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estrone

G03CC04

Forms & Strengths

Vaginal cream: 0.1 mg/g

Adult Dosing

Atrophic vaginitis or kraurosis vulvae: 2 to 4 g of vaginal cream daily intravaginally for 2 weeks, then gradually reduced to half the initial dose for another 2 weeks; maintenance dose of 1 g 1 to 3 times weekly.

Pediatric Dosing

Safety and efficacy in pediatric patients have not been established.

Indications

Treatment of moderate to severe vasomotor symptoms associated with menopause
Treatment of atrophic vaginitis and kraurosis vulvae

Mechanism of Action

Binds to nuclear estrogen receptors in estrogen-responsive tissues, stimulating the transcription of estrogen-regulated genes, leading to decreased gonadotropin release and restoration of urogenital epithelium.

Contraindications

Undiagnosed abnormal genital bleeding
Known, suspected, or history of breast cancer
Known or suspected estrogen-dependent neoplasia
Active deep vein thrombosis, pulmonary embolism, or history of these conditions
Active or recent arterial thromboembolic disease (e.g., stroke, myocardial infarction)
Liver dysfunction or disease
Known protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders
Pregnancy

Adverse Reactions

Headache
Breast tenderness or pain
Abdominal pain, bloating, or nausea
Vaginal spotting, breakthrough bleeding, or changes in menstrual flow
Vaginal candidiasis
Thromboembolic events
Gallbladder disease

Drug Interactions

Inducers of CYP3A4 (e.g., rifampin, carbamazepine, phenobarbital) may decrease estrogen plasma concentrations
Inhibitors of CYP3A4 (e.g., ketoconazole, erythromycin) may increase estrogen exposure
Concomitant use with anticoagulants may alter therapeutic efficacy of either agent
Metyrapone response may be reduced by concurrent estrogen therapy

Curated Content: Needs Vetting Before Put to Clinical Use