MYCELEX-7
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MYCELEX-7 (MYCELEX-7).
Clotrimazole, an azole antifungal, inhibits fungal cytochrome P450 14α-demethylase, disrupting ergosterol synthesis and increasing membrane permeability.
| Metabolism | Hepatic metabolism via CYP3A4 to inactive metabolites. |
| Excretion | Primarily via feces as unchanged drug (approx. 50%) and metabolites. Renal excretion of unchanged drug is minimal (<1%) as the drug is poorly absorbed from the vagina. Biliary excretion contributes to fecal elimination. |
| Half-life | The systemic half-life of clotrimazole following vaginal administration is approximately 0.5–1 hour due to rapid metabolism and elimination. This short half-life reflects minimal systemic absorption (3–10%). |
| Protein binding | Approximately 90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Apparent Vd is approximately 10–20 L/kg, suggesting extensive tissue distribution. However, due to minimal systemic absorption, this value is largely theoretical. |
| Bioavailability | Systemic bioavailability after vaginal administration is 3–10%. Oral bioavailability is low (<5%) due to poor absorption and extensive first-pass metabolism. |
| Onset of Action | Onset of antifungal effect is within 24–72 hours after vaginal insertion, corresponding to the time required to achieve therapeutic concentrations in vaginal tissues. |
| Duration of Action | Therapeutic concentrations persist in vaginal secretions for up to 72 hours after a single dose. A 7-day course is recommended for complete eradication. |
Clotrimazole 100 mg vaginal tablet inserted intravaginally once daily at bedtime for 7 days.
| Dosage form | TABLET |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment; use with caution in severe hepatic impairment. |
| Pediatric use | Not recommended for use in pediatric patients. |
| Geriatric use | No specific dosage adjustment required; same as adult dosing. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for MYCELEX-7 (MYCELEX-7).
| Breastfeeding | Clotrimazole is excreted in breast milk in negligible amounts after topical vaginal use. M/P ratio unknown due to low systemic absorption. Considered compatible with breastfeeding; apply after nursing to minimize infant exposure. |
| Teratogenic Risk | Clotrimazole (MYCELEX-7) is a category B drug. No teratogenic effects observed in animal studies. Limited human data in first trimester: no increased risk of major malformations. Vaginal absorption minimal (3-10%). Use in second and third trimesters considered safe when applied topically. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to clotrimazole or any component. Known hypersensitivity to other azole antifungals.
| Precautions | For intravaginal use only. Discontinue if irritation or hypersensitivity occurs. Avoid use during menstruation. May damage latex condoms and diaphragms. |
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| Fetal Monitoring |
| No specific monitoring required beyond routine pregnancy care. Monitor for local irritation or allergic reactions. In recurrent infections, consider diabetes screening. |
| Fertility Effects | No reported effects on fertility. Clotrimazole does not alter ovulation, implantation, or sperm function. Not indicated for use in preconception period but no adverse effects anticipated. |