug images
• Side effects
• Dosage information
• During pregnancy
• Support group
• Drug class: azole antifungals
• Breastfeeding
• En español

Patient resources

• Advanced Reading
• Clotrimazole (Oral)

Other brands

Mycelex Troche

Professional resources

• Prescribing Information

Related treatment guides

• Oral Thrush

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer

Copyright 1996-2023 Cerner Multum, Inc. Version: 2.01.

Clotrimazole – StatPearls – NCBI Bookshelf

Continuing Education Activity

Clotrimazole is a medication used in the management and treatment of fungal infections. It is in the imidazole class of drugs. This activity outlines the indications, action, and contraindications for clotrimazole as a valuable agent in the treatment of fungal infections.

Objectives:

• Identify the mechanism of action of clotrimazole.

• Describe the adverse effects of clotrimazole.

• Review the appropriate monitoring for toxicity of clotrimazole.

• Discuss interprofessional team strategies for improving care coordination and communication to advance appropriate antifungal treatment, identify warning signs of serious illness, and improve health outcomes.

Access free multiple choice questions on this topic.

Indications

Clotrimazole is a synthetic imidazole with a broad spectrum of antimycotic activity.[1] Clotrimazole is an FDA-approved drug to treat oral candidiasis, vaginal candidiasis, and dermatomycoses. Clotrimazole is effective in the treatment of skin infections such as athlete’s foot, jock itch, ringworm, pityriasis versicolor, intertrigo, and erythrasma.[2][3]

In addition, clotrimazole has some activity against certain gram-positive bacteria, and at very high concentrations, has activity against Trichomonas spp.[4] In adults and children older than 12 years, the FDA has approved the use of clotrimazole in combination with betamethasone propionate (corticosteroid) for the topical treatment of inflammatory tinea due to Epidermophyton floccosum and Trichophyton. However, caution should be exercised, as the use of such combinations can aggravate fungal infections.[5]

Mechanism of Action

Clotrimazole exerts its action primarily by damaging the permeability barrier in the fungal cytoplasmic membrane. [6] Clotrimazole thereby inhibits the biosynthesis of ergosterol in a concentration-dependent manner by inhibiting the demethylation of 14 alpha lanosterol.[7] When ergosterol synthesis becomes inhibited, the cell can no longer construct an intact and functional cell membrane.[8] Ergosterol also directly promotes the growth of fungal cells in a hormone-like fashion; therefore, the rapid onset of the above events leads to a dose-dependent inhibition of fungal growth.

Though clotrimazole exerts its anti-fungal action by decreasing ergosterol biosynthesis, clotrimazole exerts other pharmacological actions. These include the inhibition of sarcoplasmic reticulum ca2+ ATPase, depletion of intracellular calcium, and blocking of calcium-dependent potassium channels and voltage-dependent calcium channels.[9][10] Such action of clotrimazole on different cell targets accounts for other effects of this drug that are separate from its antimycotic activities.[1]

Administration

Clotrimazole is available as topical lotions, powders, oral lozenges, and vaginal inserts/tablets under various tradenames approved by the FDA.

Oral Administration of Other Oral Formulations

• Transmucosal administration

• Patients should slowly dissolve troches in the mouth, do not chew.

Topical Administration Cream/Ointment/Lotion Formulations

• Rub cream or solution gently into the cleansed affected skin.

• Topical preparations should not be used in the eye; or used intravaginally.

Intravaginal Administration

Intravaginal application is only for those clotrimazole products labeled for intravaginal use. Some commercially available preparations contain both intravaginal tablets and vaginal cream in a combination package.  The intravaginal cream may be applied externally to the affected area (vulva) to relieve itching and discomfort.

Use a special applicator supplied by the manufacturer.

Instruct patients on proper administration and treatment courses.

Patients should not use tampons, douches, or spermicides during treatment. The patient should also receive instruction to abstain from sexual activity during treatment. Vaginal clotrimazole products may cause damage to condoms, diaphragms, and cervical caps and cause them to fail.

Vaginal Dosage (vaginal cream) Adult Females

• One applicatorful of 1% cream (50 mg) vaginally for seven days or one applicatorful of 2% cream (100 mg) vaginally for three days, applied at bedtime.

• External application of the cream may also is an option if there are extra-vaginal symptoms. Guidelines recommend treatment for seven days for pregnant patients and 7 to 14 days for immunocompromised patients.[11][12]

Adolescent Females 12 to 17 years

• Apply one applicatorful of 1% cream (50 mg) vaginally for seven days or one applicatorful of 2% cream (100 mg) vaginally at bedtime for three days. External application of the cream may also are an option if there are extra-vaginal symptoms. Guidelines recommend treatment for seven days for pregnant patients and 7 to 14 days for immunocompromised patients.

For the Treatment of Oropharyngeal Candidiasis (thrush) Transmucosal Dosage

Children and Adolescents 3 to 17 years

For the Treatment of Tinea Versicolor Topical

Adults

• Apply to the affected skin and surrounding areas twice daily, both morning and evening.

