Estradiol

Indications
 Oral
Prostate cancer
Adult: For androgen-dependent, inoperable and progressing cancer: 10 mg tid for at least 3 mth.
Oral
Moderate to severe vasomotor symptoms associated with menopause
Adult: 1-2 mg/day adjusted as necessary; admin can be cyclical (3 wk on, 1 wk off) or continuous. In conjunction with a progestogen in women with uterus.
Oral
Prophylaxis of osteoporosis in postmenopausal women
Adult: 0.5 mg/day in cyclic regimen (23 days on and 5 days off).
Oral
Hypogonadism
Adult: 1-2 mg/day in a cyclic regimen for 3 wk on drug, followed by 1 wk drug-free.
Intramuscular
Prostate cancer
Adult: As valerate: ≥30 mg every 1-2 wk.
Intramuscular
Moderate to severe vasomotor symptoms associated with menopause
Adult: As cypionate: 1-5 mg every 3-4 wk; as valerate: 10-20 mg every 4 wk. In conjunction with a progestogen in women with uterus.
Transdermal
Moderate to severe vasomotor symptoms associated with menopause
Adult: Each patch delivers 0.025 mg/day: Initially, apply once wkly, adjust dose as necessary to control symptoms. Attempt to taper or discontinue treatment at 3-6 mth intervals. In conjunction with a progestogen in women with uterus.
Transdermal
Prophylaxis of osteoporosis in postmenopausal women
Adult: Each patch delivers 14 mcg/day. Apply patch once or twice wkly. Adjust dose by monitoring biochemical markers and bone mineral density. A 14-day course of progestogen is required in women with an intact uterus once every 6-12 mth.
Intramuscular
Hypogonadism
Adult: As valerate: 10-20 mg every 4 wk. As cypionate: 1.5-2 mg mthly.
Vaginal
Vulvular and vaginal atrophy
Adult: Insert 2-4 g/day of vag cream intravaginally for 2 wk, then reduce gradually to half the initial dose for 2 wk followed by a maintenance dose of 1 g 1-3 times/wk.
Vaginal
Postmenopausal vaginal atrophy
Adult: Insert a vag ring containing 2 mg of estradiol and keep in place for 90 days.
Vaginal
Urogenital symptoms
Adult: Insert a vag ring containing 2 mg of estradiol and keep in place for 90 days.
Vaginal
Atrophic vaginitis
Adult: Initial: Insert 1 tab (20 mcg) once daily for 2 wk. Maintenance: Insert 1 tab twice wkly. Attempt to discontinue or taper medication at 3-6 mthly intervals.
Contraindications
 Hypersensitivity; undiagnosed vag bleeding; thrombophloebitis or thromboembolic disorders; breast carcinoma except in selected patients being treated for metastatic disease; oestrogen-dependent tumor; porphyria; pregnancy.
Warnings / Precautions
 Conditions exacerbated by fluid retention; hypercalcaemia, cerebrovascular diorders, coronary artery disease, gall bladder diseases; lipid effects; familial defects of lipoprotein metabolism. May increase BP, risk of venous thromboembolism, breast cancer, benign hepatic adenoma, endometrial cancer and size of preexisting uterine leiomyomata. Dosage should be reduced in hepatic impairment. Lactation. Child.
Adverse Reactions
 GI disturbances, genitourinary changes, haematologic disorders, CV and CNS effects, endocrine and metabolic disorders, cholestatic jaundice, local skin reactions, chorea, contact lens intolerance, steeping of corneal curvature, pulmonary thromboembolism, carbohydrate intolerance.
Drug Interactions
 CYP1A2 and CYP3A4 inducers e.g. aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol. May enhance the effects of hydrocortisone and prednisolone when used together.
See Below for More estradiol Drug Interactions
Lab Interactions
 Reduced serum folate concentration and response to metyrapone test. May interfere with thyroid function and glucose tolerance tests.
Food Interactions
 Folic acid absorption may be reduced. Ethanol increases the risk of osteoporosis; routine use of ethanol may also increase estrogen level and thus risk of breast cancer. Black cohosh, dong quai, red clover, saw palmetto, ginseng, St John's wort.
Mechanism of Actions
 Estradiol is a naturally occurring oestrogen. Oestrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. They modulate the pituitary secretion of gonadotrophins, LH and FSH through a negative feedback system.
Absorption: Readily absorbed from the GI tract and through the skin or mucous membranes.
Distribution: Largely bound to plasma proteins.
Metabolism: Partly metabolised hepatically to less active oestrogens such as estriol and estrone.
Storage Conditions
 Intramuscular: Store at room temperature. Oral: Store at room temperature. Transdermal: Store at room temperature. Vaginal: Store at room temperature.
ATC Classification
 G03CA03 - estradiol ; Belongs to the class of natural and semisynthetic estrogens used in estrogenic hormone preparations.
Storage
 Intramuscular: Store at room temperature. Oral: Store at room temperature. Transdermal: Store at room temperature. Vaginal: Store at room temperature.
Available As
  • Estradiol 0.025 mg
  • Estradiol 0.05 mg
  • Estradiol 0.06% w/w
  • Estradiol 0.1 mg
  • Estradiol 0.1% w/w
  • Estradiol 1 mg
  • Estradiol 1.5 mg
  • Estradiol 1.8 mg
  • Estradiol 10 mg
  • Estradiol 2 mg
  • Estradiol 3 mg
  • Estradiol 3.2 mg
  • Estradiol 35% w/w
  • Estradiol Phenylpropionate 4 mg

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