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. |
| Molecular Weight | 344.84 |
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 | Generally considered safe; topical clotrimazole has minimal systemic absorption. Limited data show no increased risk of major malformations. |
| 2nd trimester | Considered safe for topical use; systemic absorption negligible. No known fetal risk. |
| 3rd trimester | Considered safe for topical use; avoid high-dose prolonged use near term due to theoretical risk of premature labor from prostaglandin release. |
Clinical note
Comprehensive clinical and safety monograph for MYCELEX-7 (MYCELEX-7).
| Placental transfer | Minimal to negligible placental transfer due to low systemic absorption after topical application. Oral clotrimazole (not typically used) shows limited transfer. |
| Breastfeeding | Topical clotrimazole has minimal systemic absorption; it is unlikely to pass into breast milk in significant amounts. However, apply to smallest area and avoid direct contact with infant's mouth. No adverse effects reported in nursed infants. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to clotrimazole or any component of the formulation
| Precautions | For intravaginal use only. Discontinue if irritation or hypersensitivity occurs. Avoid use during menstruation. May damage latex condoms and diaphragms. |
| Food/Dietary | No known food interactions. |
| Clinical Pearls | MYCELEX-7 (clotrimazole 1% vaginal cream) is approved for vulvovaginal candidiasis. For uncomplicated infections, a 7-day course is standard; for recurrent or complicated cases, extend to 14 days. Avoid in patients with hypersensitivity to clotrimazole or any component. Monitor for local irritation or hypersensitivity. Refrain from sexual intercourse during treatment. Applicator should be cleaned after each use. |
Loading safety data…
| Lactation Rating | L1 |
| 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. |
| 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. |
| Patient Advice | Insert one applicatorful of cream into the vagina at bedtime for 7 consecutive days. · Complete the full course even if symptoms improve to prevent recurrence. · Do not use tampons, douches, spermicides, or other vaginal products during treatment. · Wash hands before and after insertion. Discard the applicator after use. · Refrain from vaginal intercourse during therapy. · If you miss a dose, insert it as soon as you remember, but skip if close to next dose; do not double dose. · Contact your healthcare provider if symptoms persist beyond 7 days or if you develop fever, chills, or lower abdominal pain. · This product does not protect against sexually transmitted infections. |