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Terconazole

Generic name: terconazole topical

Brand names: Terazol, Zazole, Terazol 3, Terazol 7, Terazole 3

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Cream, Vaginal:

Terazol 7: 0.4% (45 g [DSC]) [contains cetyl alcohol, polysorbate 80, propylene glycol]

Terazol 3: 0.8% (20 g [DSC]) [contains cetyl alcohol, polysorbate 80, propylene glycol]

Zazole: 0.8% (20 g [DSC])

Generic: 0.4% (45 g); 0.8% (20 g)

Suppository, Vaginal:

Zazole: 80 mg (3 ea [DSC])

Generic: 80 mg (1 ea, 3 ea)

Pharmacology

Mechanism of Action

Terconazole is a triazole ketal antifungal agent; involves inhibition of fungal cytochrome P450. Specifically, terconazole inhibits cytochrome P450-dependent 14-alpha-demethylase which results in accumulation of membrane disturbing 14-alpha-demethylsterols and ergosterol depletion.

Pharmacokinetics/Pharmacodynamics

Absorption

Suppository: ~70% remains in vaginal area; ~10% is absorbed systemically

Excretion

Suppository: Urine (3% to 10%); feces (2% to 6%)

Time to Peak

~5 to 10 hours

Half-Life Elimination

6.4 to 8.5 hours

Protein Binding

94.9%

Use in Specific Populations

Special Populations: Gender

Following terconazole administration, absorption varies in hysterectomized subjects (5% to 8% absorption) vs nonhysterectomized subjects (12% to 16% absorption). Other than this, overall absorption is similar in all women.

Use: Labeled Indications

Candidiasis, vulvovaginal: For the local treatment of vulvovaginal candidiasis (moniliasis). As terconazole is effective only for vulvovaginitis caused by the genus Candida, the diagnosis should be confirmed by KOH smears or cultures.

Contraindications

Hypersensitivity to terconazole or any component of the formulation

Documentation of allergenic cross-reactivity for imidazole antifungals is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Dosage and Administration

Dosing: Adult

Candidiasis, vulvovaginal: Intravaginal:

Vaginal cream 0.4%: Insert 1 applicatorful intravaginally at bedtime for 7 consecutive days.

Vaginal cream 0.8%: Insert 1 applicatorful intravaginally at bedtime for 3 consecutive days.

Vaginal suppository: Insert 1 suppository intravaginally at bedtime for 3 consecutive days.

Dosing: Geriatric

Refer to adult dosing.

Administration

Intravaginal:

Vaginal cream: Use applicator provided by manufacturer. Insertion should be as far as possible into the vagina without causing discomfort. Wash applicator after each use; allow to dry thoroughly before putting back together.

Vaginal suppository: Remove foil package prior to use. Insertion should be as far as possible into the vagina without causing discomfort. If the provided applicator is used for insertion, wash and dry thoroughly prior to additional use.

Storage

Store at 15°C to 30°C (59°F to 86°F).

Drug Interactions

Progesterone: Antifungal Agents (Vaginal) may diminish the therapeutic effect of Progesterone. Avoid combination

Adverse Reactions

>10%: Central nervous system: Headache

1% to 10%:

Central nervous system: Chills, pain

Gastrointestinal: Abdominal pain

Genitourinary: Dysmenorrhea, vaginal discomfort (burning, irritation, or itching)

Miscellaneous: Fever

<1%, postmarketing, and/or case reports: Anaphylaxis, asthenia, bronchospasm, burning sensation of the penis, dizziness, facial edema, flu-like symptoms (including nausea, vomiting, myalgia, arthralgia, malaise), hypersensitivity, skin rash, toxic epidermal necrolysis, urticaria

Warnings/Precautions

Concerns related to adverse effects:

  • Dermatologic toxicity: If toxic epidermal necrolysis (TEN) occurs, discontinue therapy; implement supportive care/monitoring. Do not reinstitute therapy.
  • Hypersensitivity/anaphylaxis: If anaphylaxis occurs, discontinue therapy; implement supportive care/monitoring. Do not reinstitute therapy.
  • Idiosyncratic reactions: If fever, chills, or flu-like symptoms occur, discontinue therapy. Do not reinstitute therapy.
  • Irritation: If irritation or sensitization occurs, discontinue use. Do not reinstitute therapy.

Dosage form specific issues:

  • Vaginal suppository: The base in the suppository formulation may weaken latex or rubber (condoms or diaphragms); concurrent use is not recommended.

Other warnings/precautions:

  • Lack of response: Microbiological studies (KOH smear and/or cultures) should be repeated in patients not responding to terconazole in order to confirm the diagnosis and rule out other pathogens.

Pregnancy

Pregnancy Considerations

The rate and extent of absorption are similar in pregnant and nonpregnant patients with vulvovaginal candidiasis. Although the manufacturer recommends that use should be avoided during the first trimester of pregnancy (due to systemic absorption) and that use may be considered in the second or third trimesters if the benefits outweigh risks to the fetus, guidelines state that 7-day topical azole vaginal products are the preferred treatment of vulvovaginal candidiasis in pregnant women (CDC [Workowski 2015]. This product may weaken latex condoms and diaphragms (CDC [Workowski 2015]).

Patient Education

What is this drug used for?

  • It is used to treat vaginal infections.
  • It may be given to you for other reasons. Talk with the doctor.

Frequently reported side effects of this drug

  • Headache
  • Menstrual pain

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

  • Severe vaginal irritation
  • Chills
  • Flu-like signs
  • Stevens-Johnson syndrome/toxic epidermal necrolysis like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in mouth, throat, nose, or eyes
  • Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Source: Wolters Kluwer Health. Last updated February 6, 2020.