Terconazole (Monograph)

Brand name: Terazol
Drug class: Azoles
VA class: GU300
Chemical name: cis-1-[4-[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-4-(1-methylethyl)piperazine
Molecular formula: C₂₆H₃₁Cl₂N₅O₃
CAS number: 67915-31-5

Medically reviewed by Drugs.com on Jun 21, 2024. Written by ASHP.

Introduction

Antifungal; azole (triazole derivative).

Uses for Terconazole

Vulvovaginal Candidiasis

Treatment of uncomplicated vulvovaginal candidiasis (mild to moderate, sporadic or infrequent, most likely caused by Candida albicans, occurring in immunocompetent women). A drug of choice.

Treatment of complicated vulvovaginal candidiasis, including infections that are recurrent (≥4 episodes in 1 year), severe (extensive vulvar erythema, edema, excoriation, fissure formation), caused by Candida other than C. albicans, or occurring in women with underlying medical conditions (uncontrolled diabetes mellitus, HIV infection, immunosuppressive therapy, pregnancy). Complicated infections generally require more prolonged treatment than uncomplicated infections.

Optimal regimens for treatment of vulvovaginal candidiasis caused by Candida other than C. albicans (e.g., C. glabrata, C. krusei) not identified. CDC and others state these infections may respond to an intravaginal azole antifungal given for 7–14 days or to a 14-day regimen of intravaginal boric acid (not commercially available in the US).

Terconazole Dosage and Administration

Administration

Intravaginal Topical Administration

Administer intravaginally as a cream or suppository.

Interruption or discontinuance of terconazole therapy during a prescribed regimen, even during menstruation or in response to symptomatic relief, is not advised.

Dosage

Adults

Uncomplicated Vulvovaginal Candidiasis

Intravaginal

Cream: one applicatorful of 0.4% cream once daily at bedtime for 7 consecutive days or one applicatorful of 0.8% cream once daily at bedtime for 3 consecutive days.

Suppository: one 80-mg vaginal suppository once daily at bedtime for 3 consecutive days.

Complicated Vulvovaginal Candidiasis

Recurrent Vulvovaginal Infections Caused by Candida albicans

Intravaginal

CDC and others recommend an initial intensive regimen (7–14 days of an intravaginal azole or 3-dose regimen of oral fluconazole) to achieve mycologic remission, followed by an appropriate maintenance regimen (6-month regimen of once-weekly oral fluconazole or, alternatively, an intravaginal azole given intermittently).

Other Complicated Vulvovaginal Infections

Intravaginal

CDC and others recommend 7–14 days of an intravaginal azole for vulvovaginal candidiasis that is severe, caused by Candida other than C. albicans, or occurring in women with underlying medical conditions.

HIV-infected patients: Use same regimen recommended for other patients. Some experts recommend a duration of 3–7 days. Maintenance regimen of an intravaginal azole can be considered for those with recurrent episodes; routine primary or secondary prophylaxis (long-term suppressive or chronic maintenance therapy) not recommended.

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.

Renal Impairment

No specific dosage recommendations at this time.

Geriatric Patients

No specific dosage recommendations at this time.

Cautions for Terconazole

Contraindications

• Known hypersensitivity to terconazole or any ingredient in the formulation.

Warnings/Precautions

Sensitivity Reactions

Allergic Reactions

Possible flu-like syndrome, characterized by fever, chills, headache, and/or hypotension and occasionally by vertigo and nausea. May be immunoallergenic or may be a reaction to the dying fungi (similar to the Jarisch-Herxheimer reaction observed during penicillin therapy for syphilis).

If irritation, sensitization, fever, chills, or flu-like symptoms occur and appear to be drug related, discontinue and do not reinstitute terconazole therapy.

Photosensitivity Reactions

Photosensitivity reactions reported following repeated topical application to the skin of 0.8 or 2% terconazole cream and exposure to filtered artificial ultraviolet light; not reported to date following intravaginal administration of 0.4 or 0.8% cream or 80-mg suppositories.

General Precautions

Use of Latex/Rubber Contraceptive Diaphragms

Hydrogenated vegetable oil base contained in terconazole vaginal suppositories may interact with certain rubber or latex products such as vaginal contraceptive diaphragms; concurrent use not recommended. Consider use of terconazole vaginal cream as an alternative to the suppositories.

