Терконазол

Описание

Terconazole is an antifungal agent somewhat more potent than clotrimazole and useful in the topical treatment of vaginal dermatophytosis and candidiasis.

Химические свойства

White or almost white powder.

Использование

Terconazole belongs to a new chemical class of antifungal agents, the triazoles. Terconazole has a far greater selectively for yeast cytochrome P-450 than for mammalian microsomal cytochrome P-450 and is used as topical treatment of mycotic vaginitis. Terconazole may also be used in vitro as a potent antifungal agent to prevent the morphogenetic transformation of yeast into (pseudo-)mycelium form of Candida albicans.

Показания

Terconazole (Terazol) is a fungicidal triazole topical preparation effective against many Candida strains. It is used as either a 3-day or a 7-day course (Terazol 7—0.4% cream for 7 days or Terazol 3—0.8% cream for 3 days).

Всемирная организация здравоохранения(ВОЗ)

Terconazole, an antifungal agent, was introduced into medicine in 1980. It is indicated for the treatment of vaginal candidiasis. It is not yet clear whether the adverse effects associated with high dose formulations are due to terconazole itself, to an excipient in the preparation or to fungal constituent.

Механизм действия

Terconazole is effective for fungistatic action for many strains of Candida and dermatophytes. The exact mechanism of its action is unknown, although it inhibits the action of the enzyme lanosterol 1-demethylase of cytochrome P-450 of sensitive fungi (similar to other azols described above), causing a reduction in the amount of ergosterin, which is necessary for the organisms to construct membranes and to retain the appropriate permeability. It is only used externally for treating vulvovaginal candidoses. Synonyms of this drug are terazol, tercospor, and others.

Клиническое использование

cis-1-[4-[[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy]phenyl]-4-(1methylethyl)piperazine (Terazol), or terconazole, is a triazolederivative that is used exclusively for the control ofvulvovaginal moniliasis caused by C. albicans and otherCandida species. It is available in creams containing 0.4%and 0.8% of the free base intended for 7-day and 3-day treatmentperiods, respectively. Suppositories containing 80 mgof the free base are also available.