Funginil-K Mechanism of Action

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.