Sulconazole is an azole antifungal of the imidazole subgroup. It is used topically for a variety of fungal and yeast infections. Sulconazole's mechanism is largely fungistatic, however the in vitro antifungal spectrum is extremely broad. Sulconazole is structurally related to and similarly effective for tinea infections as other imidazole-derivative azole antifungal agents such as clotrimazole, econazole, and miconazole. In some studies of tinea pedis, sulconazole demonstrated a greater efficacy and onset of effect compared to miconazole and clotrimazole. In the management of tinea cruris/corporis, sulconazole 1% cream applied once daily was as effective as twice daily application of clotrimazole 1% cream. In the majority of patients, sulconazole provides relief from the symptoms of tinea infections and cutaneous candidiasis within 2-3 days with clinical improvement usually evident within 1 week. Full resolution of these conditions usually occurs within 3-4 weeks of sulconazole therapy. Sulconazole was approved by the FDA in 1989 and is available as a cream and a solution, which are preferred formulations for fissured or inflamed intertriginous areas such as the toe webs, groin, or scrotum.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Topical Administration
-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/Ointment/Lotion Formulations:
-Cream: Apply a thin layer to the affected and surrounding areas. Gently rub into the skin. Do not use intravaginally.
Skin irritation (primarily burning or a stinging or tingling sensation) and pruritus occurred in 1-3% of patients following cutaneous application of sulconazole nitrate cream or solution; erythema was reported in 1% of sulconazole nitrate cream recipients. Burning or irritation following topical application of sulconazole nitrate may reflect an irritant or contact sensitivity. These symptoms may be due to the vehicle or the fungal infection itself. If symptoms develop after sulconazole treatment or if they worsen, there is a higher likelihood that the drug or the vehicle may be responsible. The majority of these reactions were mild and transient and did not require drug discontinuation. The cream and solution should be used sparingly and discontinued if irritation or hypersensitivity reactions develop.
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.
Safety and efficacy of sulconazole use in children has not been established.
Sulconazole is contraindicated in patients who are hypersensitive to the drug or any ingredient in the formulation. Patients with azole antifungals hypersensitivity (imidazole or triazole derivatives) may react to sulconazole due to cross sensitivity. Statistically significant associations of cross-reactivity with sulconazole were found for miconazole and econazole. However, cross sensitivity appears to be unpredictable, with not all patients exhibiting cross sensitivity. Some patients had a cross-reaction with ketoconazole, isoconazole, and tioconazole, but none of 12 patients treated with clotrimazole had a cross-reaction with sulconazole. Hypersensitivity reactions may also be due to the various vehicles present in the sulconazole formulations. Some of these vehicles have been associated with anaphylactoid reactions. Thirteen out of 25 cases tested resulted in a positive reaction to sulconazole itself.
Sulconazole is only for application to the skin. Ophthalmic administration and vaginal administration should be avoided. Avoid accidental exposure, such as ocular exposure, with use of sulconazole. Hand washing after skin application may minimize the risk of eye exposure. If the eyes are exposed to sulconazole, immediately flush them for 15 minutes with cool, clean water. Contact a doctor if eye irritation persists.
As with many other topical antifungal drugs, topical sulconazole is not effective for onychomycosis. This condition usually requires treatment with an oral (systemic) antifungal drug.
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.
Before initiation of sulconazole, the diagnosis should be confirmed using appropriate microbiologic studies (e.g., direct microscopic examination of potassium hydroxide [KOH] wet mount and/or culture).
Per the manufacturer, this drug has been shown to be active against most strains of the following microorganisms either in vitro and/or in clinical infections: Epidermophyton floccosum, Malassezia furfur, Microsporum canis, Trichophyton mentagrophytes, Trichophyton rubrum
NOTE: The safety and effectiveness in treating clinical infections due to organisms with in vitro data only have not been established in adequate and well-controlled clinical trials.
This drug may also have activity against the following microorganisms: Candida albicans, Candida glabrata, Candida guilliermondii, Candida krusei, Candida parapsilosis, Candida pseudotropicalis, Candida tropicalis, Microsporum audouinii, Microsporum gypseum, Trichophyton tonsurans, Trichophyton violaceum
NOTE: Some organisms may not have been adequately studied during clinical trials; therefore, exclusion from this list does not necessarily negate the drug's activity against the organism.
For the treatment of tinea corporis, tinea cruris, or tinea versicolor:
NOTE: An oral antifungal drug may be needed for extensive disease, dermatophyte folliculitis, nonresponsive disease, or for immunocompromised patients.
Topical dosage (1% cream/solution):
Adults: Apply topically to the cleansed, dry, affected area(s) once or twice daily, morning and evening, for 3 weeks.
For the treatment of tinea pedis:
NOTE: An oral antifungal drug may be needed for extensive disease, dermatophyte folliculitis, nonresponsive disease, or for immunocompromised patients.
NOTE: Topical therapy is not effective for nail involvement (onychomycosis).
Topical dosage (1% cream/solution):
Adults: 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.
For the treatment of cutaneous candidiasis*:
Topical dosage (1% cream/solution):
Adults: 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.
Maximum Dosage Limits:
-Adults
2 applications/day.
-Elderly
2 applications/day.
-Adolescents
Safety and efficacy have not been established.
-Children
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
Nystatin: (Moderate) The combination of sulconazole and nystatin represents duplication of therapy whenever the drugs are used by similar routes and are usually avoided.
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.
-Route-Specific Pharmacokinetics
Topical Route
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.