Selection and Use of Antifungals for Vulvovaginal Candidiasis

Prior to initial use of terconazole in a woman with signs and symptoms of vulvovaginal candidiasis, confirm the diagnosis by demonstrating yeast or pseudohyphae with direct microscopic examination of vaginal discharge (saline or 10% potassium hydroxide [KOH] wet mount or Gram stain) or by culture.

Candida identified by culture in the absence of symptoms is not an indication for antifungal treatment since approximately 10–20% of women harbor Candida or other yeasts in the vagina.

If clinical symptoms persist, tests should be repeated to rule out other pathogens and to confirm the original diagnosis.

Specific Populations

Pregnancy

Category C.

Because terconazole is absorbed systemically following intravaginal administration, manufacturer states the drug should not be used during the first trimester of pregnancy unless the clinician considers it essential to the welfare of the patient. CDC and others state that a 7-day regimen of an intravaginal azole antifungal can be used, if necessary, for treatment of vulvovaginal candidiasis in pregnant women.

Lactation

Distributed into milk in rats; not known whether distributed into human milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established in children <18 years of age.

Geriatric Use

Insufficient experience from clinical studies to determine whether patients ≥65 years of age respond differently than younger adults. Other clinical experience has not identified age-related differences in response.

Common Adverse Effects

Headache, vulvovaginal itching/burning or pain, dysmenorrhea, abdominal pain.

Drug Interactions

Oral Contraceptives

Terconazole efficacy not affected by concomitant oral contraceptives; terconazole has no effect on estradiol or progesterone concentrations in women receiving low-dose oral contraceptives.

Terconazole Pharmacokinetics

Absorption

Small amounts of terconazole (about 5–16% of a dose) are slowly absorbed systemically following intravaginal administration. The amount of drug absorbed is proportional to the dose (regardless of dosage form) and absorption is similar in women with or without vulvovaginal candidiasis.

Distribution

Extent

Distribution into body tissues and fluids following intravaginal administration has not been determined.

Not known whether terconazole crosses the placenta or is distributed into milk.

Elimination

Metabolism

The metabolic fate of terconazole following intravaginal administration has not been fully characterized, but systemically absorbed drug appears to be rapidly and extensively metabolized.

Elimination Route

Following oral administration, 32–56% of the dose excreted in urine and 47–52% excreted in feces within 24 hours.

Half-life

Following oral administration, half-life is 6.9 hours.

Stability

Storage

Cream

15–30°C.

Suppository

15–30°C.

Actions

• Triazole-derivative azole antifungal.

• Usually fungicidal in action.

• Presumably exerts its antifungal activity by altering cellular membranes resulting in increased membrane permeability, leakage of essential elements (e.g., amino acids, potassium), and impaired uptake of precursor molecules (e.g., purine and pyrimidine precursors to DNA). Inhibits cytochrome P-450 14-α-desmethylase in susceptible fungi, which leads to accumulation of C-14 methylated sterols (e.g., lanosterol) and decreased concentrations of ergosterol.

• Spectrum of antifungal activity includes many fungi, including yeasts and dermatophytes. At high concentrations, has some in vitro activity against gram-positive and -negative bacteria.

• Candida: Active in vitro and in vivo against C. albicans, C. krusei, C. parapsilosis, C. pseudotropicalis, C. stellatoidea, and C. tropicalis.

• Dermatophytes and other fungi: Active in vitro against Trichophyton mentagrophytes, T. rubrum, T. tonsurans, T. verrucosum, and Epidermophyton floccosum. Also active against Cryptococcus neoformans.

• Cross resistance can occur among the azole antifungals (e.g., clotrimazole, ketoconazole, miconazole). Azole-resistant Candida have been reported.

• Importance of reading and understanding manufacturer’s patient instructions regarding use of applicator for intravaginal administration.

• Importance of not interrupting or discontinuing the drug and completing full course of therapy, even during menstruation or in response to symptomatic relief.

• Importance of informing clinicians if irritation, sensitization, fever, chills, or flu-like symptoms occur.

• Importance of women following clinician's advice regarding sexual intercourse and informing partner to seek medical advice if penile itching, redness, or discomfort occurs.

• Importance of not using rubber or latex products such as vaginal contraceptive diaphragms when using terconazole vaginal suppositories; use of terconazole vaginal cream should be considered as an alternative.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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