Clotrimazole

Clotrimazole Uses, Dosage, Side Effects, Food Interaction and all others data.

Clotrimazole is a broad spectrum antifungal. It also exhibits activity against Trichomonus, Staphylococci, Streptococci and Bacteroides. Clotrimazole kills fungi and yeasts by interfering with their cell membranes. It works by stopping the production of ergosterol, which is an essential component of fungal cell membranes resulting in increased membrane permeability and leakage of essential constituents of the fungal cells. Clotrimazole acts reliably on dermatophytes, yeasts and other fungi; it is also effective against Trichomonas vaginalis and Gram-positive microorganisms (streptococci/ staphylococci) and Gram-negative microorganisms (bacteroides/ Haemophilus vaginalis).

Clotrimazole is a broad-spectrum antifungal agent that inhibits the growth of pathogenic yeasts by changing the permeability of cell membranes. The action of clotrimazole is fungistatic at concentrations of drug up to 20 mcg/mL and may be fungicidal in vitro against Candida albicans and other species of the genus Candida at higher concentrations . Unfortunately, resistance to clotrimazole, which was rare in the past, is now common in various patient populations .

Clotrimazole is generally considered to be a fungistatic, and not a fungicidal drug, although this contrast is not absolute, as clotrimazole shows fungicidal properties at higher concentrations .

Trade Name Clotrimazole
Availability Prescription only
Generic Clotrimazole
Clotrimazole Other Names Clotrimazol, Clotrimazole, Clotrimazolum
Related Drugs fluconazole, nystatin, Diflucan, itraconazole, miconazole
Weight 1%w/v, 1%, , 10mg
Type Solution, Cream, Oral Lozenge, Topical Cream, Topical Powder, Topical Solution, Topical Spray
Formula C22H17ClN2
Weight Average: 344.837
Monoisotopic: 344.108026261
Protein binding

98%

Groups Approved, Vet approved
Therapeutic Class Drugs for subcutaneous and systemic mycoses, Topical Antifungal preparations
Manufacturer Karachi Chemical Industries, Amico Laboratories Ltd, Essential Drugs Company Ltd, Tillomed Laboratories Ltd
Available Country Pakistan, Bangladesh, United Kingdom, United States
Last Updated: September 19, 2023 at 7:00 am
Clotrimazole
Clotrimazole

Uses

The confirmed indication for Clotrimazole include:

  • All dermatomycoses due to dermatophytes (e.g. Trichophyton species).
  • All dermatomycoses due to yeasts (Candida species).
  • Dermatomycoses due to moulds and other fungi.
  • Skin diseases showing superinfections with these fungi.

To the dermatomycoses listed under 1-4 belong for example, interdigital myocoses (e.g. athlete’s foot), paronychias (associated with nail mycoses), myocoses in skin folds, Candida vulvitis, Candida balanitis, Pityriasis versicolor, erythrasma.

Clotrimazole rectal preparation is used for vaginal itching, burning and discharge associated with recurrent vaginal yeast infections (Vaginal candidiasis) and also in viginitis due to Candida species as well as Mycotic infections complicated by other microorganisms sensitive to the drug.

Clotrimazole Sterile Eye Ointment is used for the treatment of fungal keratitis due to filamentous fungi and Candida species.

Clotrimazole Ear Drop is used for the treatment of fungal infections of the ear.

Clotrimazole is also used to associated treatment for these conditions: Balanitis candida, Candidiasis, Dermatitis, Dermatomycoses, Ear infection fungal, Erythrasma, Fungal Vaginal Infections, Fungal skin infection, Genital candidiasis, Inflammation, Mixed Vaginal Infections, Oropharyngeal Candidiasis, Pityriasis versicolor, Pyoderma, Ringworm, Skin Infections, Skin candida, Tinea Corporis, Tinea Cruris, Tinea Pedis, Tinea inguinalis, Trichophytosis, Vaginal Candidiasis, Vaginal Mycosis, Vulvitis, Cutaneous candidiasis, Infection mycotic, Susceptible Bacterial Infections, Symptomatic Tinea Corporis caused by Trichophyton mentagrophytes, Trichophyton rubrum, Epidermophyton floccosum, Symptomatic Tinea Cruris caused by Trichophyton mentagrophytes, Trichophyton rubrum, Epidermophyton floccosum, Symptomatic Tinea Pedis caused by Trichophyton mentagrophytes, Trichophyton rubrum, Epidermophyton floccosum, Tinea versicolor caused by Malassezia infection