Children and Adolescents

• Apply to the affected skin and surrounding areas twice daily, both morning and evening.

Adverse Effects

The adverse effects of oral formulation include itching, nausea, and vomiting. More than 10% of patients using the oral formulation may have abnormal liver function tests. For this reason, liver function tests should have periodic monitoring when taking oral clotrimazole (troche). When using clotrimazole to treat vulvovaginal candidiasis, <10% of patients have a vulvar or vaginal burning sensation. Other side effects include rash, hives, blisters, burning, itching, peeling, redness, swelling, pain, or other signs of skin irritation. [14] For topical formulations, it should be used externally and discontinued if irritation or sensitivity develops at the administration site.

Contraindications

Onychomycosis

Topical clotrimazole is not effective for onychomycosis. Therefore, fungal nail infections usually require treatment with an oral (systemic) antifungal drug.

Pregnancy

Clotrimazole demonstrates poor absorption after dermal or intravaginal administration. Only topical preparations are recommended in pregnancy.[15] There are inadequate well-controlled human studies with the use of topical or intravaginal clotrimazole during the first trimester of pregnancy clotrimazole should only be used if indicated.[16] However, clinical trials showed intravaginal clotrimazole to be safe in clinical trials during the second and the third trimester of pregnancy and are recommended for use.[17][12] 

Clotrimazole is not known to cross the placenta.[11] FDA classifies clotrimazole as a class C drug in pregnancy risk classification. There are no adequate, well-controlled studies for oral clotrimazole in pregnant women. There have been no teratogenic effects demonstrated after clotrimazole therapy in pregnancy.[17] In animal studies with dosing up to 200 times the human dose, doses of 100 times the adult human dose have been embryotoxic in rats and mice. There are well-controlled studies in humans; hence the use of oral clotrimazole lozenges during pregnancy should only be an option if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

The use of clotrimazole during breastfeeding has not been studied. No data is available about the excretion of clotrimazole in breast milk. Topical clotrimazole poses little risk to nursing infants as topical clotrimazole is not expected to result in significant maternal absorption.[18] Instruct mothers not to apply clotrimazole topically to the breast during times of breastfeeding. The oral troches should be used only when needed, as this may be systemically absorbed. Report to the FDA if a breastfeeding infant experiences any adverse effects.

Contraceptive Devices, Menstruation

Patients should abstain from sexual intercourse during the treatment course. With intravaginal clotrimazole preparations, contraceptive failures can occur during the treatment due to the damage of contraceptive devices such as diaphragms, condoms, and cervical caps. In addition, tampon use is not advisable while using clotrimazole during menstruation.

Azole Antifungals Hypersensitivity

Patients with azole antifungals hypersensitivity should avoid using clotrimazole. Hypersensitivity reactions commonly occur due to the components in the formulation present in different clotrimazole preparations.

Ocular Exposure, Ophthalmic Administration

If eye contact with clotrimazole occurs, treat immediately by flushing the affected eye with cool, clean water. Contact an ophthalmologist if eye irritation persists.

Drug-drug Interactions

Clotrimazole therapy may result in a significant rise in tacrolimus levels, leading to tacrolimus-associated toxicities. Hence caution should be exercised.[19]

Monitoring

Clotrimazole is not for systemic administration; it is administered via oral/transmucosal lozenges (troches), either topically or intravaginally. Small quantities absorbed are metabolized in the liver and excreted in the bile.

Oral Route

Transmucosal Route – clotrimazole oral lozenges are used for local treatment and are not significantly bioavailable. Concentrations persisting in saliva appear to be due to clotrimazole binding to the oral mucosa.

Topical Route

There is minimal systemic absorption following topical application of clotrimazole.

Other Routes

Intravaginal Route – roughly 5 to 10% of clotrimazole undergoes absorption following vaginal use. Therefore, fungicidal concentrations can persist in the vagina for up to 3 days after application.

Toxicity

When clotrimazole is applied locally and topically, toxic effects such as pelvic cramps, hives, skin rash, occasional headache, itching, and irritation of the vulva and vagina may be observed. Stop the medication if there are any adverse effects.

Enhancing Healthcare Team Outcomes

With any atypical symptoms, careful evaluation and reassessment should take place before prescribing or dispensing clotrimazole. Vaginal candidal infections can co-exist with other sexually transmitted infections. Hence symptoms such as foul-smelling vaginal discharge, abdominal pain, or fever higher than 100 degrees F may indicate another vaginal infection or pelvic inflammatory disease. 

The clinician or the nurse practitioner should also counsel the patient on the importance of reading labels to understand the possible side effects and avoid drug-related toxicities due to overdosing. Pharmacists should also check for any associated drug interactions and inform the prescriber and the patient of any concerns. Clinicians, nurses, physician assistants, and pharmacists should cooperate with interprofessional team strategies to advance appropriate antifungal treatment, identify warning signs of serious illness, and improve health outcomes.  [level 5]

Review Questions

• Access free multiple choice questions on this topic.

• Comment on this article.

References

1.

