Zazole Vaginal Cream

Generic name:terconazole
Dosage form: vaginal cream
Drug class:Vaginal anti-infectives

Medically reviewed by Drugs.com. Last updated on May 23, 2022.

Rx only

Zazole Vaginal Cream 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.

Zazole Vaginal Cream - 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 14C-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 dru...