How Clotrimazole works

Clotrimazole acts primarily by damaging the permeability barrier in the cell membrane of fungi. Clotrimazole causes inhibition of ergosterol biosynthesis, an essential constituent of fungal cell membranes. If ergosterol synthesis is either completely or partially inhibited, the cell is no longer able to construct an intact and functional cell membrane ,. Because ergosterol directly promotes the growth of fungal cells in a hormone‐like fashion, rapid onset of the above events leads to dose-dependent inhibition of fungal growth .

Though decreased ergosterol, due to the inhibition of lanosterol 14-demethylase (also known as CYP51) is accepted to be primarily responsible for the antimycotic properties of clotrimazole, this drug also shows other pharmacological effects. 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 . The action of clotrimazole on these targets accounts for other effects of this drug that are separate from its antimycotic activities .

Dosage

Clotrimazole dosage

Topical

Wash skin with soap and water and dry thoroughly. Apply a thin layer of the cream or solution 2-3 times daily and gently massage over affected area as directed by the doctor. For Athlete’s foot, pay special attention to the spaces between the toes. Best results in Athlete's foot and ringworm are usually obtained with 4 weeks use of this product. The cream should be applied two or three times daily for one month or for at least two weeks after the disappearance of all signs of infection. If satisfactory results have not occurred within these times consultation with doctor is essential. For best results, follow directions and continue treatment for length of time indicated. The duration of treatment varies; it depends among other factors on the extent and localization of the disease.

Recommended duration of treatment :

  • Dermatomycoses: 3-4 weeks
  • Candida vulvitis and candida balanitis: 1-2 weeks
  • Erythrasma and pityriasis versicolor (approx.): 3 weeks
  • In fungal infection of the feet, to prevent relapses:Treatment should be continued for about 2 weeks beyond the disappearance of all signs of disease.

Clotrimazole cream is odourless, can be washed off and does not stain.

Rectal

First infections: In general, a 3-day treatment is sufficient for Candida vaginitis. On 3 consecutive nights, Clotrimazole 200 mg vaginal preparation is inserted as deeply as possible into the vagina. This is best achieved when lying on one's back with the knees slightly bent.

Re-infections: In general, a 6-day treatment is sufficient. This applies also to mixed infections with the above-mentioned causative organisms. On six consecutive nights, 1 Clotrimazole 100 mgvaginal preparation is inserted as deeply as possible into the vagina. If necessary, 2 Clotrimazole 100 mg(1 in the morning and 1 in the evening) or 1 Clotrimazole 200 mg daily can be used for 6-12 days. Treatment should be timed so as to avoid the menstrual period and be finished before the onset of menstruation. To avoid re-infection, the partner should undergo local treatment with Clotrimazole cream at the same time.

Clotrimazole 500 mg vaginal preparation: Single dose, complete treatment with one vaginal tablet. The tablet should be inserted as deeply as possible into the vagina. This is best achieved when lying on one's back with the knees slightly bent. It is recommended that the treatment should be timed so as to avoid the menstrual period. For prevention of re-infection the partner should be treated locally with Clotrimazole cream at the same time.

Clotrimazolevaginal preparation are colorless and do not stain the underwear.

Eye

Adult: It should be applied thinly and evenly to the conjunctival sac every 4 hours daily or as advised by a physician.

Children: Safety and effectiveness in children have been established for Clotrimazole when used as indicated and in the recommended dosage.

Ear

Instill 2-3 drops of Clarizol Ear Drops in the affected ear two or three times daily.The treatment should be continued for at least two weeks after the disappearance of all signs of infection to prevent re-infection.

For the treatment to become a complete success, reliable and sufficiently long application of Clotrimazole cream is important. The duration of treatment varies; it depends among other factors on the extent and localisation of the disease.

