Estradiol
- Atc Codes:G03CA03
- CAS Codes:50-28-2
- PHARMGKB ID:50-28-2
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Aerodiol, Climara, Dermestril-Septem, Estradot, Estramon, Estrofem, Estrogel, FemSeven, Klimapur, Östradiol; Systen, Vagifem, Belgium: Aerodiol, Climara, Dermestril, Estradiol, Estreva, Estrofem, Feminova, Meno-Implant, Oestrogel, Progynova, Systen, Vagifem, Vivelle Dot, Zumenon; Bulgaria: Climara, Estrofem, Oestrogel, Systen; Cyprus: Estraderm TTS, Evorel 50, Oestrogel, Vagifem; Czech Republic: Agofollin, Climara, Dermestril, Divigel, Estraderm MX, Estraderm TTS, Estradot, Estrahexal, Estrapatch, Estrimax, Estrofem, Linoladiol N, Neofollin, Octodiol, Oestrogel, Riselle, Systen, Vagifem; Denmark: Divigel, Estradiol, Estring, Estrofem, Estrogel, Evorel, Femanest, Incurin, Oestrogel, Progynon, Vagifem, Vivelle Dot, Ostradiol; Estonia: Climara, Divigel, Estradiol, Estrofem, Linoladiol N, Vagifem; Finland: Climara, Divigel, Estradiol, Estradot, Estrena, Estring, Estrofem, Estrogel, Evorel, Femseven, Vagifem, Zumenon; France: Avadene, Climara, Delidose, Dermestril, Estraderm TTS, Estradiol G, Estrapatch, Estreva, Estrofem, Femsept, Oesclim, Oestrodose, Oestrogel, Oromone, Progynova, Provames, Thais, Vivelledot; Germany: Aerodiol, Cutanum, Dermestril, Ephelia, Estrabeta, Estraderm MX, Estraderm TTS, Estradiol, Estradot, Estramon, Estreva, Estrifam, Estring, Estronorm, Fem 7, Femsept, Gynokadin, GynPolar, Linoladiol N, Menformon-K, Menorest, Meriestra, Merimono, Progynova, Sandrena, Tradelia, Vagifem; Greece: Dermestril, Ephelia, Estradot, Estramon, Estrofem, Femring, Oestrogel, Vagifem; Hungary: Calidiol, Dermestril, Divigel, Estraderm TTS, Estrapatch, Estrimax, Estrofem, Fem7, Femseven, Linoladiol N, Vagifem; Ireland: Aerodiol, Climara, Dermestril-Septem, Divigel, Epiestrol-Septem, Estraderm TTS, Estradiol, Estradot, Estreva, Estrofem, Evorel 50, Fematab, Oestrogel, Vagifem; Italy: Armonil, Climara, Dermestril, Epiestrol, Estraderm MX, Estraderm TTS, Estrodose, Estrofem, Gelestra, Ginaikos, Progynova, Sandrena, Systen, Vagifem, Zerella; Latvia: Climara, Dermestril, Divigel, Estrimax, Estrofem, Linoladiol N, Vagifem; Lithuania: Climara, Divigel, Estramon, Estrimax, Estrofem, Linoladiol N, Vagifem; Luxembourg: Climara, Dermestril, Divigel, Estraderm TTS, Estrofem, Estropatch, Menorest, Oestrogel, Systen, Vagifem, Zumenon; Malta: Aerodiol, Estradiol, Estreva, Estrofem, Evorel 50, Progynova, Vagifem; Netherlands: Aerodiol, Climara, Dermestril Septem, Estradiol, Estradot, Estreva, Estrofem, Fem 7, Meno-Implant, Progynova, Systen, Vagifem, Zumenon; Poland: Calidiol, Climara, Dermestril, Divigel, Estraderm MX, Estraderm TTS, Estradiol, Estradot, Estrapatch, Estreva, Estrimax, Estrium, Estrofem, Estroplast, Fem 7, Oesclim, Oestradiolum, Progynova, Systen, Vagifem; Portugal: Climara, Dermestril, Epiestrol, Estraderm MX, Estradot, Estrapatch, Estreva, Estrofem, Femsete, Oestrodose, Vagifem, Zumenon; Romania: Climara, Estradot, Estrofem, Oestrogel, Vagifem; Slovakia: Climara, Divigel, Estraderm MX, Estraderm TTS, Estradiol, Estrahexal, Estrapatch, Estreva, Estrimax, Estrofem, Fem 7, Linoladiol N, Oestrogel, Systen, Vagifem; Slovenia: Climara, Estraderm TTS, Estrofem, Vagifem; Spain: Alcis, Dermestril, Esprasone, Estraderm, Estradot, Estroffik, Evopad, Meriestra, Oestraclin, Progynova, Vagifem; Sweden: Climara, Divigel, Estradot, Evorel, Femanest, Femanor, Femasekvens, Vagifem; UK: Climaval, Elleste Solo, Estraderm MX, Estraderm TTS, Estradiol, Estradot, Estring, Evorel, Fematrix, Femseven, Kliovance, Oestrogel, Progynova, Sandrena, Vagifem, Zumenon.
