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 () , -1-[-[[2-(2,4-Dichlorophenyl)-2-(1-1,2,4-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.
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 () , -1-[-[[2-(2,4-Dichlorophenyl)-2-(1-1,2,4-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.
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 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.
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 Terconazole () suppositories or vaginal cream (0.4% and 0.8%).
Terconazole () Vaginal Cream is indicated for the local treatment of vulvovaginal candidiasis (moniliasis). As this product is effective only for vulvovaginitis caused by the genus Candida, the diagnosis should be confirmed by KOH smears and/or cultures.
Overdose of Terconazole () in humans has not been reported to date. In the rat, the oral LD 50 values were found to be 1741 and 849 mg/kg for the male and female, respectively. The oral LD 50 values for the male and female dog were ≅1280 and ≥640 mg/kg, respectively.