Side Effects

Clotrimazole is generally well tolerated after local application but the few side effects have been reported infrequently like erythema, stinging, blistering, peeling, oedema, pruritus, urticaria and general irritation.

Since there is practically no Clotrimazole absorption through the vaginal skin, no systemic effect is expected. The local tolerance of Clotrimazole vaginal tablet is generally good. Local irritation or burning sensation may occur in a very few cases but these symptoms are not considered harmful.

Rarely patients may experience burning or irritation immediately after applying the ointment.

Toxicity

Symptoms of overdose include erythema, stinging, blistering, peeling, edema, pruritus, urticaria, burning, and general irritation of the skin, and cramps. As with all topical agents, skin sensitization may result .

Oral LD50 (rat): 708 mg/kg; Intraperitoneal LD50 (rat): 445 mg/kg; Subcutaneous LDLO (rat): 10 g/kg; Oral LD50 (mouse): 761 mg/kg; Subcutaneous LDLO (mouse): 10 g/kg; Intraperitoneal LD50 (mouse): 108 mg/kg;

Overdose

This drug poses no risk of acute intoxication, as it is unlikely to occur following a single vaginal or dermal application of an overdose (application over a large area under conditions favorable to absorption) or accidental oral ingestion. There is no specific antidote .

Effects on Fertility

No human studies of the effects of clotrimazole on fertility have been conducted; however, animal studies have not shown any effects on the drug on fertility .

Use in Pregnancy

There are limited data regarding the use of clotrimazole in pregnant women. Animal studies do not show direct or indirect harmful effects on reproduction. Although the topical application of clotrimazole may result in very low serum and tissue levels, the use of clotrimazole topical cream by pregnant women is not recommended unless it is advised by the prescribing physician. Clotrimazole topical cream should not be used in the first trimester of pregnancy unless it is considered by the physician to be essential to patient well-being .

Use in Breastfeeding

Available pharmacodynamic/toxicological studies in animals have shown excretion of clotrimazole/metabolites in breastmilk. Clotrimazole should not be administered during breastfeeding. Although the topical application of clotrimazole has resulted in very low serum and tissue levels, the use of clotrimazole topical cream by lactating women is not recommended unless it recommended by the prescribing physician .

Precaution

If local intolerance develops, consider withdrawal of the medicine and institution of appropriate therapy. Clotrimazole solution is not intended for ophthalmic use. Avoid contact with eyes upon topical application. Children 3 yrs. Pregnancy, lactation. If irritation or sensitivity develops with the use of Clotrimazole ointment, treatment should be discontinued.

Interaction

There have been reports of a heat reaction when this medication used concomitantly with Sofradex drops in the ear.

Antagonism with polyene antibiotics.

Food Interaction

No interactions found.

Clotrimazole Disease Interaction

Moderate: hepatic dysfunction

Volume of Distribution

The topical form is minimally absorbed in the serum and tissues . Clotrimazole is a lipophilic drug , and has been shown to be secreted in breastmilk in animal studies . There are limited data available regarding the volume of distribution following oral troche administration.

Elimination Route

Because clotrimazole is generally not significantly absorbed, drug interactions are not a major issue with its use .

Elimination Route

Mainly hepatic .

Pregnancy & Breastfeeding use

Pregnancy:Clotrimazole is recommended during pregnancy only after first consulting a doctor.

Lactation:Because systemic absorption of clotrimazole following topical application is marginal, there should be no risk for the infant during lactation.

Contraindication

Hypersensitivity to clotrimazole.

Acute Overdose

Supportive measures should be taken incase of accidental oral ingestion.

In case of accidental oral ingestion, supportive measures should be taken.

Interaction with other Medicine

There have been reports of a heat reaction when this medication used concomitantly with Sofradex drops in the ear.

Storage Condition

Store at a cool and dry place. Protect from light. Do not freeze.

Innovators Monograph

You find simplified version here Clotrimazole

Clotrimazole contains Clotrimazole see full prescribing information from innovator Clotrimazole Monograph, Clotrimazole MSDS, Clotrimazole FDA label

FAQ

What is Clotrimazole used for?

