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Estradiol information from DrugsUpdate  

See Available Brands of Estradiol in India

P - Contraindicated in pregnancy
L - Caution when used during lactation
FI - Food *
LI - Lab *

Estradiol (E2 or 17β-estradiol) (also oestradiol) is a sex hormone. Estradiol is the predominant sex hormone present in females; however, it is present in males, albeit at lower levels, as well. It represents the major estrogen in humans. Estradiol has not only a critical impact on reproductive and sexual functioning, but also affects other organs including the bones.

Pharmacodynamics

Pharmacokinetics

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.

Estradiol Indications / Estradiol Uses

Information Not Available

Estradiol Adverse Reactions / Estradiol Side Effects

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.

Precautions

Warnings
Endometrial cancer

Close clinical surveillance of all women taking estrogens is important. The use of unopposed estrogen in women with intact uteri has been associated with an increased risk of endometrial cancer. Diagnostic measures, including endometrial sampling when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding.

CV and other risks

Estrogens with or without progestins should not be used for prevention of CV disease. The Women's Health Initiative (WHI) study reported increased risk of MI, stoke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women 50 to 79 yr of age during 5.6 yr of treatment with oral conjugated estrogens 0.625 mg combined with medroxyprogesterone acetate 2.5 mg compared with placebo.

Dementia
A subsidiary of WHI, the WHI Memory Study, reported increased risk of developing probable dementia in postmenopausal women 65 yr of age or older during 4 yr of treatment with oral conjugated estrogens plus medroxyprogesterone acetate compared with placebo. It is unknown if this finding applies to younger postmenopausal women or women taking estrogen alone.

Monitor
Monitor BP at beginning of therapy and at regular intervals during treatment. Periodically monitor thyroid function.

Special 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.

Other 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.

Other Interactions

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.

Dosage

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
Osteoporosis prophylaxis 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.

Intramuscular
Hypogonadism
Adult: As valerate: 10-20 mg every 4 wk. As cypionate: 1.5-2 mg mthly.

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
Osteoporosis prophylaxis 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.

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.

Food(before/after)

Information Not Available

List of Contraindications

Estradiol and Pregnancy

Contraindicated in pregnancy

Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Estradiol and Lactation

Caution when used during lactation

Estradiol and Children

Safety and effectiveness in pediatric patients have not been established. Large and repeated doses of estrogen over an extended period of time have been shown to accelerate epiphyseal closure, resulting in short adult stature if treatment is initiated before the completion of physiologic puberty in normally developing children. In patients in whom bone growth is not complete, periodic monitoring of bone maturation and effects on epiphyseal centers is recommended.

Estrogen treatment of prepubertal children also induces premature breast development and vaginal cornification, and may potentially induce vaginal bleeding in girls. In boys, estrogen treatment may modify the normal pubertal process. All other physiological and adverse reactions shown to be associated with estrogen treatment of adults could potentially occur in the pediatric population, including thromboembolic disorders and growth stimulation of certain tumors. Therefore, estrogens should only be administered to pediatric patients when clearly indicated and the lowest effective dose should always be utilized.

Estradiol and Geriatic

The safety and efficacy of Estradiol tablets in geriatric patients has not been established. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greatest frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.

In the Women’s Health Initiative Memory Study, including 4,532 women 65 years of age and older, followed for an average of 4 years, 82% (n = 3,729) were 65 to 74 while 18% (n = 803) were 75 and over. Most women (80%) had no prior hormone therapy use. Women treated with conjugated estrogens plus medroxyprogesterone acetate were reported to have a two-fold increase in the risk of developing probable dementia. Alzheimer’s disease was the most common classification of probable dementia in both the conjugated estrogens plus medroxyprogesterone acetate group and the placebo group. Ninety percent of the cases of probable dementia occurred in the 54% of women that were older than 70.

It is unknown whether these findings apply to estrogen alone therapy.

Estradiol and Other 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.

Storage

Intramuscular
Store at room temperature.

Oral

Store at room temperature.

Transdermal
Store at room temperature.

Vaginal

Store at room temperature.

Lab interference

Intramuscular
Store at room temperature.

Oral

Store at room temperature.

Transdermal
Store at room temperature.

Vaginal

Store at room temperature.

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