ZAZOLE terconazole cream

Summary of Product characteristics

                                ZAZOLE- TERCONAZOLE CREAM
PHARMADERM A DIVISION OF FOUGERA PHARMACEUTICALS INC.
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ZAZOLE VAGINAL CREAM 0.4%
(TERCONAZOLE VAGINAL CREAM 0.4%)
RX ONLY
DESCRIPTION
Zazole
Vaginal Cream 0.4% (terconazole vaginal cream 0.4%) is a white to
off-white, water washable
cream for intravaginal administration containing 0.4% 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 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
                                
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