Lotrimin

Antiinfectives and Antiseptics for Local Oral Treatment
Gynecological Antifungals
Topical Dermatological Antifungals

For storage information, see specific product information within the How Supplied section.

Transmucosal Administration
Troches should be dissolved slowly in the mouth, do not chew.

Topical preparations should not be applied to the eye; do not use intravaginally.
Rub cream or solution gently into cleansed affected skin.

Apply intravaginally only those clotrimazole products labeled for intravaginal use.
Some products supply both intravaginal tablets and vaginal cream in a combination package; the intravaginal cream may be applied to the externally to the affected area (vulva) to relieve itching and discomfort.
Use special applicator supplied by the manufacturer.
Instruct patient on proper administration and treatment course.
Instruct patient not to use tampons, douches, or spermicides during the treatment course; the patient should also be instructed to abstain from sexual activity during treatment. Vaginal clotrimazole products may damage condoms, diaphragms, and cervical caps and cause them to fail.

elevated hepatic enzymes / Delayed / 15.0-15.0
vaginal pain / Early / 1.0-10.0
erythema / Early / Incidence not known
edema / Delayed / Incidence not known

skin irritation / Early / 1.0-10.0
vaginal irritation / Early / 1.0-10.0
abdominal pain / Early / 7.0-7.0
nausea / Early / 5.0-5.0
pruritus / Rapid / Incidence not known
urticaria / Rapid / Incidence not known
diarrhea / Early / Incidence not known
vomiting / Early / Incidence not known

Alevazol, Anti-Fungal, Antifungal, Cruex, Desenex, Fungoid, Gyne-Lotrimin, Lotrimin, Lotrimin AF, Lotrimin AF Ringworm, Micotrin AC, Mycelex, Mycelex Troche, Mycozyl AC

OTC, Rx

Imidazole antifungal agent marketed in a variety of preparations including vaginal suppositories and cream, topical lotion and cream, topical solution, and lozenges. Used for infections due to pathogenic dermatophytes, yeasts, and Malassezia furfur including ringworm (dermatophytosis), vaginal and oral candidiasis, and tinea infections. Not indicated for subcutaneous mycoses.

Apply to affected and surrounding area(s) twice daily.

Apply to affected and surrounding area(s) twice daily.

10 mg PO 5 times daily for 7 to 14 days.

10 mg PO 5 times daily for 7 to 14 days.

10 mg PO 3 times daily for the duration of chemotherapy or until steroids are reduced to maintenance levels.

1 applicatorful (50 mg clotrimazole/5 g cream) intravaginally at bedtime for 7 to 14 days in pregnant and non-pregnant patients. External application of the cream may also be used if there are extra-vaginal symptoms. [40267]

1 applicatorful (50 mg clotrimazole/5 g cream) intravaginally at bedtime for 7 to 14 days in pregnant and non-pregnant patients. External application of the cream may also be used if there are extra-vaginal symptoms. [40267]

1 applicatorful (100 mg clotrimazole/5 g cream) intravaginally at bedtime for 3 days in non-pregnant patients. External application of the cream may also be used if there are extra-vaginal symptoms. [45254]

1 applicatorful (100 mg) intravaginally at bedtime for 3 days in non-pregnant patients. External application of the cream may also be used if there are extra-vaginal symptoms. [45254]

1 applicatorful (50 mg clotrimazole/5 g cream) intravaginally at bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.

1 applicatorful (50 mg clotrimazole/5 g cream) intravaginally at bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.

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

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

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

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

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

Progesterone: (Moderate) Vaginal preparations of progesterone (e.g., Crinone, Endometrin, and Prochieve) should not be used with other intravaginal products (e.g., vaginal antifungals, such as clotrimazole, miconazole nitrate, terconazole, or tioconazole vaginal) as concurrent use may alter progesterone release and absorption from the vagina. Separate the times of administration to avoid the interaction. The manufacturers of Crinone and Prochieve indicate that other intravaginal products can be used as long as 6 hours has lapsed either before or after vaginal administration of progesterone. Endometrin is generally not recommended for use with other vaginal products (e.g., antifungal products) as this may alter progesterone release and absorption from the vaginal insert and the potential for interaction has not been formally assessed; use other vaginal products if medically necessary, but be aware that the response to Endometrin may be altered.

