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GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › ESTROGENS › Estrogens, combinations with other drugs
methallenestril
G03CC03
Forms & Strengths
- Oral tablets: 3 mg
- Oral tablets: 6 mg
Adult Dosing
- Menopausal symptoms: 3 mg to 6 mg orally daily for 3 weeks, followed by a 1-week rest period
- Suppression of lactation: 6 mg orally twice daily for 5 days
Pediatric Dosing
- Not indicated for pediatric use
Indications
- Menopausal vasomotor symptoms
- Postpartum lactation suppression
- Hypogonadism in females (historical)
Mechanism of Action
- Non-steroidal estrogen receptor agonist
- Binds to estrogen receptors in target tissues, mimicking the effects of endogenous estradiol
- Suppresses pituitary gonadotropin secretion (FSH and LH)
Contraindications
- Known or suspected pregnancy
- Active or history of breast cancer
- Estrogen-dependent neoplasia
- Active deep vein thrombosis, pulmonary embolism, or history of these conditions
- Active arterial thromboembolic disease (stroke, myocardial infarction)
- Undiagnosed abnormal genital bleeding
- Severe hepatic impairment or active liver disease
Adverse Reactions
- Nausea, vomiting, abdominal cramps
- Breast tenderness and enlargement
- Breakthrough bleeding, spotting, changes in menstrual flow
- Headache, migraine
- Edema, weight gain
- Increased risk of thromboembolism
- Cholestatic jaundice
Drug Interactions
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease estrogen efficacy
- Anticoagulants: estrogens may diminish the therapeutic effect of anticoagulant therapy
- Corticosteroids: potential for enhanced pharmacologic effects of corticosteroids
- Insulin and oral antidiabetic agents: estrogens may impair glucose tolerance, requiring dosage adjustments
Curated Content: Needs Vetting Before Put to Clinical Use