Sertaconazole

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Sertaconazole
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Rabin Bista, M.B.B.S. [2]

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Overview

Sertaconazole is a azole antifungal that is FDA approved for the treatment of interdigital tinea pedis in immunocompetent patients 12 years of age and older, caused by: Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum. Common adverse reactions include contact dermatitis, dry skin, burning skin, application site skin tenderness.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

  • ERTACZO® (sertaconazole nitrate) cream, 2%, is indicated for the topical treatment of interdigital tinea pedis in immunocompetent patients 12 years of age and older, caused by: Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum

Dosage

  • In the treatment of interdigital tinea pedis, ERTACZO cream, 2%, should be applied twice daily for 4 weeks. Sufficient amount of ERTACZO cream, 2%, should be applied to cover both the affected areas between the toes and the immediately surrounding healthy skin of patients with interdigital tinea pedis.

Not for ophthalmic, oral, or intravaginal use.

DOSAGE FORMS AND STRENGTHS

  • Cream, 2%. Each gram of ERTACZO cream, 2%, contains 17.5 mg of sertaconazole (as sertaconazole nitrate, 20 mg) in a white cream base.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Sertaconazole in adult patients.

Non–Guideline-Supported Use

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding FDA-Labeled Use of Sertaconazole in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Sertaconazole in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Sertaconazole in pediatric patients.

Contraindications

  • None

Warnings

  • Local Adverse Reactions

If irritation develops, treatment should be discontinued and appropriate therapy instituted.

Physicians should exercise caution when prescribing ERTACZO cream, 2%, to patients known to be sensitive to imidazole antifungals, since cross-reactivity may occur.

Adverse Reactions

Clinical Trials Experience

Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug, and may not reflect the rates observed in practice.

In clinical trials, cutaneous adverse events occurred in 7 of 297 (2%) subjects (2 of them severe) receiving ERTACZO® cream, 2%, and in 7 of 291 (2%) subjects (2 of them severe) receiving vehicle. These reported cutaneous adverse events included contact dermatitis, dry skin, burning skin, application site skin tenderness.

In a dermal sensitization trial, 8 of 202 evaluable subjects tested with ERTACZO® cream, 2%, and 4 of 202 evaluable subjects tested with vehicle, exhibited a slight erythematous reaction in the challenge phase. There was no evidence of cumulative irritation or contact sensitization in a repeated insult patch test involving 202 healthy volunteers.

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of ERTACZO cream, 2%. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

In post-marketing surveillance for ERTACZO cream, 2%, the following were reported:

Cutaneous adverse events: erythema, pruritus, vesiculation, desquamation, and hyperpigmentation.

Drug Interactions

There is limited information regarding Sertaconazole Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C

  • There are no adequate and well-controlled studies conducted with ERTACZO cream in pregnant women. ERTACZO cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Reproduction studies have not been performed with ERTACZO cream. Sertaconazole nitrate did not produce any evidence of maternal toxicity, embryotoxicity or teratogenicity in rats and rabbits at an oral dose of 160 mg/kg/day (40 times (rats) and 80 times (rabbits) the maximum recommended human dose based on a body surface area comparison). A reduction in live birth indices and an increase in the number of still-born pups were seen at doses of 80 and 160 mg/kg/day sertaconazole nitrate in an oral peri- and post-natal development study in rats.
Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Sertaconazole in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Sertaconazole during labor and delivery.

Nursing Mothers

  • It is not known if sertaconazole is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when prescribing ERTACZO cream, 2%, to a nursing woman.

Pediatric Use

  • The efficacy and safety of ERTACZO cream, 2%, have not been established in pediatric patients below the age of 12 years.

Geriatic Use

  • Clinical trials of ERTACZO cream, 2%, did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.

Gender

There is no FDA guidance on the use of Sertaconazole with respect to specific gender populations.

Race

There is no FDA guidance on the use of Sertaconazole with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Sertaconazole in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Sertaconazole in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Sertaconazole in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Sertaconazole in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Topical application

Monitoring

There is limited information regarding Monitoring of Sertaconazole in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Sertaconazole in the drug label.

Overdosage

There is limited information regarding Overdose of Sertaconazole in the drug label.

Pharmacology

There is limited information regarding Sertaconazole Pharmacology in the drug label.

Mechanism of Action

  • Sertaconazole, an azole antifungal agent, inhibits fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylase enzyme. This enzyme functions to convert lanosterol to ergosterol. Ergosterol is a key component of fungal cell membranes and lack of this component leads to fungal cell injury by leakage of key constituents in the cytoplasm from the cell.

Structure

  • ERTACZO (sertaconazole nitrate) cream, 2%, is for topical application. It contains the azole antifungal, sertaconazole nitrate. Sertaconazole nitrate contains one asymmetric carbon atom and exists as a racemic mixture of equal amounts of R and S enantiomers.

