Each gram contains: Ketoconazole USP 20 mg.
Pharmacotherapeutic group: Antifungals for Topical Use, Imidazole and triazole derivatives.
Pharmacology: Pharmacodynamics: Usually Ketoconazole cream acts rapidly on pruritus, which is commonly seen in dermatophyte and yeast infections, as well as skin conditions associated with the presence of Malassezia spp. This symptomatic improvement is observed before the first signs of healing are observed.
Ketoconazole, a synthetic imidazole dioxolane derivative, has a potent antimycotic activity against dermatophytes such as Trichophyton spp., Epidermophyton floccosum and Microsporum spp. and against yeasts, including Malassezia spp. and Candida spp. The effect on Malassezia spp. is particularly pronounced.
A study in 250 patients has shown that application twice daily for 7 days of Ketoconazole 2% cream vs clotrimazole 1% cream for 4 weeks on both feet demonstrated efficacy in patients with Tinea pedis (athlete's foot) presenting lesions between the toes. The primary efficacy endpoint was negative microscopic KOH examination at 4 weeks. Ketoconazole 2% treatment showed equivalent efficacy to 4 weeks clotrimazole 1% treatment. There was no evidence of relapse following treatment with Ketoconazole cream at 8 weeks.
Pharmacokinetics: Ketoconazole, a synthetic imidazole, has an antimycotic activity against dermatophytes such as Trichophyton spp., Epidermophyton floccosum and Microsporum spp., and against yeast. Ketoconazole does not produce detectable blood levels after topical application.
Plasma concentrations of Ketoconazole were not detectable after topical administration of Ketoconazole cream in adults on the skin. In one study in infants with seborrhoeic dermatitis (n=19), where approximately 40 g of Ketoconazole 2% 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.
Microbiology: Antimicrobial Action: Polyene antifungal antibiotic which appears to act mainly by interfering with the permeability of the cell membrane of sensitive fungi by binding to sterols, chiefly ergosterol. It is reported to be fungistatic at concentrations achieved clinically. It is active against Absidia spp., Aspergillus spp., Basidiobolus spp., Blastomyces dermatitidis, Candida spp., Coccidioides immitis, Canidiobolus spp., Cryptococcus neoformans, Histoplasma capsulatum, Mucor spp., Paracoccidioides brasilliensis, Rhizopus spp., Rhodotorula spp., and Sporothrix schenckii. Other organisms that have been reported to be sensitive. It is inactive against bacteria (including rickettsia) and viruses. Some resistant strains of Candida have been isolated from immunocompromised patients receiving prolonged treatment.
Ketoconazole is 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. Ketoconazole 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 brasilliensis, Trichophyton mentagrophytes and T. rubrum. Some strains of Aspergillus spp., Cryptococcus neoformans, and Sporothrix schenchkii are sensitive. Ketoconazole has activity against some Gram-positive bacteria and some antiprotozoal activity against Leishmania spp. There are reports of Candida albicans acquiring resistance to Ketoconazole. Microbiological interactions for the effects of imidazoles and amphotericin B on each other's antimicrobial activity.
Ketoconazole is indicated for topical application in the treatment of dermatophyte infections of the skin Tinea corporis, Tinea cruris, Tinea manus, and Tinea pedis due to Trichophyton rubrum, as well as in the treatment of cutaneous candidiasis and Tinea (pityriasis) versicolor.
Ketoconazole should be applied to affected areas once daily. Treatment should be continued for a sufficient period, at least until a few days after disappearance of all symptoms. The diagnosis and/or treatment should be reconsidered if no clinical improvement is noted after 4 weeks of therapy. General measures in regard to hygiene should be observed to control sources of infection or re-infection. The usual duration of treatment is: Tinea versicolor (2-3 weeks), yeast infections (2-3 weeks), Tinea cruris (2-4 weeks), Tinea corporis (3-4 weeks), Tinea pedis (4-6 weeks). Or as prescribed by the physician.
Topical Application: Excessive topical application may lead to erythema, edema 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 is contraindicated in individuals who have shown hypersensitivity to any of its ingredients.
Ketoconazole is not for ophthalmic use. Irritation may occur when Ketoconazole is used immediately after prolonged treatment with topical corticosteroids. Therefore, 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 apply Ketoconazole in the evening, and to subsequently and gradually withdraw the steroid therapy over a period of 2-3 weeks. Ketoconazole has been shown to be teratogenic in animals.
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 fetus/newborn child. Animal studies have shown reproductive toxicity at doses that are not relevant to the topical administration of Ketoconazole.
Plasma concentrations of Ketoconazole are not detectable after topical application of Ketoconazole 2% Cream to the skin of non-pregnant humans. There are no known risks associated with the use of Ketoconazole 2% Cream in pregnancy or lactation.
Pruritus, irritation, and burning sensation have been reported during treatment with Ketoconazole.
Also, in rare circumstances, allergic local skin phenomena, such as contact dermatitis, have been associated with Ketoconazole cream or one of its components, namely sodium sulphite or propylene glycol.
Store at temperatures not exceeding 30°C.
D01AC08 - ketoconazole ; Belongs to the class of imidazole and triazole derivatives. Used in the topical treatment of fungal infection.
Funginil-K cream 20 mg/g
15 g x 1's
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