Country: Ամերիկայի Միացյալ Նահանգներ
language: անգլերեն
source: NLM (National Library of Medicine)
TERCONAZOLE (UNII: 0KJ2VE664U) (TERCONAZOLE - UNII:0KJ2VE664U)
PharmaDerm a division of Fougera Pharmaceuticals Inc.
TERCONAZOLE
TERCONAZOLE 80 mg
PRESCRIPTION DRUG
Abbreviated New Drug Application
ZAZOLE- TERCONAZOLE SUPPOSITORY PHARMADERM A DIVISION OF FOUGERA PHARMACEUTICALS INC. ---------- ZAZOLE VAGINAL SUPPOSITORIES (TERCONAZOLE VAGINAL SUPPOSITORIES, 80 MG) DESCRIPTION: Zazole Vaginal Suppositories (terconazole vaginal suppositories, 80 mg) are white to off-white suppositories for intravaginal administration containing 80 mg of the antifungal agent terconazole, _cis_-1- [_p_-[[2-(2,4-Dichlorophenyl)-2-(1_H_-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-4- isopropylpiperazine, in triglycerides derived from coconut and/or palm kernel oil (a base of hydrogenated vegetable oils) and butylated hydroxyanisole. The structural formula of terconazole is as follows: Terconazole, a triazole derivative, is a white to almost white powder with a molecular weight of 532.47. It is insoluble in water; sparingly soluble in ethanol; and soluble in butanol. CLINICAL PHARMACOLOGY Following intravaginal administration of terconazole in humans, absorption ranged from 5-8% in three hysterectomized subjects and 12-16% in two non-hysterectomized subjects with tubal ligations. Following oral (30 mg) administration of C-labelled terconazole, the harmonic half-life of elimination from the blood for the parent terconazole was 6.9 hours (range 4.0-11.3). Terconazole is extensively metabolized; the plasma AUC for terconazole compared to the AUC for total radioactivity was 0.6%. Total radioactivity was eliminated from the blood with a harmonic half-life of 52.2 hours (range 44- 60). Excretion of radioactivity was both by renal (32-56%) and fecal (47-52%) routes. _In vitro_, terconazole is highly protein bound (94.9%) and the degree of binding is independent of drug concentration. Photosensitivity reactions were observed in some normal volunteers following repeated dermal application of terconazole 2.0% and 0.8% creams under conditions of filtered artificial ultraviolet light. Photosensitivity reactions have not been observed in U.S. and foreign clinical trials in patients who were treated with Zazole Vaginal Suppositor read_full_document