Sertaconazole is an imidazole-type antifungal used for the treatment of interdigital tinea pedis in immunocompetent patients. Diagnosis of the disease should be confirmed either by direct microscopic evaluation of infected superficial epidermal tissue in a solution of potassium hydroxide (KOH preparation) or by culture on an appropriate medium. Relief of symptoms is usually seen within 7-14 days. The duration of therapy is typically 4 weeks. Sertaconazole is not indicated for ophthalmic, oral, intravenous, or intravaginal use. Sertaconazole 2% cream (Ertaczo(TM)) is a prescription product which was approved by the FDA in December 2003.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Topical Administration
Cream/Ointment/Lotion Formulations
-For topical administration only.
-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.
-Apply a thin layer of the cream to the affected area between the toes and the immediately surrounding healthy skin of immunocompetent patients with tinea pedis. Gently rub into the skin.
-Avoid the use of occlusive dressings or wrappings.
In clinical trials, cutaneous adverse events were reported in 2% (7/297) patients using sertaconazole, compared to 2% (7 of 291) patients using the placebo (vehicle). Adverse events include contact dermatitis, xerosis, application site reaction, burning, and tenderness. The cream should be used sparingly and discontinued if skin irritation or hypersensitivity reactions develop; then appropriate therapy should be instituted. In non-US post-marketing surveillance for sertaconazole, adverse events reported included contact dermatitis, erythema, pruritus, vesiculation (vesicular rash), desquamation, and skin hyperpigmentation.
Physicians should use caution when prescribing sertaconazole to patients who have a history of azole antifungals hypersensitivity, since cross-reactivity may occur.
As with many other topical antifungal drugs, sertaconazole is not effective for the treatment of onychomycosis. This condition usually requires treatment with an oral (systemic) antifungal drug.
There are no available data for topical sertaconazole use during pregnancy to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal studies, there were no adverse developmental effects observed with oral administration of sertaconazole at doses 40 to 80 times the maximum recommended human dose (MRHD) based on body surface area comparisons. In studies involving pregnant rats, a reduction in live birth indices and an increase in the number of still-born pups was observed at oral doses 20 and 40 times the MRHD based on body surface area. In pharmacokinetic trials, sertaconazole plasma concentrations were below the limit of quantitation (2.5 ng/mL).
There are no data available on the presence of sertaconazole in human or animal milk, its effects on the breastfed infant, or its effects on milk production. However, topical application is not expected to result in significant maternal absorption. Instruct nursing mothers not to apply sertaconazole to the breast. 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. The development and health benefits of breast-feeding should be considered along with the mother's need for sertaconazole cream and any potential adverse effects on the breastfed infant from sertaconazole cream or from the underlying maternal condition.
The safety and efficacy of sertaconazole cream in neonates, infants, and children under the age of 12 has not been established. The manufacturer does not recommend use of topical sertaconazole in pediatric patients less than 12 years of age.
Clinical studies of sertaconazole did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger subjects. However, it is not expected that geriatric patients would respond differently to topical sertaconazole than younger patients.
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, 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.
For the topical treatment of interdigital tinea pedis in immunocompetent patients:
Topical application (cream):
Adults including the Geriatric, Adolescents, and Children >= 12 years: Apply a thin layer of the 2% cream to the cleansed, dry, infected area twice daily for 4 weeks.
Infants and Children < 12 years: Safety and efficacy have not been established.
Maximum Dosage Limits:
-Adults
No maximum dosage information is available.
-Elderly
No maximum dosage information is available.
-Adolescents
>= 12 years: No maximum dosage information is available.
-Children
< 12 years: Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
No dosage adjustment needed.
Patients with Renal Impairment Dosing
No dosage adjustment needed.
*non-FDA-approved indication
Nystatin: (Moderate) The combination of sertaconazole and nystatin represent duplication of therapy whenever the drugs are used by similar route, and is usually avoided.
Sertaconazole, like other azole antifungals, exerts it effect primarily by inhibiting the cytochrome P450-dependent synthesis of ergosterol. Ergosterol is a key component of the cell membrane of fungi, and the lack of this component results in fungal cell injury primarily by leakage of key constituents in the cytoplasm from the cell. Sertaconazole does not appear to have the same effect on human cell cholesterol synthesis. Other antifungal effects of azole compounds have been proposed and include: inhibition of endogenous respiration, interaction with membrane phospholipids, and inhibition of yeast transformation to mycelial phospholipid forms. Other mechanisms may involve inhibition of purine uptake and impairment of triglyceride and/or phospholipid biosynthesis.
The azole antifungals have a broad spectrum of activity against common fungal pathogens including: Blastomyces dermatitidis, Candida species, Cryptococcus neoformans, Coccidiodes immitis, Histoplasma capsulatum, Paracoccidioides brasiliensis, and Sporothrix schenckii. In general, sertaconazole is active against the following organisms: Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
Pharmacokinetics:
Sertaconazole cream is administered topically to the skin.
-Route-Specific Pharmacokinetics
Topical Route
Following topical administration of sertaconazole, systemic absorption is negligible. In a multiple dose pharmacokinetic study of 5 male patients with interdigital tinea pedis, sertaconazole cream 2% was topically applied every 12 hours for a total of 13 doses to the diseased skin. Sertaconazole concentrations in the plasma measured by serial sampling for 72 hours after the thirteenth dose were below the limit of quantitation of the analytical method.