Terconazole

Terconazole is an anti-fungal cream and suppository used for treating vaginal yeast infections (Candida). It is related to several other anti-fungal drugs including fluconazole (Diflucan), ketoconazole (Nizoral), itraconazole (Sporanox), miconazole (Micatin, Monistat), and clotrimazole (Lotrimin). It prevents growth of yeast by preventing production of the membranes that surround the yeast cells. The FDA approved terconazole in December 1987.

Absorption

Small amounts of terconazole (about 5–16% of a dose) are slowly absorbed systemically following intravaginal administration.1 3 14 The amount of drug absorbed is proportional to the dose (regardless of dosage form)3 14 and absorption is similar in women with or without vulvovaginal candidiasis.3

Distribution

Extent

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

Not known whether terconazole crosses the placenta43 or is distributed into milk.1

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.1 3

Elimination Route

Following oral administration, 32–56% of the dose excreted in urine and 47–52% excreted in feces1 within 24 hours.43

Half-life

Following oral administration, half-life is 6.9 hours.1

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

Store at 20-25°C (68-77°F) [see USP Controlled Room Temperature].

Manufactured By Perrigo

Bronx, NY 10457

Distributed By

Perrigo®

Allegan, MI 49010 • www.perrigo.com

Rev 01-17

:2X300 RC J6

Rx Only

Terconazole Vaginal Suppositories, 80 mg

3 SUPPOSITORIES with vaginal applicator

• Terazol 3 [DSC]
• Terazol 7
• Zazole [DSC]

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.

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%

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.

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

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.