Generic
17 β Estradiol
1 brands available in the market
At a glance
17 β Estradiol is a hormonal preparation used in the treatment of moderate to severe vasomotor symptoms (hot flashes) due to menopause and symptoms of vulvar and vaginal atrophy due to menopause. It is a topical gel applied to the skin.
Description
17 β Estradiol is an estrogen hormone used in the treatment of menopausal symptoms. Estradiol is the principal intracellular human estrogen and is substantially more potent than its metabolites, estrone and estriol, at the receptor level.
In normally cycling adult women, the primary source of estrogen is the ovarian follicle, which secretes 70-500 mcg of estradiol daily depending on the phase of the menstrual cycle. After menopause, most endogenous estrogen is produced by conversion of androstenedione to estrone in peripheral tissues.
Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate pituitary secretion of gonadotropins (LH and FSH) through a negative feedback mechanism.
Indications
- Moderate to severe vasomotor symptoms (hot flashes) due to menopause
- Symptoms of vulvar and vaginal atrophy due to menopause
Therapeutic class
Hormonal Therapy
Pharmacological class
Estrogen
Pharmacology
Estrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estradiol is the principal intracellular human estrogen and is substantially more potent than estrone and estriol at the receptor level. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues, regulating gene transcription. Circulating estrogens modulate pituitary secretion of gonadotropins (LH and FSH) through a negative feedback mechanism, reducing elevated levels seen in postmenopausal women.
Mechanism of action
Estrogens bind to estrogen receptors (ERα and ERβ), activating gene transcription in target tissues. They affect the thermoregulatory center to reduce vasomotor symptoms (hot flashes) and promote estrogenization of vaginal and vulvar tissues to prevent atrophy.
Dosage
Vasomotor Symptoms and Vulvar/Vaginal Atrophy:
• Estradiol 0.06% gel 1.25 g once daily.
• Recommended application site: Arm (from wrist to shoulder, both inner and outer surfaces).
• In women with a uterus, consider adding a progestogen to reduce endometrial cancer risk.
• Women without a uterus generally do not need a progestogen (except those with a history of endometriosis).
• Use the lowest effective dose for the shortest duration.
• Reevaluate periodically to determine if treatment is still necessary.
For Vulvar and Vaginal Atrophy: First consider the use of topical vaginal products.
Priming before first use: Remove the large canister cover and fully depress the pump 5 times. Discard unused gel.
Application: Apply a thin layer over the entire arm from wrist to shoulder on both inner and outer surfaces.
Administration
For topical application only. Apply a thin layer on the arm (wrist to shoulder). Wash hands thoroughly after application. Follow the dose and duration as advised by your physician.
Missed dose
If you miss a dose, apply it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
Side effects
- Breast pain or tenderness
- Headache
- Nausea
- Abdominal cramps
- Weight gain
- Skin irritation at application site
- Other estrogen-related side effects
Precautions & warnings
- Do not use during pregnancy.
- Caution in patients with liver disease or impairment.
- Caution in patients with history of thromboembolic disease.
- May reduce milk production during breastfeeding.
- Regular breast and pelvic examinations are recommended.
- Inform your doctor if you experience undiagnosed abnormal genital bleeding.
Contraindications
- Undiagnosed abnormal genital bleeding
- Breast cancer or history of breast cancer
- Estrogen-dependent neoplasia
- Active DVT, PE, or history of these conditions
- Active arterial thromboembolic disease (e.g., stroke or MI) or history
- Anaphylactic reaction, angioedema, or hypersensitivity to Estradiol
- Hepatic impairment or disease
- Protein C, protein S, or antithrombin deficiency, or other thrombophilic disorders
Drug interactions
- CYP3A4 inducers (St. John's wort, phenobarbital, carbamazepine, rifampin): May reduce plasma concentrations of estrogens, resulting in decreased therapeutic effects and/or changes in uterine bleeding profile.
- CYP3A4 inhibitors (erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice): May increase plasma concentrations of estrogen and may result in adverse reactions.
Food interactions
CYP3A4 inhibitors such as grapefruit juice may increase plasma concentrations of estrogen and may result in adverse reactions.
Use in pregnancy
Estradiol is not indicated for use in pregnancy. No adequate controlled studies in pregnant women. Epidemiologic studies have not found an increased risk of birth defects following exposure to combined hormonal contraceptives before conception or during early pregnancy.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Estrogens are present in human milk and can reduce milk production in breastfeeding women. Consider the developmental and health benefits of breastfeeding, the mother's clinical need, and potential adverse effects on the breastfed child.
Pediatric use
Not indicated for use in children.
Geriatric use
No specific dose adjustment required for elderly, but consult your physician.
Renal / hepatic impairment
Contraindicated in hepatic impairment or disease.
Overdose effects
Overdose may increase estrogen-related side effects. Consult your doctor if overdose is suspected.
Storage conditions
Store below 25°C, away from light and moisture. Keep out of reach of children.
Chemical structure
17 β Estradiol