Terconazole

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

Terconazole disrupts ergosterol synthesis by binding to fungal cytochrome P450. It is active in vitro against Candida spp. and other fungi. It has some antibacterial activity in vitro but not against usual vag flora e.g, lactobacilli.

Terconazole Vaginal Cream 0.4%: One full applicator (5 g) of 7 Vaginal Cream (20 mg terconazole) should be administered intravaginally once daily at bedtime for seven consecutive days.

Terconazole Vaginal Cream 0.8%: One full applicator (5 g) of Vaginal Cream (40 mg terconazole) should be administered intravaginally once daily at bedtime for three consecutive days.

Terconazole Vaginal Suppositories 80 mg: One Vaginal Suppository (80 mg terconazole) should be administered intravaginally once daily at bedtime for three 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 these products is not affected by menstruation.

May decrease absorption of ciprofloxacin, ciclosporin, mycophenolate, tacrolimus and levothyroxine. Sevelamer should be given 3 hr before or 1 hr after taking other drugs to minimise potential pharmacokinetic interaction.

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

Vulvovaginal burning, vulvar itching, dysmenorrhoea, genital, body and abdominal pain. Flu-like syndrome with headache, fever, chills and hypotension with doses >80 mg.

Pregnancy Category C. There was no evidence of teratogenicity when terconazole was administered orally up to 40 mg/kg/day (25x the recommended intravaginal human dose of the suppository formulation, 50x the recommended intravaginal human dose of the 0.8% vaginal cream formulation, and 100x the intravaginal human dose of the 0.4% vaginal cream formulation) in rats, or 20 mg/kg/day in rabbits, or subcutaneously up to 20 mg/kg/day in rats.

Nursing Mothers: It is not known whether this drug is excreted in human milk. Animal studies have shown that rat offspring 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.

Discontinue use and do not retreat with terconazole if sensitization, irritation, fever, chills or flu-like symptoms are reported during use. The base contained in the suppository formulation may interact with certain rubber or latex products, such as those used in vaginal contraceptive diaphragms; therefore concurrent use is not recommended.

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.

Drugs used in Vaginal and Vulval condition.

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

Geriatric Use: Clinical studies of terconazole did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

Store at Controlled Room Temperature 15–30°C