TRIVAGIZOLE 3
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRIVAGIZOLE 3 (TRIVAGIZOLE 3).
Terconazole is an imidazole antifungal agent that inhibits fungal cytochrome P450 14α-demethylase, disrupting ergosterol synthesis and fungal cell membrane integrity.
| Metabolism | Hepatic via cytochrome P450 enzymes, primarily CYP3A4 and CYP1A2. |
| Excretion | Renal excretion accounts for approximately 70-80% of the administered dose, with about 20% excreted as unchanged drug and the remainder as metabolites. Fecal excretion is minimal (<5%). |
| Half-life | Terminal elimination half-life is approximately 7-9 hours in healthy adults, allowing for twice-daily dosing. In patients with hepatic impairment, half-life may be prolonged up to 18 hours, requiring dose adjustment. |
| Protein binding | Approximately 90% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.7-1.0 L/kg, indicating extensive tissue distribution, with high concentrations achieved in vaginal mucosa, skin, and nails. |
| Bioavailability | Vaginal cream: systemic absorption is minimal (<10%), with local bioavailability approaching 100% at the target site. Oral bioavailability is 40-60% when taken with food. |
| Onset of Action | For topical vaginal cream, onset of symptomatic relief (itching, discharge) typically occurs within 48-72 hours after initiation, with maximal effect by day 3. |
| Duration of Action | Duration of therapeutic effect is maintained for 24 hours with twice-daily application. Complete eradication of Candida species typically requires 3-7 days of continuous therapy. |
One vaginal tablet (200 mg) inserted intravaginally at bedtime for 3 consecutive days.
| Dosage form | CREAM |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment; not studied in severe impairment. |
| Pediatric use | Safety and efficacy not established; not recommended for pediatric use. |
| Geriatric use | No specific dosage adjustment; use standard adult dosing with caution due to potential comorbidities and polypharmacy. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TRIVAGIZOLE 3 (TRIVAGIZOLE 3).
| Breastfeeding | Not recommended during breastfeeding. In vitro data show tioconazole is highly protein-bound (99.7%) and excreted in human milk in unknown amounts; the M/P ratio is not determined. Potential for oral absorption by infant from milk; however, vaginal use leads to negligible systemic levels. Alternative antifungal agents preferred during lactation. |
| Teratogenic Risk | FDA Pregnancy Category C. No adequate well-controlled studies in pregnant women. In animal studies, intravaginal administration of 200 mg/kg/day (11 times human dose) resulted in maternal toxicity and fetal effects including increased resorptions and reduced ossification. First trimester: limited data, avoid unless clearly needed. Second and third trimesters: systemic absorption is minimal (<2%) with vaginal use, but caution advised. Not associated with major malformations in available human data. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to terconazole or any component of the formulation.","Known hypersensitivity to other imidazole antifungals."]
| Precautions | ["For intravaginal use only, not for ophthalmic or oral use.","If irritation or sensitization occurs, discontinue use.","May interact with latex products (e.g., condoms) causing reduced efficacy.","Safety in pregnancy (Category C) not established; use only if clearly needed."] |
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| Fetal Monitoring | No specific monitoring required for standard use. For prolonged therapy or in high-risk pregnancies, monitor for vaginal irritation or hypersensitivity. If used in pregnancy, monitor for signs of preterm labor or infection persistence. |
| Fertility Effects | No known effect on fertility. Animal studies at doses up to 200 mg/kg/day showed no impairment of fertility. No human data on fertility alteration. |