Sulconazole

Summary

Synopsis

Sulconazole is a substituted imidazole antimicrobial agent structurally related to other drugs in this group. It possesses a broad spectrum of activity in vitro against dermato-phytes, yeasts and some Grampositive bacteria. The efficacy and safety of sulconazole 1% cream has been demonstrated in controlled clinical studies in patients with superficial dermatophyte or yeast infections. In these trials, sulconazole generally displayed similar efficacy to clotrimazole, econazole and miconazole, although in a few studies sulconazole produced better and/or quicker improvement than clotrimazole or miconazole in small numbers of patients with tinea pedis. Further studies in larger groups of patients are needed to confirm these encouraging preliminary findings.

Thus, sulconazole is an effective and well tolerated alternative to other topical imidazole drugs in the treatment of superficial fungal infections of the skin.

Pharmacodynamic Properties

Sulconazole possesses a broad spectrum of antifungal activity, inhibiting the growth of dermatophytes, yeasts and various filamentous and dimorphic fungi at concentrations below 5 mg/L in vitro. To overcome inconsistencies in MIC values caused by varying experimental conditions, the determination of relative inhibition factors (RIF) of antifungal drugs has been proposed. It has been shown that against representatives of pathogenic yeasts, dermatophytes and Aspergilli, the RIF values of sulconazole were broadly similar to those of other imidazoles. The fungicidal potency of sulconazole in vitro depends on its concentration and on the growth phase of the inoculum cells. Sulconazole has also demonstrated antibacterial activity in vitro, with MIC values below 12.5 mg/L, against several Staphylococcus species, Streptococcus faecalis and certain Grampositive anaerobes.

It appears that sulconazole exerts antifungal activity through effects which destroy the capacity of the fungal cell membrane to maintain the intracellular environment.

Pharmacokinetic Properties

About 12% of a topically administered (forearm) dose of sulconazole 1% cream was estimated to be percutaneously absorbed in humans. This value varied markedly in different animal species.

Therapeutic Use

In controlled, comparative clinical trials of patients with superficial fungal infections of the skin, sulconazole has demonstrated clear superiority over placebo and was generally of similar overall clinical efficacy to clotrimazole, econazole and miconazole. Treatment was normally administered twice daily for between 2 and 5 weeks in these studies. Two studies showed that compared with clotrimazole, sulconazole possessed significantly greater overall clinical efficacy in patients with tinea cruris or tinea pedis, and it appears that sulconazole may relieve some of the symptoms of tinea pedis (erythema, scaling, pruritus and maceration/erosion) more quickly than clotrimazole. The 2 drugs were otherwise found to be of similar efficacy, with mycological cure achieved in over 70% of patients. No significant differences were reported in the results of 2 comparisons with econazole, both drugs achieving very high cure rates in patients with tinea pedis or tinea cruris. Likewise, sulconazole and miconazole were generally of similar overall clinical efficacy, although in 2 studies of patients with tinea pedis sulconazole tended towards superiority, but the differences were not statistically significant. Sulconazole again tended to cause a more rapid relief of some clinical symptoms.

Reported relapse rates 4 to 12 weeks following the end of treatment were low for sulconazole and the other imidazole antifungal drugs tested. Differences that were observed usually favoured sulconazole.

Side Effects

Sulconazole has generally been very well tolerated in clinical trials. In the largest study, involving 323 patients, the overall incidence rate of adverse effects was 3.4%, with redness, irritation, contact dermatitis and pruritus being the most frequently reported. Few patients have withdrawn from sulconazole treatment due to side effects.

Administration

Sulconazole 1% cream should be rubbed gently into the affected and surrounding skin area twice daily. To minimise the risk of reinfection treatment should continue for 3 weeks in Candida infections, tinea cruris, tinea corporis and pityriasis versicolor, and for 4 weeks in patients with tinea pedis.