Estradiol


Full Generic Medicine Info
Dosage/Direction for Use

Oral
Advanced prostate cancer
Adult: As palliative treatment: 1-2 mg tid.

Oral
Prophylaxis of osteoporosis in postmenopausal women
Adult: 2 mg daily continuously (hysterectomised women) or cyclically (non-hysterectomised women).

Oral
Menopausal hormone replacement therapy
Adult: 1-2 mg daily continuously (hysterectomised women) or cyclically (non-hysterectomised women).

Oral
Menopausal atrophic vaginitis
Adult: 1-2 mg daily continuously (hysterectomised women) or cyclically (non-hysterectomised women).

Oral
Moderate to severe vasomotor symptoms associated with menopause
Adult: 1-2 mg daily continuously (hysterectomised women) or cyclically (non-hysterectomised women).

Oral
Castration-associated oestrogen deficiency
Adult: 1-2 mg daily continuously (hysterectomised women) or cyclically (non-hysterectomised women).

Oral
Primary ovarian failure-associated oestrogen deficiency
Adult: 1-2 mg daily continuously (hysterectomised women) or cyclically (non-hysterectomised women).

Oral
Hypogonadism-associated oestrogen deficiency
Adult: 1-2 mg daily continuously (hysterectomised women) or cyclically (non-hysterectomised women).

Oral
Metastatic breast cancer
Adult: As palliative treatment: 10 mg tid for at least 3 months.

Intramuscular
Moderate to severe vasomotor symptoms associated with menopause
Adult: As estradiol cypionate: 1-5 mg every 3-4 weeks.

Intramuscular
Hypogonadism-associated oestrogen deficiency
Adult: As estradiol cypionate: 1.5-2 mg monthly.

Intramuscular
Primary ovarian failure-associated oestrogen deficiency
Adult: As estradiol valerate: 10-20 mg every 4 weeks.

Intramuscular
Hypogonadism-associated oestrogen deficiency
Adult: As estradiol valerate: 10-20 mg every 4 weeks.

Intramuscular
Castration-associated oestrogen deficiency
Adult: As estradiol valerate: 10-20 mg every 4 weeks.

Intramuscular
Moderate to severe vasomotor symptoms associated with menopause
Adult: As estradiol valerate: 10-20 mg every 4 weeks.

Intramuscular
Menopausal atrophic vaginitis
Adult: As estradiol valerate: 10-20 mg every 4 weeks.

Intramuscular
Advanced prostate cancer
Adult: As palliative treatment: As estradiol valerate: ≥30 mg every 1-2 weeks.

Transdermal
Menopausal hormone replacement therapy
Adult: Each patch delivers 0.025-0.1 mg estradiol per 24 hours: Apply once or twice weekly on a clean, dry area of skin of the lower abdomen or upper buttock. As gel containing 0.5 or 1 mg estradiol per single-dose container: Apply 0.5-1.5 mg daily as a thin layer on either the right or left upper thigh. May be used continuously (hysterectomised women) or cyclically (non-hysterectomised women).

Transdermal
Moderate to severe vasomotor symptoms associated with menopause
Adult: Each patch delivers 0.025-0.1 mg estradiol per 24 hours: Apply once or twice weekly on a clean, dry area of skin of the lower abdomen or upper buttock. As gel containing 0.25, 0.5 or 1 mg estradiol per single-dose container: Apply 0.5-1.5 mg once daily as a thin layer on either the right or left upper thigh. As gel in metered dose pump releasing 0.52 or 0.75 mg estradiol per actuation: Apply once daily as a thin layer on either the right or left upper arm. As spray releasing 1.53 mg estradiol per actuation: 1-3 sprays once daily (in the morning) on adjacent, non-overlapping areas on the inner surface of the forearm.

