Mechanism_of_action Sertaconazole







sertaconazole has several known mechanisms of action. considered fungistatic, fungicidal, antibacterial, antiinflammatory, antitrichomonal, , antipruritic.


like other imidazole antifungals, sertaconazole blocks synthesis of ergosterol inhibiting 14α-demethylase enzyme. ergosterol critical component of fungal cell membrane. inhibition of ergosterol synthesis prevents fungal cells multiplying , impairs hyphae growth.


chemically, sertaconazole contains benzothiophene ring makes unique other imidazole antifungals. benzothiophene ring sulfur analogue of indole ring found in amino acid tryptophan. tryptophan found in fungal membrane in addition lipids such ergosterol. benzothiophene ring in sertaconazole mimics tryptophan , increases drugs ability form pores in fungal cell membrane. if cell membrane made sufficiently leaky these pores fungal cell die loss of atp , other effects can include calcium disregulation. these pores believed open @ 10 minutes following topical application of sertaconazole. 1 hour following topical application, approximately 90% of fungal cells die lack of energy (due atp loss) , general loss of homeostasis. sertaconazole thought imidazole antifungal mechanism of action.


sertaconazole has antiinflammatory , antipruritic action. inhibits release of proinflammatory cytokines activated immune cells. has been shown sertaconazole activatates of p38/cox2/pge2 pathway. pge2 can have variety of important effects in body including activation of body s fever response.


sertaconazole has antibacterial action. hypothesized mechanism of action again involves sertaconazole s ability form pores mimicking tryptophan.


it has been shown sertaconazole can kill trichomonas vaginalis in vitro. exact mechanism of action yet unknown.


sertaconazole appears inhibit dimorphic transformation of candida albicans pathogenic fungi.







Comments