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GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › GONADOTROPINS AND OTHER OVULATION STIMULANTS › Ovulation stimulants, synthetic
epimestrol
G03GB03
Adult Dosing
- 5 mg orally once daily from day 5 to day 14 or 16 of the menstrual cycle
- Duration of treatment typically 2 to 3 consecutive cycles for ovulation induction
Pediatric Dosing
- Not indicated for pediatric use
Indications
- Anovulatory infertility
- Secondary amenorrhea due to estrogen deficiency or hypothalamic-pituitary dysfunction
Mechanism of Action
- Weak estrogen receptor agonist/antagonist with partial estrogenic activity
- Competes with endogenous estrogens at hypothalamic-pituitary receptor sites
- Stimulates the release of gonadotropin-releasing hormone (GnRH), subsequently increasing secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) to induce ovulation
Contraindications
- Known or suspected pregnancy
- Undiagnosed abnormal uterine bleeding
- Active or history of venous thromboembolism (VTE) or thrombophlebitis
- Active hepatic disease or liver dysfunction
- Estrogen-dependent malignant neoplasm (e.g., breast cancer, endometrial cancer)
- Hypersensitivity to epimestrol or excipients
Adverse Reactions
- Hot flashes and vasomotor symptoms
- Nausea and abdominal discomfort
- Headache and dizziness
- Ovarian enlargement
- Breast tenderness
- Breakthrough bleeding or spotting
Drug Interactions
- CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort) may decrease systemic exposure and efficacy
- Anticoagulants: Estrogenic activity may diminish the therapeutic effect of anticoagulant therapy
- Hormonal contraceptives: Concurrent use diminishes the intended pharmacodynamic response of ovulation induction
Curated Content: Needs Vetting Before Put to Clinical Use