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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
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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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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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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
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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.
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Arzneimittelforschung. 2005;55(6):338-42.
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The stability of the mycologic cure rates through weeks 5 and 6 (2 weeks after cessation of therapy) indicate that sertaconazole protects against reinfection.
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