Crowley PD, Gallagher HC. Clotrimazole as a pharmaceutical: past, present and future. J Appl Microbiol. 2014 Sep;117(3):611-7. [PubMed: 24863842]

2.

Woo TE, Somayaji R, Haber RM, Parsons L. Diagnosis and Management of Cutaneous Tinea Infections. Adv Skin Wound Care. 2019 Aug;32(8):350-357. [PubMed: 31335433]

3.

Kalra MG, Higgins KE, Kinney BS. Intertrigo and secondary skin infections. Am Fam Physician. 2014 Apr 01;89(7):569-73. [PubMed: 24695603]

4.

Sawyer PR, Brogden RN, Pinder RM, Speight TM, Avery Clotrimazole: a review of its antifungal activity and therapeutic efficacy. Drugs. 1975;9(6):424-47. [PubMed: 1097234]

5.

Ely JW, Rosenfeld S, Seabury Stone M. Diagnosis and management of tinea infections. Am Fam Physician. 2014 Nov 15;90(10):702-10. [PubMed: 25403034]

6.

Haller I. Mode of action of clotrimazole: implications for therapy. Am J Obstet Gynecol. 1985 Aug 01;152(7 Pt 2):939-44. [PubMed: 3895959]

7.

Hitchcock CA, Dickinson K, Brown SB, Evans EG, Adams DJ. Interaction of azole antifungal antibiotics with cytochrome P-450-dependent 14 alpha-sterol demethylase purified from Candida albicans. Biochem J. 1990 Mar 01;266(2):475-80. [PMC free article: PMC1131156] [PubMed: 2180400]

8.

Ghannoum MA, Rice LB. Antifungal agents: mode of action, mechanisms of resistance, and correlation of these mechanisms with bacterial resistance. Clin Microbiol Rev. 1999 Oct;12(4):501-17. [PMC free article: PMC88922] [PubMed: 10515900]

9.

Bartolommei G, Tadini-Buoninsegni F, Hua S, Moncelli MR, Inesi G, Guidelli R. Clotrimazole inhibits the Ca2+-ATPase (SERCA) by interfering with Ca2+ binding and favoring the E2 conformation. J Biol Chem. 2006 Apr 07;281(14):9547-51. [PubMed: 16452481]

10.

Jan CR, Tseng CJ, Chou KJ, Chiang HT. Novel effects of clotrimazole on Ca2+ signaling in Madin Darby canine kidney cells. Life Sci. 2000;66(23):2289-96. [PubMed: 10855950]

11.

Sobel JD. Use of antifungal drugs in pregnancy: a focus on safety. Drug Saf. 2000 Jul;23(1):77-85. [PubMed: 10915033]

12.

Sexually Transmitted Diseases: Summary of 2015 CDC Treatment Guidelines. J Miss State Med Assoc. 2015 Dec;56(12):372-5. [PubMed: 26975162]

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Pappas PG, Kauffman CA, Andes DR, Clancy CJ, Marr KA, Ostrosky-Zeichner L, Reboli AC, Schuster MG, Vazquez JA, Walsh TJ, Zaoutis TE, Sobel JD. Clinical Practice Guideline for the Management of Candidiasis: 2016 Update by the Infectious Diseases Society of America. Clin Infect Dis. 2016 Feb 15;62(4):e1-50. [PMC free article: PMC4725385] [PubMed: 26679628]

14.

Jelen G, Tennstedt D. Contact dermatitis from topical imidazole antifungals: 15 new cases. Contact Dermatitis. 1989 Jul;21(1):6-11. [PubMed: 2530045]

15.

van Schalkwyk J, Yudin MH., INFECTIOUS DISEASE COMMITTEE. Vulvovaginitis: screening for and management of trichomoniasis, vulvovaginal candidiasis, and bacterial vaginosis. J Obstet Gynaecol Can. 2015 Mar;37(3):266-274. [PubMed: 26001874]

16.

Black RA, Hill DA. Over-the-counter medications in pregnancy. Am Fam Physician. 2003 Jun 15;67(12):2517-24. [PubMed: 12825840]

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Czeizel AE, Tóth M, Rockenbauer M. No teratogenic effect after clotrimazole therapy during pregnancy. Epidemiology. 1999 Jul;10(4):437-40. [PubMed: 10401880]

18.

Spencer JP, Gonzalez LS, Barnhart DJ. Medications in the breast-feeding mother. Am Fam Physician. 2001 Jul 01;64(1):119-26. [PubMed: 11456429]

19.

Vasquez E, Pollak R, Benedetti E. Clotrimazole increases tacrolimus blood levels: a drug interaction in kidney transplant patients. Clin Transplant. 2001 Apr;15(2):95-9. [PubMed: 11264634]

Disclosure: Neil Khatter declares no relevant financial relationships with ineligible companies.

Disclosure: Moien AB Khan declares no relevant financial relationships with ineligible companies.

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

Contents

• Structural formula

• Russian name

• English title

• 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 cell membrane of fungi), 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

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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

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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.

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Clotrimazole instructions for use: indications, contraindications, side effects – description of Clotrimazole ointment for external use.

approx. 1%: tube 30 g (18636)