Sertaconazole Nitrate

Generic name: Sertaconazole Nitrate

Therapeutic class: Antifungal

US FDA Approved for the treatment of Tinea pedis.

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Sertaconazole Nitrate
Therapeutic Class: Benzothiophene Imidazole antifungal.

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Role of ATP
ATP
Adenosine Tri Phosphate.
Is an important membrane of all the cells. Without ATP the cell membrane cannot survive.

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Mechanism of Action

Sertaconazole causes direct cell membrane damage within 10 min of exposure by causing leakage of ATP.
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Mechanism of Action
Fungistatic
Lanosterol Sertaconazole Ergosterol
sterol 14 Alpha demethylase

Proper fungal development and growth

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Broad Spectrum of Coverage with low MIC

Dermatophytes: Epidermophyton, Microsporum & Trichophyton Pathogenic yeasts : Candida albicans, Candida tropicalis Malassezia furfur Opportunistic fungi :Aspergillus, Alternaria, Scopulariopsis, Fusarium, Torulopsis & Trichosporon. Activity has also been observed against Trichomonas and some gram-positive organisms (staphylococci & streptococci )
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Broad Spectrum of Coverage with low MIC

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Anti-inflammatory and Anti-itch activity

Sertaconazole inhibits inflammatory mediators released from activated Lymphocytes like IL-2, TNF , IL-4, GM-CSF and INF and reduces inflammation better than miconazole, ketoconazole and fluconazole
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Faster Penetration and Reservoir effect

Highly Lipophyllic Benzothiophene matrix increases Dermal Penetration and retained even after 72 hrs of topical application.
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Pharmacokinetics
Absorption and bioavailability:
Highly lipophilic fragment. Topical sertaconazole has undetectable serum and urine levels, even on repeat administration

Distribution: High epidermal concentrations on topical application. Cutaneous absorption: 64% of the dose at 12 hours and 72% at 24 hours following topical 2% cream.

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Onset and duration of action in dermatophytosis

Initial action: 1 week

Adults : Superficial dermatophytic or candidal infections. Clinical cure 20% after one week.

Peak action: 2 to 4 weeks

Superficial mycoses (dermatophytosis, candidal infection) microbiological cure was 85% in 2 wk and 98 % in 4 wk.
Cure is seen in most patients after 4 weeks

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Indications and Dosage

Tinea and Candida Infections
Superficial fungal infections: Twice daily for 2 weeks Tinea Pedis: Twice daily for 4 weeks

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CLINICAL STUDIES

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Direct membrane-damaging effect of sertaconazole on Candida albicans as a mechanism of its fungicidal activity. Sertaconazole caused a dose-dependent decrease in intracellular ATP after only 10-min exposure and a concomitant significant increase in extracellular ATP. This behaviour is characteristic of antifungals which are fungicidal as a result of a direct membrane damage. Thus sertaconazole, in addition to the mechanism of action responsible for its fungistatic activity (inhibition of ergosterol synthesis), has a second mechanism of action providing a significant fungicidal activity due to direct cell membrane damage.
Arzneimittelforschung. 1992 May;42(5A):721-4. Sales Training

Anti-inflammatory and anti-itch activity of sertaconazole nitrate.

While butoconazole, ciclopirox olamine, fluconazole, and Miconazole nitrate were all found to have anti-inflammatory activity, only sertaconazole nitrate reduced the release of cytokines from activated lymphocytes and mitigated inflammation in animal models of irritant contact dermatitis and neurogenic inflammation. In addition, sertaconazole nitrate inhibited contact hypersensitivity and scratching responses in a murine model of pruritus.
Arch Dermatol Res. 2006 Sep;298(4):191-9. Epub 2006 Jul 26..

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Rate and extent of percutaneous absorption of sertaconazole nitrate after topical administration.

Its rapid appearance in the stratum corneum after application and the earlier finding that Sertaconazole nitrate is not distributed into blood in substantial quantities the pharmacokinetic properties of this antifungal preparation therapy can be regarded as favourable.

1.

Arzneimittelforschung. 2005;55(6):338-42.

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The safety and efficacy of sertaconazole nitrate

cream 2% for tinea pedis.

The stability of the mycologic cure rates through weeks 5 and 6 (2 weeks after cessation of therapy) indicate that sertaconazole protects against reinfection.

1.

Cutis. 2006 Oct; 78(4):268-74.

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