Estradiol


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular
Advanced prostate cancer
Adult: As palliative treatment: As estradiol valerate: ≥30 mg every 1-2 weeks.

Intramuscular
Castration-associated oestrogen deficiency, Hypogonadism-associated oestrogen deficiency, Menopausal atrophic vaginitis, Moderate to severe vasomotor symptoms associated with menopause, Primary ovarian failure-associated oestrogen deficiency
Adult: As estradiol valerate: 10-20 mg every 4 weeks.

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

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

Oral
Castration-associated oestrogen deficiency, Hypogonadism-associated oestrogen deficiency, Menopausal atrophic vaginitis, Menopausal hormone replacement therapy, Moderate to severe vasomotor symptoms associated with menopause, Primary ovarian failure-associated oestrogen deficiency
Adult: 1-2 mg daily continuously (hysterectomised women) or cyclically (non-hysterectomised women).

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

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

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

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, Hypogonadism-associated oestrogen deficiency, Menopausal atrophic vaginitis, Moderate to severe vasomotor symptoms associated with menopause, 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
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.

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.
Cách dùng
May be taken with or without food.
Chống chỉ định
Hypersensitivity. History 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.
Thận trọng
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.
Phản ứng phụ
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.
IM/Parenteral/PO/Topical/Transdermal/Vag: X
MonitoringParameters
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.
Quá liều
Symptoms: Nausea, vomiting, bloating, abdominal pain, breast pain or tenderness, withdrawal bleeding. Management: Administer gastric lavage and symptomatic treatment.
Tương tác
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.
Tác dụng
Description: 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.
Pharmacokinetics:
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.
Đặc tính

Chemical Structure Image
Estradiol

Source: National Center for Biotechnology Information. PubChem Database. Estradiol, CID=5757, https://pubchem.ncbi.nlm.nih.gov/compound/Estradiol (accessed on Jan. 22, 2020)

Bảo quản
Store between 20-25°C.
Phân loại ATC
G03CA03 - estradiol ; Belongs to the class of natural and semisynthetic estrogens used in estrogenic hormone preparations.
References
Anon. Estradiol (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/03/2018.

Anon. Estradiol (Topical). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/03/2018.

Buckingham R (ed). Estradiol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/03/2018.

Climara Patch (Bayer HealthCare Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Delestrogen Injection (Par Pharmaceutical, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Depo-Estradiol Injection (Pharmacia and Upjohn Company LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Elestrin Gel, Metered (Meda Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Estrace Cream (Allergan, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Estrace Tablet (Allergan, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Estradiol Gel (Vertical Pharmaceuticals, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Estring Ring (Pharmacia and Upjohn Company LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Estrogel Gel, Metered (Ascend Therapeutics US, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Evamist Spray (Paddock Laboratories, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Femring Ring (Allergan, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Menostar Patch (Bayer HealthCare Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

Vagifem Insert (Novo Nordisk). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/03/2018.

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