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estrone

G03CA07

Forms & Strengths

Vaginal cream: 0.1 mg/g

Adult Dosing

Atrophic vaginitis / Kraurosis vulvae: Apply 2 to 4 g of vaginal cream daily intravaginally for 2 weeks, then gradually taper to 1 g 1 to 3 times weekly for maintenance

Pediatric Dosing

Not indicated for pediatric use

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 and promoting proliferation and development of female genital structures

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
Known or suspected pregnancy

Adverse Reactions

Headache
Breast tenderness or enlargement
Nausea and abdominal pain
Vaginal spotting or breakthrough bleeding
Vaginal candidiasis
Thromboembolism
Gallbladder disease
Hypertension

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
May diminish the efficacy of anticoagulants and antidiabetic agents
Concomitant administration with corticosteroids may lead to increased corticosteroid effects

Curated Content: Needs Vetting Before Put to Clinical Use