Full Prescribing Info
Composition: Ketoconazole USP 2.0% w/w; Excipients q.s.
Pharmacology: Pharmacodynamics: Ketoconazole is a broad spectrum synthetic antifungal agent which impairs the synthesis of ergosterol, which is a vital component of fungal cell membranes. Ketoconazole works principally by inhibiting the enzyme cytochrome P450 14-alpha-demethylene (P45014DM).
Ketoconazole has a potent antimycotic action against dermatophytes and yeasts. Ketoconazole cream acts rapidly on the pruritus, which is commonly seen in dermatophyte and yeast infections. This symptomatic improvement often occurs before the first signs of healing are observed.
Pharmacokinetics: Plasma concentrations of ketoconazole were not detectable after topical administration of Cream in adults on the skin. In one study in infants with seborrhoeic dermatitis [n=19], where approximately 40 g of cream was applied daily on 40% of the body surface area, plasma levels of ketoconazole were detected in 5 infants, ranging from 32 to 133 ng/mL.
Ketoconazole Cream, 2% is indicated for the topical treatment of tinea corporis, tinea cruris and tinea pedis caused by Trichophyton rubrum, T. mentagrophytes and Epidermophyton floccosum; in the treatment of tinea (pityriasis) versicolor caused by Malassezia furfur (Pityrosporum orbiculare); and in the treatment of cutaneous candidiasis caused by Candida spp.
Dosage/Direction for Use
To treat cutaneous candidiasis, tinea corporis, tinea cruris, tinea pedis, and tinea (pityriasis) versicolor the recommended dose of ketoconazole cream, 2% is to apply once daily for 2 weeks to cover the affected and immediate surrounding area.
For tinea (pityriasis) versicolor, the recommended dose of ketoconazole cream 2% is to apply once daily for two weeks to cover the affected and immediate surrounding area.
To treat seborrheic dermatitis, apply Ketoconazole cream, 2% to the affected area twice daily for four weeks or until clinical clearing.
Administration: Topical application.
Topical Application: Excessive topical application may lead to erythema, oedema and a burning sensation, which will disappear upon discontinuation of the treatment.
Ingestion: In the event of accidental ingestion, supportive and symptomatic measures should be carried out.
Ketoconazole Cream, 2% is contraindicated in persons who have shown hypersensitivity to the active or excipient ingredients of this formulation.
Special Precautions
Ketoconazole Cream, 2% is not for ophthalmic use.
To prevent a rebound effect after stopping a prolonged treatment with topical corticosteroids it is recommended to continue applying a mild topical corticosteroid in the morning and to apply Ketoconazole 2% cream in the evening and to subsequently and gradually withdraw the steroid therapy over a period of 2-3 weeks.
Ketoconazole Cream, 2% contains sodium sulfite anhydrous, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in non-asthmatic people.
General: If a reaction suggesting sensitivity or chemical irritation should occur, use of the medication should be discontinued. Hepatitis (1:10,000 reported incidence) and, at high doses, lowered testosterone and ACTH induced corticosteroid serum levels have been seen with orally administered ketoconazole; these effects have not been seen with topical ketoconazole.
Carcinogenesis, Mutagenesis, Impairment of Fertility: A long term feeding study in Swiss Albino mice and in Wistar rats showed no evidence of oncogenic activity. The dominant lethal mutation test in male and female mice revealed that single oral doses of Ketoconazole as high as 80 mg/kg produced no mutation in any stage of germ cell development. The Ame's Salmonella microsomal activator assay was also negative.
Teratogenic effects: Use in Pregnancy: Pregnancy Category C: Ketoconazole has been shown to be teratogenic (syndactylia and digodactylia) in the rat when given orally in the diet at 80 mg/kg/day. (10 times the maximum recommended human oral dose.) However, these effects may be related to maternal toxicity which was seen at this and higher dose levels.
Use in Lactation: It is not known whether Ketoconazole Cream, 2% administered topically could result in sufficient systemic absorption to produce detectable quantities in breast milk. Nevertheless, a decision should be made whether to discontinue the drug, taking into account the importance of the drug to the mother.
Use in Children: Safety and effectiveness in Children have not been established.
Effects on ability to drive and use machines: Not Stated.
Use In Pregnancy & Lactation
There are no adequate and well controlled studies in pregnant or lactating women. Data on a limited number of exposed pregnancies indicate no adverse effects of topical ketoconazole on pregnancy or on the health of the foetus / new born child. Animal studies have shown reproductive toxicity at doses that are not relevant to the topical administration of ketoconazole.
Ask the doctor or pharmacist for advice before taking any medicine if pregnant or breast-feeding.
Side Effects
Safety of the ketoconazole cream was evaluated in 1079 subjects who participated in 30 clinical trials. Ketoconazole was applied topically to the skin. Based on pooled safety data from these clinical trials, the most commonly reported (→1% incidence) ADRs were (with % incidence): application site pruritus (2%), skin burning sensation (1.96%), and application site erythema (1%).
Serious Side effects: severe itching, burning, or irritation where the medicine is applied; oily or dry scalp, mild hair loss; redness, pain, or oozing of treated skin areas; or Eye redness, swelling, or irritation.
Less serious side effects include: mild skin itching or irritation; Dry skin; or headache.
If the patient gets any side effects, talk to the doctor or pharmacist. This includes any possible side effects not listed.
Drug Interactions
Ketoconazole cream does not normally react with other medicines. However, tell the doctor or pharmacist if the patient is taking or has recently taken any other medicines. This includes medicines that the patient buys without a prescription or herbal medicines.
Keep tightly closed and Store below 30°C, in a dry place. Protect from sunlight. Do not freeze.
ATC Classification
D01AC08 - ketoconazole ; Belongs to the class of imidazole and triazole derivatives. Used in the topical treatment of fungal infection.
Cream 2% w/w x 5 g x 1's.
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