Terconazole is a triazole antifungal indicated for the intravaginal treatment of vulvovaginal candidiasis. Terconazole possesses fungicidal activity against Candida albicans and other Candida species. The hydrogenated vegetable oil base contained in the suppository formulation of terconazole may interact with certain rubber or latex products, such as latex condoms or vaginal contraceptive diaphragms; therefore, concurrent use of these contraceptive devices with the suppository formulation is not recommended. Headache and vulvovaginal burning or pruritis are among the most common adverse reactions reported with terconazole.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Intravaginal Administration
-Efficacy is unaffected by menstruation. However, avoid concurrent use with tampons as they may absorb the medication.
-To clean the applicator, pull the plunger out of the barrel. Wash the pieces with lukewarm, soapy water and dry thoroughly. Put the applicator back together by gently pushing the plunger into the barrel as far as it will go.
-If an adequate response is not achieved, reconfirm diagnosis with smears or cultures to rule out other pathogens commonly associated with vulvovaginitis.
Vaginal Cream
-Remove the cap from the tube and use the pointed tip on the cap to puncture the seal on the tube.
-Screw the applicator onto the tube.
-Squeeze the tube from the bottom and fill the applicator until the plunger stops.
-Unscrew the applicator from the tube.
-Hold the applicator by the ribbed end of the barrel and insert the filled applicator into the vagina as far as it will comfortably go.
-Slowly press the plunger of the applicator to release the cream into the vagina.
-Remove the applicator from the vagina.
Vaginal Suppository
-Break off the suppository from the plastic strip.
-Pull the plastic completely apart at the notched end.
-The terconazole suppository is self-lubricating and may be inserted with or without the applicator.
--To insert with the applicator, place the flat end of the suppository into the open end of the applicator. Hold the applicator by the ribbed end of the barrel and insert the filled applicator into the vagina as far as it will comfortably go. Press the plunger to release the suppository into the vagina. Remove the applicator from the vagina.
-To insert without the applicator, place the flat end of the suppository on the tip of finger and insert the suppository gently into the vagina as far as it will comfortably go.
During controlled clinical trials, headache was the most common adverse reaction reported in subjects treated with terconazole vaginal cream or suppositories. Headache occurred in 21% to 30.3% of subjects treated with terconazole and in 16% to 20.7% of subjects given placebo. Other systemic adverse events reported more frequently in subjects treated with terconazole than in those given placebo include generalized body pain (2.1% to 3.9% vs. 0% to 1.7%), fever (1% to 2.8% vs. 0.3% to 1.4%), and chills (0.4% to 1.8% vs. 0% to 0.7%). Additionally, dysmenorrhea and abdominal pain were reported with terconazole at a rate that was higher than placebo (6% vs. 2% and 3.4% vs. 1%, respectively). Adverse events reported during postmarketing use include asthenia, bronchospasm, dizziness, face edema, hypersensitivity, anaphylaxis or anaphylactoid reactions, influenza-like illness (with symptoms such as arthralgia, chills, fever, malaise, myalgia, nausea and vomiting), rash, toxic epidermal necrolysis, and urticaria. Discontinue use and avoid retreatment in any person who develops sensitization, irritation, fever, chills, or flu-like symptoms during treatment.
Photosensitivity reactions have been observed in volunteers after repeated dermal application of terconazole 0.8% and 2% creams under conditions of filtered artificial UV light. However, photosensitivity reactions have not been observed in subjects who were treated with terconazole suppositories or vaginal cream (0.4% or 0.8%) in clinical trials.
Vulvovaginal burning, vulvovaginal pruritus, and vaginal irritation have been reported with terconazole. Subjects treated with terconazole vaginal suppositories experienced more vulvovaginal burning and vaginal pain than subjects receiving placebo (15.2% vs. 11.2% and 4.2% vs. 0.7%, respectively) in controlled clinical trials. Vulvovaginal burning or pruritus was the adverse reaction most frequently associated with discontinuation of therapy. Discontinue terconazole and avoid retreatment in any person who develops sensitization or irritation while receiving terconazole.