Alevazol Topical Ointment: 1%
Antifungal/Anti-Fungal/Clotrimazole/Cruex/Desenex/Lotrimin/Lotrimin AF/Lotrimin AF Ringworm/Micotrin AC/Mycozyl AC Topical Cream: 1%
Clotrimazole/Fungoid/Lotrimin/Lotrimin AF Topical Sol: 1%
Clotrimazole/Gyne-Lotrimin/Mycelex Vaginal Cream: 1%, 2%
Clotrimazole/Mycelex Troche Oropharyngeal Troche: 10mg

50 mg/day PO; 1 applicatorful (50 or 100 mg clotrimazole/5 g cream) intravaginally/day. Maximum dosage not available for topical products.

50 mg/day PO; 1 applicatorful (50 or 100 mg clotrimazole/5 g cream) intravaginally/day. Maximum dosage not available for topical products.

50 mg/day PO; 1 applicatorful (50 or 100 mg clotrimazole/5 g cream) intravaginally/day. Maximum dosage not available for topical products.

12 years: 50 mg/day PO; 1 applicatorful (50 or 100 mg clotrimazole/5 g cream) intravaginally/day. Maximum dosage not available for topical products.
3 to 11 years: 50 mg/day PO. Maximum dosage not available for topical products. Safety and efficacy of other formulations have not been established.
1 to 2 years: Maximum dosage not available for topical products. Safety and efficacy of other formulations have not been established.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Like other azole antifungals, clotrimazole exerts its effect by altering the fungal cell membrane. Clotrimazole inhibits ergosterol synthesis by interacting with 14-alpha demethylase, a cytochrome P-450 enzyme that is necessary for converting lanosterol to ergosterol, an essential component of the membrane. In contrast, amphotericin B binds to ergosterol after it is synthesized. Inhibition of ergosterol synthesis results in increased cellular permeability, causing leakage of cellular contents such as phosphorous-containing compounds and potassium. Clotrimazole does not appear to have the same activity upon human cholesterol synthesis. Other antifungal effects of azole compounds have been proposed and include: inhibition of endogenous respiration, interaction with membrane phospholipids, and inhibition of transformation of yeasts to mycelial forms. Additional mechanisms may involve inhibition of purine uptake and impairment of triglyceride and/or phospholipid biosynthesis.  As a treatment for infectious diarrhea, clotrimazole is thought to interfere with chloride and resulting fluid accumulation in epithelial cells lining the intestine.
 
Clotrimazole inhibits the movement of calcium and potassium ions across the cell membrane. This action may be responsible for in vitro and animal data demonstrating an antitumor effect of clotrimazole. This action may also explain why clotrimazole prevents the dehydration of the red blood cell in patients with sickle cell disease. Clotrimazole inhibits the loss of intracellular potassium by blocking the ion transport pathway known as the Gardos channel.

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

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

There is little systemic absorption following clotrimazole topical application.

Intravaginal Route
Roughly 5—10% of clotrimazole is absorbed after vaginal use. Fungicidal concentrations persist in the vagina for up to 3 days after application.

There are no adequate and well-controlled studies of oral clotrimazole in pregnant women. No teratogenic effects have been demonstrated in animal studies at doses up to 200-times the human dose; however, doses of 100-times the adult human dose were embryotoxic in rats and mice. Use oral clotrimazole lozenges during pregnancy only if the potential benefit justifies the potential risk to the fetus. Clotrimazole is very poorly absorbed after dermal or intravaginal administration. In clinical trials, vaginal use during the second and third trimesters in humans has not resulted in any adverse effects; there are no adequate and well-controlled studies of pregnant women during the first trimester. In animal studies, no fetal harm occurred after intravaginal doses up to 100 mg/kg in pregnant rats. Use topical or vaginal clotrimazole during the first trimester of pregnancy only if clearly indicated; however, CDC guidelines recommend 7 days of therapy with a topical azole preparation (including clotrimazole) for the treatment of vulvovaginal candidiasis that occurs during pregnancy.[40267] [45251] [45253] [45254]

The use of clotrimazole during breast-feeding has not been studied. Topical application is not expected to result in significant maternal absorption, and should not be of significant risk to a breast-feeding infant. Instruct mothers not to apply clotrimazole topically to the breast during times of breast-feeding. The oral troches may be absorbed systemically, but significant infant exposure is unknown and expected to be low; observe the infant for any possible adverse effects. Fluconazole, miconazole, and nystatin may be potential alternatives to consider, though site of infection, local susceptibility patterns, and specific microbial susceptibility should be assessed before choosing an alternative agent. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested or administered drug, health care providers are encouraged to report the adverse effect to the FDA.