Exelderm

Topical Dermatological Antifungals

Wash hands before and after use. Use universal precautions (i.e., gloves) for application, if needed.
Cleanse the affected area and dry thoroughly prior to application.
In the treatment of cutaneous Candida infections, occlusive dressings should be avoided, since these dressings provide favorable conditions for yeast growth.

Cream: Apply a thin layer to the affected and surrounding areas. Gently rub into the skin. Do not use intravaginally.

erythema / Early / 1.0-1.0

pruritus / Rapid / 1.0-3.0
skin irritation / Early / 1.0-3.0

Exelderm

Rx

A topical azole antifungal used or a variety of fungal and yeast infections, like tinea and cutaneous candidiasis; available as a cream and a solution.

Apply topically to the cleansed, dry, affected area(s) once or twice daily, morning and evening, for 3 weeks.

Apply topically to the cleansed, dry, affected area(s) twice daily, morning and evening, for 4 weeks. For chronic moccasin-type (dry-type) tinea pedis, 4—8 weeks of therapy may be needed.

Applied topically to the affected area(s) once or twice daily for three weeks for interdigital or intertriginous forms of candidiasis resulted in a negative KOH prep in 100% of patients and a negative culture result in 87.5% and in 100% of patients, respectively.

†Indicates off-label use

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

Nystatin: (Moderate) The combination of sulconazole and nystatin represents duplication of therapy whenever the drugs are used by similar routes and are usually avoided.

Exelderm/Sulconazole/Sulconazole Nitrate Topical Cream: 1%
Exelderm/Sulconazole/Sulconazole Nitrate Topical Sol: 1%

2 applications/day.

2 applications/day.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Mechanism of Action: Sulconazole inhibits the cytochrome P-450 isoenzyme, C-14-alpha demethylase by binding to the heme iron of the enzyme. This results in a largely fungistatic effect. The selectivity of azole antifungal agents for pathogenic organisms compared with mammalian cells appears to depend on a preferred affinity of these drugs for fungal versus mammalian cytochrome P-450 sterol demethylases. Enzyme inhibition by sulconazole prevents the synthesis of ergosterol, a sterol found in fungal cell membranes but, in general, not in mammalian cell membranes. Additionally, lanosterol accumulates, which changes membrane permeability, cell volume, secondary metabolic effects, and causes defective cell division and growth inhibition. As sulconazole is primarily fungistatic, an intact immune system may be needed for infection resolution.In selected situations, sulconazole may have growth phase-dependent fungicidal activity against very susceptible organisms. The 1% concentration of sulconazole may greatly exceed the minimum inhibitory concentration and exert a direct physiochemical effect on the fungal cell membrane. The fungicidal effect may be due to hydrophobic interactions between sulconazole and unsaturated fatty acids in the membrane. Mammalian cells generally have little or no unsaturated fatty acids. Sulconazole may also prevent DNA and RNA synthesis and increase their degradation.Sulconazole has activity against many dermatophytes and yeast. One measure of the drug's antifungal activity is the relative inhibition factor (RIF). The RIF approaches 0% for a drug to which a fungus is highly sensitive and 100% for a drug that is non-inhibitory. The RIF values of sulconazole for Candida species, Aspergillus species, and dermatophytes are broadly similar to those of clotrimazole, econazole, ketoconazole, miconazole, and tioconazole. The mean RIF values were 69% (30—98%) for Candida species, 71% (61—82%) for Aspergillus species, and 12% (5—18%) for dermatophytes.

Sulconazole is applied topically to the skin. Systemic exposure is possible with topical use. Eight hours after the topical application of a 1 gram dose of Sulconazole 1% cream to the flexural forearms of healthy adults, approximately 12% was absorbed through the skin regardless of the presence or absence of stratum corneum; while about 80% of the dose was recovered from the skin. Pharmacokinetic values were also measured in a study following the application of 4.5 g of the 1% cream twice daily on the abdomen of healthy adults for one day. In this study, where the skin was not washed for 24 hours and an occlusive dressing was not used, the estimated total skin absorption was 11.28% of the dose. Sulconazole was detected systemically for up to seven days after application. Drug elimination included 6.7% of the dose excreted in the urine and 2% of the dose excreted in the feces.

Eight hours after the topical application of a 1 gram dose of Sulconazole 1% cream to the flexural forearms of healthy adults, approximately 12% was absorbed through the skin regardless of the presence or absence of stratum corneum; while about 80% of the dose was recovered from the skin.

No adequate and well controlled studies have been conducted with topical sulconazole in pregnant women. In animal studies, oral doses of 50 mg/kg/day were not teratogenic in rats or rabbits; however, doses of 125 times the recommended human dose were found to be embryotoxic in rats. Administer sulconazole during pregnancy only if the potential benefits justify the potential risks to the fetus.[40034] [45650]

Data are limited regarding use of sulconazole during breast-feeding, and its' excretion into breast milk is unknown. One study (n=7) estimated that absorption after topical application of the 1% cream was 8.7—11.3% of the total dose, which was the highest reported among the imidazole derivatives. There are no reports describing use during lactation, so the effect of any potential exposure on the nursing infant is unknown. Because sulconazole is systemically absorbed, it may be prudent to use an alternative agent in lactating mothers. Fluconazole, clotrimazole, miconazole, and nystatin may be potential alternatives to consider during breast-feeding. However, site of infection, local susceptibility patterns, and specific microbial susceptibility should be assessed before choosing an alternative agent. If sulconazole is used, avoid direct application to the breast. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.