Ketoconazole

FORMULATION
Each gram contains:
Ketoconazole USP……………………20 mg

INDICATION
Ketoconazole is indicated for topical application in the treatment of dermatophytes infections of the skin; tinea corporis, tinea cruris, tinea manus and tinea pedis due to Trichophyton rubrum, Trichophyton mentagrophytes, Microsporum canis and Epidermophyton floccosum, as well as in the treatment of cutaneous candidiasis and tinea (pityriasis) versicolor

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.

CONTRAINDICATIONS
Ketoconazole is contraindicated in individuals who have shown hypersensitivity to any of its ingredients.

WARNINGS
Ketoconazole is not for opthalmic use.

DOSAGE AND ADMINISTRATiON
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: tines versicolor (2-3 weeks), yeast infections (2-3 weeks) tinea cruris (2-4 weeks), tinea corporis (3-4 weeks), tinea pedis (4-6 weeks).

SIDE EFFECTS
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 also associated with Ketoconazole cream or one of its components, namely sodium sulphite or propylene glycol.

ANTIMICROBIAL INTERACTION
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., Crytococcus neoformans, Histoplasma capsulatam, Mucor spp., Paracoccidiodes brasilliensis, Rhizopus spp., Rhodotorula spp., and Sporothrix schenckii. Other organisms that have been reported to be sensitive. It is inactive against bacteria (including ricketssia) and viruses. Some resistant strains of Candida have been isolated from immunocompromised patients receiving prolonged treatment.

ANTIMICROBIAL ACTION
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 anti-microbial activity including activity against Blastomyces dermatitidis, Candida spp., Coccidiodes immitis, Epidermophyton floccosum, Histoplasma capsulatum, Malassezia spp., Microsporum canis, Paracoccidiodes braselliensis, Trichophyton mentagrophytes and T. rubrum. Some strains of Aspergillus spp., Crytoccus 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.

PRECAUTIONS
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 to apply Ketoconazole in the evening, and to subsequently and gradually withdraw the steroid therapy over period of 2-3 weeks. Ketoconazole has been shown to be teratogenic in animals.

PREGNANCY
The safety in pregnancy and lactation has not been established.

STORAGE CONDITION
Store at temperatures not exceeding 300C.

KEEP ALL MEDICINES OUT OF REACH OF CHILDREN

CAUTION
Foods, Drugs, Devices, and Cosmetics Act prohibits dispensing without prescription.

AVAILABILITY
15 grams Aluminum Collapsible tube (Box of 1 ‘s).

“For suspected adverse drug reaction, report to the FDA: www.fda.gov.ph“.