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Clotrimazole , 2 % cream vaginal

Drug formSoft

ATC categoryAnifungals

ATC subcategoryAzole antifungals (for topical use)

Brand nameClotrimazole

Generic nameClotrimazole

Composition

Each gram of Clotrimazole, vaginal cream 2%, contains:

active ingredient: clotrimazole – 20 mg;
excipients: ceteareth-12, ceteareth-20, paraffin liquid, cetostearyl alcohol, methylparaben, propylparaben, propylene glycol (8%), dimethicone.

Chemical name and CAS number

1-(α-2-Chlorotrityl)imidazole; 23593-75-1.

Pharmacological group and ATC code

Antifungal; A01AB18; D01AC01; G01AF02.

Pharmacology

Clotrimazole, an imidazole derivative, is a synthetic azole antifungal agent.

Mechanism of Action

Clotrimazole exerts its antifungal activity by altering cell membrane permeability, apparently by binding with phospholipids in the fungal cell membrane. In contrast to polyene antibiotics (e.g., amphotericin B), the action of Clotrimazole is less dependent on the sterol content of the cell membrane. As a result of alteration of permeability, the cell membrane is unable to function as a selective barrier, and potassium and other cellular constituents are lost.

Antimicrobial Action

Clotrimazole s an imidazole antifungal that interferes with ergosterol synthesis and therefore alters the permeability of the cell membrane of sensitive fungi. It is reported to be fungistatic at concentrations achieved clinically. Clotrimazole has a wide spectrum of antimicrobial activity including activity against Blastomyces dermatitidis, Candida spp., Coccidioides immitis, Epidermophyton floccosum, Histoplasma capsulatum, Malassezia spp., Microsporum canis, Paracoccidioides brasiliensis, Trichophyton mentagrophytes, and T. rubrum. Some strains of Aspergillus spp., Cryptococcus neoformans, and Sporothrix schenckii are sensitive.

Clotrimazole has activity against some Gram-positive bacteria and some antiprotozoal activity against Leishmania spp.

There are rare reports of Candida albicans acquiring resistance to Clotrimazole.

The emergence of strains of Candida spp. resistant to Clotrimazole has become increasingly important, particularly in immunocompromised patients receiving long-term prophylaxis with clotrimazole. In addition to resistance in C. albicans, infections with C. dubliniensis, C. glabrata, and C. krusei, all of which may be less sensitive to Clotrimazole than C. albicans, have been noted in these patients,and secondary resistance of C. glabrata has been reported during clotrimazole therapy. Cross-resistance with other azoles and with amphotericin B has been reported.

Pharmacokinetics

Absorption of 3 to 10% of a dose has been reported following vaginal administration. Clotrimazole is metabolised in the liver to inactive compounds and excreted in the faeces and urine.

Uses
Clotrimazole vaginal creamis indicated for the treatment vaginal superinfections, suscepted to treatment by clotrimazole.

The cream is indicated for the treatment of candidal vulvitis and balanits.

Dosage and administration
For the treatment of vaginal infections, 1/2 applicatorful of the 2% cream (approximately 2.5 g) may be inserted intravaginally once daily (preferably at bedtime) for 7–14 consecutive days. In patients who do not respond, the diagnosis should be reevaluated before instituting another course of therapy.

Clotrimazole vaginal cream should be administered twice or three time per day for 1-2 weeks in candidal vulvits and balanits.

It may be necessary to treat balanitis in male partners concurrently.

Adverse effects

Although Clotrimazole is usually well tolerated when administered intravaginally, erythema, burning, irritation, cystitis occasionally have occurred.

Precautions and Contraindications
If vulvovaginal candidiasis does not improve within 3 days during medication with Clotrimazole vaginal cream, the patient should consult a physician, as a condition other than vulvovaginal candidiasis may exist.

Clotrimazole is contraindicated in patients who are hypersensitive to the drug or any ingredient in the formulation.

Patients advised to discontinue treatment by Clotrimazole vaginal cream, if abdominal pain, fever occur, such patients should consult a physician immediately.

Pediatric Precautions

Clotrimazole vaginal cream contraindicared in children younger than 12 years of age.

Pregnancy

It is not advised to useClotrimazole vaginal cream in pregnancy.

Lactation

Since it is not known whether Clotrimazole is distributed into milk, the drug should be used with caution in nursing women.

Presentation

Clotrimazole Vaginal cream, 2% is supplied in a aluminum tube (50 g).

Expiry date

3 years. Do not use after the expiration date.

Storage conditions

Store in a cool and dry place, out of the reach of children. Protect from light.

Prescription status

To be dispensed with prescription.