TERAZOL 7
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TERAZOL 7 (TERAZOL 7).
Terconazole is an imidazole antifungal agent that inhibits the synthesis of ergosterol, a key component of fungal cell membranes, by inhibiting the enzyme lanosterol 14α-demethylase. This disruption increases membrane permeability and leads to fungal cell death.
| Metabolism | Terconazole is primarily metabolized in the liver via oxidation and glucuronidation. The metabolic pathways involve cytochrome P450 enzymes, likely CYP3A4. |
| Excretion | Primarily fecal (approximately 60%) as unchanged drug and metabolites; renal excretion accounts for about 20% (mostly metabolites). |
| Half-life | Terminal elimination half-life is approximately 7-10 hours; clinically, it allows for once-daily vaginal application, but systemic accumulation is minimal with vaginal dosing. |
| Protein binding | Approximately 90-95% bound to plasma proteins, mainly albumin. |
| Volume of Distribution | Vd is 2-4 L/kg, indicating extensive tissue distribution; clinical relevance: high concentrations in vaginal tissues. |
| Bioavailability | Vaginal: systemic absorption is low (approximately 4-14% of the dose); oral: not applicable (not administered orally). |
| Onset of Action | Vaginal: relief of symptoms (itching, discharge) typically begins within 24-72 hours after the first dose. |
| Duration of Action | Vaginal: clinical cure is achieved after a full 7-day course; effects persist if infection is eradicated, but recurrence may occur if incomplete treatment. |
Intravaginal: One full applicator (approximately 5 g of cream containing 40 mg of terconazole) inserted vaginally once daily at bedtime for 7 consecutive days.
| Dosage form | CREAM |
| Renal impairment | No dosage adjustment required for renal impairment. Safety and efficacy not established in severe renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. Safety and efficacy not established in severe hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established. Use not recommended. |
| Geriatric use | No specific dosage adjustment required. Use with caution due to potential for increased systemic absorption from atrophic vaginal mucosa. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TERAZOL 7 (TERAZOL 7).
| Breastfeeding | It is not known if terconazole is excreted in human milk. After vaginal administration, systemic levels are low, making significant excretion into breast milk unlikely. The manufacturer recommends caution during breastfeeding. M/P ratio not available. |
| Teratogenic Risk | Terazol 7 (terconazole) is a topical azole antifungal. Systemic absorption is minimal (approximately 5-16%) after vaginal application. No teratogenic effects have been observed in animal studies at systemic exposures several times the human vaginal dose. Human data are limited; however, due to low systemic absorption, the risk of fetal harm is considered low. Use during pregnancy, particularly in the first trimester, should be limited to cases where benefit outweighs potential unknown risk. |
■ FDA Black Box Warning
None
| Serious Effects |
["Known hypersensitivity to terconazole or any component of the formulation.","Not to be used in children less than 17 years of age (safety and efficacy not established)."]
| Precautions | ["For vaginal use only; not for ophthalmic or oral use.","Discontinue if sensitization or irritation occurs.","Do not use during menstruation; wait until menses has ended.","Use condoms during treatment to avoid possible irritation to the partner.","If lack of response, repeat cultures to confirm diagnosis and rule out other pathogens.","Safety in pregnancy has not been established; use only if clearly needed."] |
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| Fetal Monitoring | No specific monitoring required beyond standard prenatal care. Monitor for local adverse effects (e.g., burning, irritation). Efficacy should be assessed by resolution of symptoms. |
| Fertility Effects | No adverse effects on fertility have been reported. Terconazole is not expected to impact female or male fertility at therapeutic doses. |