ZAZOLE terconazole cream

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Pharmaderm, A division of Nycomed US Inc.

INN (International Name):

terconazole

Composition:

terconazole 8 mg in 1 g

Prescription type:

PRESCRIPTION DRUG

Authorization status:

New Drug Application

Summary of Product characteristics

ZAZOLE- TERCONAZOLE CREAM
PHARMADERM, A DIVISION OF NYCOMED US INC.
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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