ZAZOLE terconazole suppository

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 Fougera Pharmaceuticals Inc.

INN (International Name):

TERCONAZOLE

Composition:

TERCONAZOLE 80 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ZAZOLE- TERCONAZOLE SUPPOSITORY
PHARMADERM A DIVISION OF FOUGERA PHARMACEUTICALS INC.
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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