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moxestrol

G03CB04

Forms & Strengths

Oral tablets: 50 mcg
Oral tablets: 250 mcg

Adult Dosing

Menopausal symptoms: 50 mcg to 150 mcg daily
Advanced breast cancer: 1 mg to 2 mg daily in divided doses
Suppression of lactation: 500 mcg daily for 3 days

Pediatric Dosing

Not indicated for pediatric use

Indications

Hormone replacement therapy for estrogen deficiency symptoms
Palliative treatment of advanced breast cancer in postmenopausal women
Suppression of postpartum lactation

Mechanism of Action

Synthetic, methylated estrogen receptor agonist
Binds to nuclear estrogen receptors in target tissues, regulating gene transcription
Suppresses gonadotropin secretion via negative feedback on the hypothalamus-pituitary axis

Contraindications

Known or suspected breast cancer (except when used for its treatment)
Estrogen-dependent neoplasia
Active deep vein thrombosis, pulmonary embolism, or history of thromboembolic disease
Active or recent arterial thromboembolic disease (stroke, myocardial infarction)
Undiagnosed abnormal genital bleeding
Known or suspected pregnancy
Severe hepatic impairment or active liver disease

Adverse Reactions

Thromboembolism (deep vein thrombosis, pulmonary embolism, stroke)
Endometrial hyperplasia and carcinoma in women with an intact uterus
Breast tenderness and enlargement
Nausea, vomiting, abdominal cramps, bloating
Headache, migraine
Cholestatic jaundice, hepatic dysfunction
Edema, weight changes
Changes in libido

Drug Interactions

CYP3A4 inducers (e.g., rifampin, carbamazepine, phenobarbital) may decrease estrogen efficacy
CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase plasma concentrations
Concomitant anticoagulants may have altered therapeutic efficacy
Antidiabetic agents may require dosage adjustment due to potential effects on glucose tolerance

Curated Content: Needs Vetting Before Put to Clinical Use