Transdermal
Menopausal atrophic vaginitis
Adult: Each patch delivers 0.025-0.1 mg estradiol per 24 hours: Apply once or twice weekly on a clean, dry area of skin of the lower abdomen or upper buttock. As gel in metered dose pump releasing 0.75 mg estradiol per actuation: Apply once daily as a thin layer over the entire arm on the inside and outside from wrist to shoulder.

Transdermal
Prophylaxis of osteoporosis in postmenopausal women
Adult: Each patch delivers 0.014-0.1 mg estradiol per 24 hours: Apply once or twice weekly on a clean, dry area of skin of the lower abdomen or upper buttock.

Transdermal
Castration-associated oestrogen deficiency
Adult: Each patch delivers 0.025-0.1 mg estradiol per 24 hours: Apply once or twice weekly on a clean, dry area of skin of the lower abdomen or upper buttock.

Transdermal
Hypogonadism-associated oestrogen deficiency
Adult: Each patch delivers 0.025-0.1 mg estradiol per 24 hours: Apply once or twice weekly on a clean, dry area of skin of the lower abdomen or upper buttock.

Transdermal
Primary ovarian failure-associated oestrogen deficiency
Adult: Each patch delivers 0.025-0.1 mg estradiol per 24 hours: Apply once or twice weekly on a clean, dry area of skin of the lower abdomen or upper buttock.

Vaginal
Moderate to severe vasomotor symptoms associated with menopause
Adult: As vaginal ring releasing 0.05 or 0.1 mg estradiol per 24 hours: Place 1 ring into the upper third of the vagina for 90 days.