Terconazole is contraindicated in patients with a history of hypersensitivity to terconazole or any component of the formulations. Hypersensitivity reactions, including anaphylaxis and toxic epidermal necrolysis, have been reported during treatment with terconazole. Instruct patients to discontinue use and seek immediate medical attention if anaphylaxis or toxic epidermal necrolysis develops.
The hydrogenated vegetable oil base contained in the suppository formulation of terconazole may interact with certain rubber or latex products, such as latex condoms or vaginal contraceptive diaphragms; therefore, concurrent use of these contraceptive devices with the suppository formulation is not recommended. Although terconazole may be used during menstruation, advise against concurrent tampon use as tampons may absorb the medication; recommend use of external pads or napkins during terconazole therapy.
Terconazole is for vulvovaginal use only. Terconazole is not for oral or ophthalmic administration. Avoid accidental ocular exposure. If ocular exposure to terconazole cream occurs, wash with clean water or saline and advise persons to seek medical attention if eye irritation persists. Supportive/symptomatic measures are advised in the event of oral ingestion of terconazole suppository or cream.
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. 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. There was no evidence of teratogenicity when terconazole was administered orally or subcutaneously 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 mean peak plasma concentrations observed 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.
Per the manufacturer, this drug has been shown to be active against most strains of the following microorganisms either in vitro and/or in clinical infections: Candida albicans, Candida sp.
NOTE: The safety and effectiveness in treating clinical infections due to organisms with in vitro data only have not been established in adequate and well-controlled clinical trials.
For the treatment of vulvovaginal candidiasis (VVC):
-for the treatment of uncomplicated VVC:
Intravaginal dosage (0.4% vaginal cream):
Adults: 5 g (20 mg terconazole) intravaginally once daily at bedtime for 7 days in pregnant and non-pregnant persons.
Adolescents*: 5 g (20 mg terconazole) intravaginally once daily at bedtime for 7 days in pregnant and non-pregnant persons.
Intravaginal dosage (0.8% vaginal cream):
Adults: 5 g (40 mg terconazole) intravaginally once daily at bedtime for 3 days in non-pregnant persons.
Adolescents*: 5 g (40 mg terconazole) intravaginally once daily at bedtime for 3 days in non-pregnant persons.
Intravaginal dosage (vaginal suppository):
Adults: 80 mg intravaginally once daily at bedtime for 3 days in non-pregnant persons.
Adolescents*: 80 mg intravaginally once daily at bedtime for 3 days in non-pregnant persons.
-for the treatment of severe or recurrent VVC*:
Intravaginal dosage (0.4% vaginal cream):
Adults: 5 g (20 mg terconazole) intravaginally once daily at bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.
Adolescents: 5 g (20 mg terconazole) intravaginally once daily at bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.
Intravaginal dosage (vaginal suppository):
Adults: 80 mg intravaginally once daily at bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.
Adolescents: 80 mg intravaginally once daily at bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.
Maximum Dosage Limits:
-Adults
40 mg/day intravaginally for cream; 80 mg/day intravaginally for suppository.
-Geriatric
40 mg/day intravaginally for cream; 80 mg/day intravaginally for suppository.
-Adolescents
Safety and efficacy have not been established; however, 40 mg/day intravaginally for cream or 80 mg/day intravaginally for suppository has been used off-label.
-Children
Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
There are no drug interactions associated with Terconazole products.
Terconazole is a triazole antifungal that works by inhibiting the biosynthesis of ergosterol, an essential component of fungal cell membrane. Azole antifungals block ergosterol synthesis by inhibiting lanosterol 14-alpha demethylase, a cytochrome P450 dependent enzyme, which is needed to convert lanosterol to ergosterol. The depletion of ergosterol within the fungal cell membrane results in increased cellular permeability causing leakage of cellular content.
Terconazole displays fungicidal activity against Candida albicans and other Candida species.
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
-Route-Specific Pharmacokinetics
Other Route(s)
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 subjects (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).