ZAZOLE terconazole cream

国家: 美国

语言: 英文

来源: NLM (National Library of Medicine)

有效成分:

terconazole (UNII: 0KJ2VE664U) (terconazole - UNII:0KJ2VE664U)

可用日期:

Pharmaderm, A division of Nycomed US Inc.

INN（国际名称）:

terconazole

组成:

terconazole 8 mg in 1 g

处方类型:

PRESCRIPTION DRUG

授权状态:

New Drug Application

产品特点

ZAZOLE- TERCONAZOLE CREAM
PHARMADERM, A DIVISION OF NYCOMED US INC.
----------
ZAZOLE VAGINAL CREAM 0.8% (TERCONAZOLE VAGINAL CREAM 0.8%)
RX ONLY
DESCRIPTION
Zazole
Vaginal Cream 0.8% (terconazole vaginal cream 0.8%) is a white to
off-white, water washable
cream for intravaginal administration containing 0.8% 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, compounded in a cream base consisting of
butylated hydroxyanisole, cetyl
alcohol, isopropyl myristate, polysorbate 60, polysorbate 80,
propylene glycol, stearyl alcohol, and
purified water. 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 daily intravaginal administration of 0.8% terconazole 40 mg
(0.8% cream x 5 g) for seven
days to normal humans, plasma concentrations were low and gradually
rose to a daily peak (mean of 5.9
ng/mL or 0.006 mcg/mL) at 6.6 hours. Results from similar studies in
patients with vulvovaginal
candidiasis indicate that the slow rate of absorption, the lack of
accumulation, and the mean peak plasma
concentration of terconazole was not different from that observed in
healthy women. The absorption
characteristics of terconazole 0.8% in pregnant or non-pregnant
patients with vulvovaginal candidiasis
were also similar to those found in normal volunteers.
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