Sertaconazole nitrate is designated chemically as (±)-1-[2,4-dichloro-β-[(7-chlorobenzo-[b]thien-3-yl)methoxy]phenethyl]imidazole nitrate. It has a molecular weight of 500.8. The molecular formula is C20H15Cl3N2OS ∙ HNO3, and the structural formula is as follows:

This image is provided by the National Library of Medicine.
  • Sertaconazole nitrate is a white or almost white powder. It is practically insoluble in water, soluble in methanol, sparingly soluble in alcohol and in methylene chloride. Each gram of ERTACZO cream, 2%, contains 17.5 mg of sertaconazole (as sertaconazole nitrate, 20 mg) in a white cream base of ethylene glycol, glyceryl isostearate, glycolized saturated glycerides, light mineral oil, methylparaben, polyethylene glycol palmitostearate, polyoxyethylened saturated glycerides, sorbic acid and purified water.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Sertaconazole in the drug label.

Pharmacokinetics

In a multiple dose pharmacokinetic trial that included 5 male subjects with interdigital tinea pedis (range of diseased area, 42 - 140 cm2; mean, 93 cm2), ERTACZO cream, 2%, was topically applied every 12 hours for a total of 13 doses to the diseased skin (0.5 grams sertaconazole nitrate per 100 cm2). Sertaconazole concentrations in plasma measured by serial blood sampling for 72 hours after the thirteenth dose were below the limit of quantitation (2.5 ng/mL) of the analytical method used.

Microbiology

Activity In Vitro and in Clinical Infections: Sertaconazole nitrate has been shown to be active against isolates of the following microorganisms in clinical infections [see INDICATIONS AND USAGE (1)].

Trichophyton rubrum Trichophyton mentagrophytes Epidermophyton floccosum

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility In a rat dermal carcinogenicity study, topical administration of sertaconazole nitrate cream for up to 102 weeks did not increase the number of neoplastic lesions compared to control animals, at sertaconazole nitrate doses of up to 800 mg/kg/day (approximately 200 times the maximum recommended human dose based on a body surface area comparison).

No clastogenic potential was observed in a mouse micronucleus test. Sertaconazole nitrate was considered nonclastogenic in the in vivo mouse sister chromatid exchange assay. There was no evidence that sertaconazole nitrate induced unscheduled DNA synthesis in primary rat hepatocyte cultures.

At oral doses up to 60 mg/kg/day (16 times the maximum recommended human dose based on a body surface area comparison), sertaconazole nitrate exhibited no toxicity or adverse effects on reproductive performance or fertility in male or female rats.

Clinical Studies

In two randomized, double-blind, clinical trials, subjects 12 years and older with interdigital tinea pedis applied either ERTACZO cream, 2%, or vehicle, twice daily for four weeks. Subjects with moccasin-type (plantar) tinea pedis and/or onychomycosis were excluded from the trial. Two weeks after completion of therapy (six weeks after beginning therapy), subjects were evaluated for signs and symptoms related to interdigital tinea pedis.

Treatment outcomes are summarized in the table below.

This image is provided by the National Library of Medicine.

In clinical trials, complete cure in sertaconazole treated subjects was achieved in 32 of 160 (20%) subjects with Trichophyton rubrum, in 7 of 28 (25%) subjects with Trichophyton mentagrophytes and in 1 of 13 (15%) subjects with Epidermophyton floccosum.

How Supplied

  • ERTACZO cream, 2%, is white in color and supplied in tubes in the following size:
60-gram tube NDC 0187-5115-60

Storage

  • Store at 20°C-25°C (68°F-77°F); excursions permitted to 15°-30°C (59°-86°F)

Images

Drug Images

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Package and Label Display Panel

File:Sertaconazole01.png
This image is provided by the National Library of Medicine.
File:Sertaconazole01.png
This image is provided by the National Library of Medicine.

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Sertaconazole in the drug label.

Precautions with Alcohol

  • Alcohol-Sertaconazole interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. ↑ Dellenbach P, Thomas JL, Guerin V, Ochsenbein E, Contet-Audonneau N (2000). "Topical treatment of vaginal candidosis with sertaconazole and econazole sustained-release suppositories". Int J Gynaecol Obstet. 71 Suppl 1: S47–52. PMID 11118564.
  2. ↑ Nasarre J, Umbert P, Herrero E, Roset P, Márquez M, Torres J; et al. (1992). "Therapeutic efficacy and safety of the new antimycotic sertaconazole in the treatment of Pityriasis versicolor". Arzneimittelforschung. 42 (5A): 764–7. PMID 1627203.
  3. ↑ 3.0 3.1 Umbert P, Nasarre J, Bello A, Herrero E, Roset P, Márquez M; et al. (1992). "Phase II study of the therapeutic efficacy and safety of the new antimycotic sertaconazole in the treatment of superficial mycoses caused by Candida albicans". Arzneimittelforschung. 42 (5A): 757–60. PMID 1627201.
  4. ↑ Empty citation (help)
  5. ↑ "http://www.ismp.org". External link in |title= (help)

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