Zazole Vaginal 0.8%

Uses

Zazole Vaginal 0.8% Vaginal Cream and Vaginal Suppositories are used 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.

Zazole Vaginal 0.8% is also used to associated treatment for these conditions: Vulvovaginal Candidiasis

How Zazole Vaginal 0.8% works

Zazole Vaginal 0.8% may exert its antifungal activity by disrupting normal fungal cell membrane permeability. Zazole Vaginal 0.8% and other triazole antifungal agents inhibit cytochrome P450 14-alpha-demethylase in susceptible fungi, which leads to the accumulation of lanosterol and other methylated sterols and a decrease in ergosterol concentration. Depletion of ergosterol in the membrane disrupts the structure and function of the fungal cell leading to a decrease or inhibition of fungal growth.

Dosage

Zazole Vaginal 0.8% dosage

Zazole Vaginal 0.8% 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.

Zazole Vaginal 0.8% 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.

Zazole Vaginal 0.8% Vaginal Suppositories 80 mg: One Vaginal Suppository (80 mg terconazole) should be administered intravaginally once daily at bedtime for three consecutive days.

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.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.

Store at Controlled Room Temperature 15–30°C

Side Effects

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

Toxicity

The oral LD₅₀ values were found to be 1741 and 849 mg/kg for the male and female in rat.

Precaution

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.

Interaction

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.

Food Interaction

Elimination Route

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

Half Life

6.9 hours (range 4.0-11.3)

Elimination Route

Following oral (30 mg) administration of 14C-labelled terconazole, excretion of radioactivity was both by renal (32-56%) and fecal (47-52%) routes.

Pregnancy & Breastfeeding use

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.

Contraindication

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

Special Warning

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.

Acute Overdose

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.

Innovators Monograph

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