Clotrimazole is used to treat vaginal yeast infections, oral thrush, diaper rash, pityriasis versicolor, and types of ringworm including athlete's foot and jock itch. It is also used to treat skin infections such as athlete's foot, jock itch, ringworm, and other fungal skin infections (candidiasis). Clotrimazole is used to treat skin infections caused by a fungus (yeast).

How safe is Clotrimazole?

Food and Drug Administration and is safe and effective when used according to the Clotrimazole facts label directions.

How does Clotrimazole work?

Clotrimazole work by killing the fungus (yeast) that is causing the infection. Clotrimazole kills fungus by causing holes to appear in its cell membrane and the contents leak out.

What are the common side effects of Clotrimazole?

Common side effects of Clotrimazole are include: Burning, stinging, swelling, irritation, redness, pimple-like bumps, tenderness, or flaking of the treated skin may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Is Clotrimazole safe during pregnancy?

Clotrimazole is generally considered safe for pregnant women to use. If you are using the pessary to treat vaginal thrush during pregnancy it is recommended that you insert it with your fingers rather than with the applicator provided.

Is Clotrimazole safe during breastfeeding?

Clotrimazole is generally considered safe to use while you're breastfeeding. If your baby is being treated for oral thrush you can carry on breastfeeding but you'll need to be treated at the same time. Apply Clotrimazole cream on and around your nipples after each time you breastfeed your baby.

Can I drink alcohol with Clotrimazole?

Yes, you can drink alcohol while using Clotrimazole.

When should be taken of Clotrimazole?

Apply Clotrimazole to the affected area 2 to 3 times a day. It will work better if you use it 3 times a day. If the affected area is large or hairy, it's best to use either the spray or solution.

Should Clotrimazole be taken with food?

Do not eat or drink while Clotrimazole is in your mouth.

How long does Clotrimazole take to work?

Clotrimazole usually takes 7 days for fungal infections to improve. Apply Clotrimazole to the infected area 2 or 3 times a day for at least 2 weeks.

What is the half life of Clotrimazole?

The elimination half-life of Clotrimazole is 3.5-5 hours.

Can I take Clotrimazole for long time?

Do not use Clotrimazole cream, spray or solution for more than 4 weeks, unless a doctor tells you to.

What happens if I use too much Clotrimazole?

Using too much of this medicine or using it for a long time may increase your risk of having adrenal gland problems. The risk is greater for children and patients who use large amounts for a long time.

When should I not use Clotrimazole?

Do not use Clotrimazole cream, spray or solution for more than 4 weeks, unless a doctor tells you to. A fungal infection can become resistant to Clotrimazole, which means it will no longer work properly.

How many times a day can I use Clotrimazole?

Adults and children use two times a day, morning and evening.

Does Clotrimazole stop itching?

Clotrimazole reduces vaginal burning, itching, and discharge that may occur with this condition.

Does Clotrimazole raise blood sugar?

Clotrimazole can raise blood glucose level by antagonizing the action and suppressing the secretion of insulin, which results in inhibition of peripheral glucose uptake and increased gluconeogenesis.

Can a man use Clotrimazole cream?

Clotrimazole can be used for men and women.

Will Clotrimazole cure toenail fungus?

Over the counter fungal creams like Clotrimazole don't work well for treating toenail fungus.

Does Clotrimazole affect the liver?

The cause of the serum enzyme elevations during Clotrimazole therapy is unknown, but many of the antifungal azoles have been implicated in causing liver injury.

Can I overdose on Clotrimazole?

An overdose of Clotrimazole topical is not expected to be dangerous. Seek emergency medical attention if anyone has accidentally swallowed the medication.

What happens if I stop taking Clotrimazole?

Stopping the Clotrimazole too early may allow fungus to continue to grow, which may result in a relapse of the infection. Inform your doctor if your condition persists or worsens.

Does Clotrimazole dry out skin?

 Burning, tingling, dry skin, or stinging may occur.

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*** Taking medicines without doctor's advice can cause long-term problems.
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