Terazol 3

Gynecological Antifungals

Terconazole is administered intravaginally as a cream or suppository.
Therapy with terconazole should be continued during menstruation.
If an adequate response is not achieved, the diagnosis should be reconfirmed by smears and/or cultures and other pathogens commonly associated with vulvovaginitis ruled out.

toxic epidermal necrolysis / Delayed / Incidence not known
anaphylactoid reactions / Rapid / Incidence not known
bronchospasm / Rapid / Incidence not known
teratogenesis / Delayed / Incidence not known

vaginal pain / Early / 4.2-4.2

headache / Early / 21.0-30.3
dysmenorrhea / Delayed / 6.0-6.0
abdominal pain / Early / 3.4-3.4
fever / Early / 1.0-2.8
chills / Rapid / 0.4-1.8
dizziness / Early / Incidence not known
vomiting / Early / Incidence not known
myalgia / Early / Incidence not known
arthralgia / Delayed / Incidence not known
rash / Early / Incidence not known
asthenia / Delayed / Incidence not known
nausea / Early / Incidence not known
malaise / Early / Incidence not known
urticaria / Rapid / Incidence not known
photosensitivity / Delayed / Incidence not known
vaginal irritation / Early / Incidence not known
pruritus / Rapid / Incidence not known

Terazol 3, Terazol 7, Zazole, Zazole Suppository

Rx

Intravaginal azole antifungal
Used for vaginal candidiasis; usually fungicidal against Candida albicans

1 applicatorful (20 mg terconazole/5 g cream) intravaginally at bedtime for 7 days in pregnant and non-pregnant patients.

1 applicatorful (20 mg terconazole/5 g cream) intravaginally at bedtime for 7 days in pregnant and non-pregnant patients.

1 applicatorful (40 mg terconazole/5 g cream) intravaginally at bedtime for 3 days in non-pregnant patients.

1 applicatorful (40 mg terconazole/5 g cream) intravaginally at bedtime for 3 days in non-pregnant patients.

1 suppository (80 mg terconazole) intravaginally at bedtime for 3 days in non-pregnant patients.

1 suppository (80 mg terconazole) intravaginally once daily at bedtime for 3 days in non-pregnant patients.

1 suppository (80 mg terconazole) or 1 applicatorful (20 mg terconazole/5 g cream) intravaginally at bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.

1 suppository (80 mg terconazole) or 1 applicatorful (20 mg terconazole/5 g cream) intravaginally at bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.

No dosage adjustment is needed.

No dosage adjustment is needed.

There are no drug interactions associated with Terconazole products.

Terazol 3/Terazol 7/Terconazole/Zazole Vaginal Cream: 0.4%, 0.8%
Terazol 3/Terconazole/Zazole Vaginal Supp: 80mg

1 applicatorful (20 or 40 mg terconazole/5 g cream) intravaginally/day; 1 suppository (80 mg terconazole) intravaginally/day.

1 applicatorful (20 or 40 mg terconazole/5 g cream) intravaginally/day; 1 suppository (80 mg terconazole) intravaginally/day.

Safety and efficacy have not been established; however, 1 applicatorful (20 or 40 mg terconazole/5 g cream) intravaginally/day and 1 suppository (80 mg terconazole) intravaginally/day have been used off-label.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Terconazole exerts its antifungal activity by disrupting normal fungal cell membrane permeability. Terconazole and other triazole antifungal agents (e.g., itraconazole, fluconazole) inhibit cytochrome P450 14-alpha-desmethylase in susceptible fungi, which leads to the accumulation of lanosterol and other methylated sterols and a decrease in ergosterol concentration. This mechanism of action is similar to that of the imidazole-derivative antifungal agents (e.g., butoconazole, clotrimazole, miconazole).

Terconazole is administered intravaginally. After intravaginal application, approximately 70% (range: 64% to 76%) of the dose remains in the vaginal area during the 16 hour suppository retention period. Once systemically absorbed, the drug is 94.9% bound to human plasma proteins and appears to be extensively metabolized (more than 95%). The mean elimination half-life of the parent drug ranges from 6.4 to 8.5 hours, with 3% to 10% eliminated in the urine and 2% to 6% eliminated in the feces.
 
Affected cytochrome P450 isoenzymes and drug transporters: none

Intravaginal Route
After intravaginal administration, absorption ranges from 5% to 16%, with the amount absorbed being proportional to the applied dose. The rate and extent of absorption are similar in women (pregnant or non-pregnant) with or without vulvovaginal candidiasis. Mean peak plasma terconazole concentrations (Cmax) are achieved 5 to 10 hours post-dose. Neither the Cmax nor overall drug exposure (AUC) are significantly increased after multiple daily applications (suppository, 3 days; cream, 7 days).

Because terconazole is absorbed from the human vagina and exposure to the fetus could occur through direct transfer of terconazole from the irritated vagina to the fetus by diffusion across amniotic membranes, avoid terconazole use during the first trimester of pregnancy unless essential to the health of the mother. Terconazole may be used during the second and third trimesters of pregnancy if the potential benefits outweigh the possible risks to the fetus. There was no evidence of teratogenicity when terconazole was administered to pregnant rats or rabbits at dosages of up to 100 times the recommended intravaginal human dose; however, there was some evidence of embryotoxicity in rats and rabbits at dosages that produced mean plasma concentrations which exceeded by 17 to 44 times the concentrations seen in healthy adults after intravaginal administration of terconazole.

It is not known if terconazole is excreted in human milk. Because of the potential for adverse effects in nursing infants, discontinue breast-feeding or discontinue terconazole, taking into account the importance of the drug to the mother. Fluconazole, clotrimazole, and miconazole may be potential alternatives to consider during breast-feeding. However, site of infection, local susceptibility patterns, and specific microbial susceptibility should be assessed before choosing an alternative agent.