Clotrimazole

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish):

Note. Compounded preparations of clotrimazole may be represented by the following names:

• Co-climasone (PEN) — clotrimazole and betamethasone di-propionate.

Adverse Effects and Precautions

Nausea, vomiting, unpleasant mouth sensations, and pruritus have been reported after the use of oral clotrimazole lozenges.

Raised liver enzyme values have also occurred. Local reactions including irritation and a burning sensation may occur in patients treated topically contact allergic dermatitis has been reported. Intravaginal preparations of clotrimazole may damage latex contraceptives and additional contraceptive measures are therefore necessary during local application.

Gastrointestinal disturbance, elevation of liver enzymes, dysuria, and mental depression have been reported after oral clotrimazole (although this route is no longer used).

Antimicrobial Action

Clotrimazole is an imidazole antifungal with antimicrobial activity similar to that of ketoconazole.

Pharmacokinetics

When applied topically clotrimazole penetrates the epidermis but there is little i any systemic absorption. Absorption of 3 to 10% of a dose has been reported after vaginal use. Clotrimazole is metabolised in the liver to inactive compounds and excreted in the faeces and urine.

Uses and Administration

Clotrimazole is an imidazole antifungal used topically in superficial candidiasis, and in the skin infections pityriasis versicolor and dermatophytosis (see Skin Infections). Clotrimazole may also be used occasionally for symptomatic relie of the protozoal infection trichomoniasis when other drugs are contra-indicated.

Clotrimazole is applied topically two or three times daily for 2 to 4 weeks as a 1% cream, lotion, spray, or solution in the treatment of fungal skin infections a 1% powder may be used with the cream or solution and has been applied to prevent re-infection. The 1% solution is also used topically for fungal otitis externa.

Clotrimazole is given as pessaries in dosage regimens of 100 mg for 6 days, 200 mg for 3 days, or a single dose of 500 mg in the treatment of vulvovaginal candidiasis; similar doses are given as a 1, 2, or 10% vaginal cream. It may be necessary to treat balanitis in male partners concurrently.

For the treatment of oropharyngeal candidiasis one 10-mg lozenge of clotrimazole is dissolved in the mouth five times daily for 14 days.

For the prophylaxis of oropharyngeal candidiasis in patients receiving immu-nosuppressant therapy the dose is one 10-mg lozenge three times daily for the duration of the immunosup-pressant treatment. Clotrimazole has also been given orally but has now been largely superseded by other azole drugs.

Sickle-cell disease

Oral clotrimazole has been investigated for the treatment of sickle-cell disease.

Preparations

British Pharmacopoeia: Clotrimazole Cream Clotrimazole Pessaries

The United States Pharmacopeia: Clotrimazole and Betamethasone Dipropionate Cream Clotrimazole Cream Clotrimazole Lotion Clotrimazole Lozenges Clotrimazole Topical Solution Clotrimazole Vaginal Tablets.

Proprietary Preparations

Multi-ingredient

The symbol denotes a preparation no longer actively marketed.