Sulconazole

D01AC09

D - Dermatologicals

QD - Dermatologicals

Sulconazole is a broad-spectrum antifungal that inhibits the growth of dermatophytes, yeasts and other filamentous and dimorphic fungi. The relative inhibition factor (RIF), a measurement that represents a fixed portion of the antigungal dose-response curve, can be determined to measure the inhibitory activity of antifungal drugs. Against pathogenic yeasts such as dermatophytes and Aspergilli, sulconazole had similar RIF values compared to other imidazoles. In _in vitro_ conditions, the fungicidal potency of sulconazole depends on its concentration and the growth phase of the inoculum cells. Sulconazole has also shown antibacterial properties _in vitro_, with inhibitory concentrations (MICs) under 12.5 mg/L against several _Staphylococcus_ species, as well as _Streptococcus faecalis_ and several Gram-positive anaerobes.

The mechanism of action of sulconazole is not well established; however, it is thought to be similar to other imidazole derivatives. The function of imidazoles can be attributed to their structural resemblance to purines essential to metabolism. Imidazoles inhibit lanosterol 14-alpha demethylase, a cytochrome P-450-dependent enzyme in fungi responsible for converting lanosterol to ergosterol. Since ergosterol is required to maintain the integrity of the fungi membrane, the inhibition of lanosterol 14-alpha demethylase leads to increased fungal cellular permeability. Therefore, the use of an imidazole such as sulconazole inhibits fungal growth.

5D9HAA5Q5S

SULCONAZOLE

Established Pharmacologic Class [EPC] - Azole Antifungal

Chemical Structure [CS] - Azoles

Sulconazole is an Azole Antifungal.

A study done on healthy subjects given sulconazole 1% cream over a seven-day period, showed that the total percutaneous absorption of sulconazole after topical administration was 8.71-11.3% of the dose. Another study also done on healthy volunteers given 1 g of sulconazole 1% cream, estimated that about 12% of the dose was absorbed through the skin. In general, topical imidazoles are poorly absorbed (<15%); however, sulconazole may have higher levels of absorption compared to others.

About 6.70% of the dose was recovered in urine, and 2.01% in feces over a 7 day collection period. Radioactivity could be detected in both urine and feces at 7 days potentially due to a reservoir effect.