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GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › ESTROGENS › Synthetic estrogens, plain
dienestrol
G03CB01
Adult Dosing
- Atrophic vaginitis and kraurosis vulvae: 1 applicatorful (approx. 5 g) intravaginally daily or 1-2 times weekly as maintenance for 1-2 weeks, then gradually reduced to half initial dose
Pediatric Dosing
- Safety and efficacy not established in pediatric patients
Indications
- Treatment of atrophic vaginitis
- Treatment of kraurosis vulvae associated with the menopause
Mechanism of Action
- Synthetic nonsteroidal estrogen that binds to nuclear estrogen receptors in vaginal and vulvar tissues, restoring mucosal epithelium, elasticity, and acidic pH
Contraindications
- Known or suspected breast cancer
- Known or suspected estrogen-dependent neoplasia
- Active deep vein thrombosis, pulmonary embolism, or a history of these conditions
- Active arterial thromboembolic disease (e.g., stroke, myocardial infarction)
- Liver dysfunction or disease
- Undiagnosed abnormal genital bleeding
- Pregnancy
Adverse Reactions
- Headache
- Breast tenderness or enlargement
- Vaginal candidiasis
- Breakthrough bleeding or spotting
- Nausea and vomiting
- Local irritation or burning at application site
Drug Interactions
- CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort) may decrease estrogen concentrations
- CYP3A4 inhibitors (e.g., erythromycin, ketoconazole) may increase estrogen exposure
- Concomitant corticosteroids may increase corticosteroid efficacy and toxicity
- May diminish the efficacy of anticoagulants and antidiabetic agents
Curated Content: Needs Vetting Before Put to Clinical Use