TERAZOL 7 Vaginal Cream 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-(1H-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, 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.

Microbiology:   Terconazole exhibits fungicidal activity in vitro against Candida albicans. Antifungal activity also has been demonstrated against other fungi. The MIC values for terconazole against most species of lactic acid bacteria typically found in the human vagina were >/=128 mcg/mL, therefore these beneficial bacteria are not affected by drug treatment.

The exact pharmacologic mode of action of terconazole is uncertain; however, it may exert its antifungal activity by the disruption of normal fungal cell membrane permeability. No resistance to terconazole has developed during successive passages of C. albicans.

Human 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 14 C-labelled terconazole, the 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 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 0.4% vaginal cream.

TERAZOL 7 Vaginal Cream is indicated for the local treatment of vulvovaginal candidiasis (moniliasis). As TERAZOL 7 Vaginal Cream is effective only for vulvovaginitis caused by the genus Candida, the diagnosis should be confirmed by KOH smears and/or cultures.


Patients known to be hypersensitive to terconazole or to any of the components of the cream.



General:   Discontinue use and do not retreat with terconazole if sensitization, irritation, fever, chills or flu-like symptoms are reported during use. If there is lack of response to TERAZOL 7 Vaginal Cream, appropriate microbiological studies (standard KOH smear and/or cultures) should be repeated to confirm the diagnosis and rule out other pathogens.

Drug Interactions:   The therapeutic effect of TERAZOL 7 Vaginal Cream is not affected by oral contraceptive usage.

Carcinogenesis, Mutagenesis, Impairment of Fertility:

Carcinogenesis:   Studies to determine the carcinogenic potential of terconazole have not been performed.

Mutagenicity:   Terconazole was not mutagenic when tested in vitro for induction of microbial point mutations (Ames test) or for inducing cellular transformation, or in vivo for chromosome breaks (micronucleus test) or dominant lethal mutations in mouse germ cells.

Impairment of Fertility: No impairment of fertility occurred when female rats were administered terconazole orally up to 40 mg/kg/day.

Pregnancy:   Pregnancy Category C.

There was no evidence of teratogenicity when terconazole was administered orally up to 40 mg/kg/day (100 × the recommended intravaginal human dose) in rats, or 20 mg/kg/day in rabbits, or subcutaneously in rats up to 20 mg/kg/day.

Dosages at or below 10 mg/kg/day produced no embryotoxicity; however, there was a delay in fetal ossification at 10 mg/kg/day in rats. There was some evidence of embryotoxicity in rabbits and rats at 20-40 mg/kg. In rats this was reflected as a decrease in litter size and number of viable young and reduced fetal weight. There was also delay in ossification and an increased incidence of skeletal variants.

The no-effect oral dose of 10 mg/kg/day resulted in a mean peak plasma level of terconazole in pregnant rats of 0.176 mcg/mL which exceeds by 44 times the mean peak plasma levels (0.004 mcg/mL) seen in normal subjects after intravaginal administration of terconazole. This safety assessment does not account for possible exposure of the fetus through direct transfer of terconazole from the irritated vagina to the fetus by diffusion across amniotic membranes.

Since terconazole is absorbed from the human vagina, it should not be used in the first trimester of pregnancy unless the physician considers it essential to the welfare of the patient.

Nursing Mothers:   It is not known whether this drug is excreted in human milk. Animal studies have shown that rat off-spring exposed via the milk of treated (40 mg/kg/orally) dams showed decreased survival during the first few post-partum days, but overall pup weight and weight gain were comparable to or greater than controls throughout lactation. Because many drugs are excreted in human milk, and because of the potential for adverse reaction in nursing infants from terconazole, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use:   Safety and efficacy in children have not been established.


During controlled clinical studies conducted in the United States, 521 patients with vulvovaginal candidiasis were treated with terconazole 0.4% vaginal cream. Based on comparative analyses with placebo, the adverse experiences considered most likely related to terconazole 0.4% vaginal cream were headaches (26% vs 17% with placebo) and body pain (2.1% vs 0% with placebo). Vulvovaginal burning (5.2%), itching (2.3%) or irritation (3.1%) occurred less frequently with terconazole 0.4% vaginal cream than with the vehicle placebo. Fever (1.7% vs 0.5% with placebo) and chills (0.4% vs 0.0% with placebo) have also been reported. The therapy-related dropout rate was 1.9%. The adverse drug experience on terconazole most frequently causing discontinuation was vulvovaginal itching (0.6%), which was lower than the incidence for placebo (0.9%).


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 [cong ]1280 and >/=640 mg/kg, respectively.


One full applicator (5 g) of TERAZOL 7 Vaginal Cream (20 mg terconazole) is administered intravaginally once daily at bedtime for seven consecutive days. Before prescribing another course of therapy, the diagnosis should be reconfirmed by smears and/or cultures and other pathogens commonly associated with vulvovaginitis ruled out. The therapeutic effect of TERAZOL 7 Vaginal Cream is not affected by menstruation.


TERAZOL® 7 (terconazole) Vaginal Cream 0.4% is available in 45 g (NDC 0062-5350-01) tubes with an ORTHO® Measured-Dose Applicator. Store at controlled room temperature 15°-30°C (59°-86°F).

Caution: Federal (USA) law prohibits dispensing without a prescription.

631-11-301-6                          Revised September 1996


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The product samples shown here have been supplied by the manufacturer and reproduced in full color by PDR as a quick-reference identification aid. While every effort has been made to assure accurate reproduction, please remember that any visual identification should be considered preliminary. In cases of poisoning or suspected overdosage, the drug' identity should be verified by chemical analysis.