Vaginal
Menopausal atrophic vaginitis
Adult: As vaginal ring releasing 0.0075, 0.05 or 0.1 mg estradiol per 24 hours Place 1 ring into the upper third of the vagina for 90 days. As vaginal tab containing 0.01 mg estradiol: Place 1 tab daily for 2 weeks then, 1 tab twice weekly. As vaginal insert containing 0.01 mg or 0.025 mg estradiol: Place 1 insert daily for 2 weeks then, 1 insert twice weekly. As 0.01% vaginal cream: 2-4 g daily for 1 or 2 weeks, reduce to 1-2 g daily for 1 or 2 weeks, then 1 g 1-3 times weekly as maintenance.
Administration
May be taken with or without food.
Contraindications
Hypersensitivity. History of or current breast cancer (except for certain metastatic breast cancer cases), CV disorders (e.g. MI, stroke, pulmonary embolism, DVT). Oestrogen-dependent tumours (e.g. endometrial cancer). Undiagnosed genital bleeding. Untreated endometrial hyperplasia. Thrombophilic disorders (e.g. protein C, protein S, antithrombin deficiency). Porphyria. Hepatic impairment. Pregnancy and lactation.
Special Precautions
Patient with history of endometrial hyperplasia, cholestatic jaundice; risk factors for CV disorders (e.g. personal or family history, obesity, diabetes mellitus, hypertension, hypercholesterolaemia, SLE, prolonged immobilisation); leiomyoma (uterine fibroids) or endometriosis, coronary artery disease, migraine, epilepsy, asthma, cholelithiasis, hepatic haemangiomas, hypertriglyceridemia, hypoparathyroidism, severe hypocalcaemia, otosclerosis, cardiac impairment, hereditary angioedema; short narrow vagina, uterovaginal prolapse, vaginal infection (vaginal). Patient who underwent surgery. Not intended for prevention of dementia. Renal impairment. Non-hysterectomised women. Smoking. Monitoring Parameters Assess personal and family medical history before and regularly during therapy. Include blood pressure, breast and endometrial examinations including mammography, endometrial sampling and Papanicolaou smear. Also monitor bone density (when used as prophylaxis of osteoporosis); for signs and symptoms of retinal vascular thrombosis, thromboembolic disorders. Periodically evaluate the need to continue treatment.
Adverse Reactions
Significant: Breast, endometrial or ovarian cancers; endometrial hyperplasia, breakthrough bleeding and spotting, CV disorders (e.g. MI, stroke, pulmonary embolism, DVT), retinal vascular thrombosis, dementia, gallbladder disease, hypertension, increased HDL-cholesterol and decreased LDL-cholesterol, increased thyroid binding globulin levels, chloasma; impotence and feminising effects in males (when used as palliative treatment for advanced prostate cancer); UTI, vaginal irritation or infection (vaginal); breast budding or masses in prepubertal females, gynecomastia and breast masses in prepubertal males (due to secondary exposure). Ear and labyrinth disorders: Otitis media. Eye disorders: Conjunctivitis. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, constipation, dyspepsia, flatulence, abdominal pain, gastroenteritis. General disorders and administration site conditions: Weakness, lethargy, oedema, pain, flu-like symptoms. Infections and infestations: Infections (e.g. fungal infections). Injury, poisoning and procedural complications: Application site reactions (transdermal). Metabolism and nutrition disorders: Weight fluctuation. Musculoskeletal and connective tissue disorders: Arthropathy, arthalgia, myalgia, back, neck or limb pain. Nervous system disorders: Headache, dizziness, hypoaesthesia. Psychiatric disorders: Nervousness, anxiety, depression, insomnia, libido disorder. Renal and urinary disorders: Bladder discomfort (vaginal) Reproductive system and breast disorders: Dysmenorrhoea, metrorrhagia, vaginal discharge, breast tenderness, pain or enlargement; vulvovaginal discomfort, vaginal haemorrhage (vaginal). Respiratory, thoracic and mediastinal disorders: Cough, sinus congestion, sinusitis, nasopharyngitis, pharyngitis, upper respiratory tract infection, bronchitis, rhinitis, asthma. Skin and subcutaneous tissue disorders: Rash, erythema, pruritus, hyperhidrosis. Vascular disorders: Hot flushes.
Potentially Fatal: Anaphylaxis.
Overdosage
Symptoms: Nausea, vomiting, bloating, abdominal pain, breast pain or tenderness, withdrawal bleeding. Management: Administer gastric lavage and symptomatic treatment.
Drug Interactions
May cause increased exposure with CYP3A4 inhibitors (e.g. fluconazole, clarithromycin, diltiazem. May cause decreased exposure with CYP3A4 inducers (e.g. phenobarbital, griseofulvin, rifampicin, efavirenz. Decreases absorption of folic acid.
Food Interaction
Avoid alcohol. May cause increased exposure with grapefruit juice. May cause decreased exposure with St. John's Wort.
Lab Interference
May interfere with results of tests for coagulation factors, lipids, glucose tolerance and binding proteins. Decreases response to metyrapone test.
Action
Estradiol is a synthetic sex hormone similar to endogenous oestrogen. During menopause, estradiol substitutes for oestrogen production and alleviates its symptoms. Estradiol also prevents bone loss following menopause or ovariectomy. Synonym: oestradiol.
Absorption: Well absorbed from the gastrointestinal tract, skin and mucous membranes. Time to peak plasma concentration: 1.5-2 hours (oral).
Distribution: Widely distributed. Enters breast milk. Plasma protein binding: 61% to albumin and approx 37% to sex hormone binding globulin (SHBG).
Metabolism: Metabolised in the liver partially by CYP3A4 enzymes to estrone and estriol. Undergoes enterohepatic recirculation (oral).
Excretion: Mainly via urine as estradiol, estrone, estriol and its glucuronide and sulfate conjugates; faeces, as unconjugated metabolites.
Storage
Intramuscular: Store between 20-25°C. Oral: Store between 20-25°C. Transdermal: Store between 20-25°C. Vaginal: Store between 20-25°C.
CIMS Class
Oestrogens & Progesterones & Related Synthetic Drugs
ATC Classification
G03CA03 - estradiol ; Belongs to the class of natural and semisynthetic estrogens used in estrogenic hormone preparations.
Disclaimer: This information is independently developed by CIMS based on estradiol from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 CIMS. All rights reserved. Powered by CIMSAsia.com
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in