North America
Canada: Climara, Estrace, Estraderm, Estradiol, Estradot, Estring, EstroGel, Oesclim, Vagifem; USA: Alora, Climara, Delestrogen, Depo-Estradiol, Divigel, Elestrin, Estrace, Estraderm, Estradiol, Estrasorb, Estring, EstroGel, Evamist, Femring, Femtrace, Menostar, Vagifem, Vivelle.
Latin America
Argentina: Estrofem, Etrosteron, Eutocol, Evorel, Ginatex, Hormodiol, Lindisc 50, Progynova, Trial Gel, Trial Sat; Brazil: Aerodiol, Avicis, Benzo-Ginestryl AP, Climaderm 7 Días, Estradot, Estreva, Estrofem, Fem 7, Hormodose, Lindisc, Merimono, Natifa, Oestrogel, Primogyna, Riselle, Sandrena, Systen; Mexico: Benzo-Ginestryl, Climaderm, Essventia, Estraderm-Dot, Evorel 25, Evorel 50, Ginedisc, Oestrogel, Primogyn, Sandrena, Systen.
Asia
Japan: Divigel, Estraderm, Estradiol, Julina, L’estrogel.
Drug combinations
Estradiol and Algestona
Estradiol and Cyproterone
Estradiol and Dydrogesterone
Estradiol and Dienogest
Estradiol and Drospirenone
Estradiol and Hydroxyprogesterone
Estradiol and Levonorgestrel
Estradiol and Medroxyprogesterone
Estradiol and Norethindrone
Estradiol and Norgestrel
Estradiol and Prednisolone
Estradiol and Progesterone
Estradiol and Testosterone
Estradiol, Benzyl Benzoate, and Prasterone
Estradiol, Estriol and Levonorgestrel
Chemistry
Estradiol: C~18~H~24~O~2~. Mw: 272.38. Estra-1,3,5(10)-triene-3,17-diol, (17β)-. CAS-50-28-2.
Pharmacologic Category
Estrogens and Estrogen Agonist-Antagonists; Estrogens. Bone Resorption Inhibitors. Estrogen Derivative. (ATC-Code: G03CA03).
Mechanism of action
Estrogens modulate the pituitary secretion of gonadotropins, luteinizing hormone, and follicle-stimulating hormone through a negative feedback system. Estrogen replacement reduces elevated levels of these hormones in postmenopausal women.
Therapeutic use
Treatment of moderate-to-severe vasomotor symptoms associated with menopause. Treatment of vulvar and vaginal atrophy. Hypoestrogenism (due to hypogonadism, castration, or primary ovarian failure). Prostatic cancer (palliation), breast cancer (palliation), osteoporosis (prophylaxis). Abnormal uterine bleeding due to hormonal imbalance. Postmenopausal urogenital symptoms of the lower urinary tract (urinary urgency, dysuria).
Pregnancy and lactiation implications
Estrogens not indicated for use during pregnancy or immediately postpartum. Estrogen has been shown to decrease quantity and quality of human milk; use only if clearly needed.
Unlabeled use
Contraindications
Hypersensitivity to estradiol or any component of the formulation. Abnormal vaginal bleeding. Thrombophlebitis or venous thromboembolic disorders (including DVT, PE). Thromboembolic disease (e.g. stroke, MI). Breast carcinoma. Estrogen-dependent tumor. Hepatic dysfunction or disease. Porphyria. Pregnancy.
Warnings and precautions
Estrogens may increase risk of breast cancer. Estrogen use may lead to severe hypercalcemia in breast cancer and bone metastases. Risk of dementia may be increased in postmenopausal women. Unopposed estrogens may increase the risk of endometrial carcinoma in postmenopausal women with intact uterus. Estrogens may exacerbate endometriosis. Estrogen compounds generally associated with lipid effects such as increased HDL-C and decreased LDL-C. Triglycerides may also be increased (use with caution in familial lipoprotein metabolism defects). Estrogens may cause retinal vascular thrombosis. Estrogens with or without progestin should not be used to prevent coronary heart disease. Use caution with cardiovascular disease or dysfunction. Use caution with history of cholestatic jaundice associated with past estrogen use or pregnancy. Use with caution in diseases which may be exacerbated by fluid retention, including asthma, diabetes, epilepsy, migraine or renal dysfunction, in gallbladder disease, hepatic hemangiomas, severe hypocalcemia, and porphyria (use is contraindicated with certain products). Use with caution in systemic lupus erythematosus. Whenever possible, estrogens should be discontinued at least 4 weeks prior to and for 2 weeks following elective surgery associated with increased risk of thromboembolism or during periods of prolonged immobilization. Absorption of topical emulsion and topical gel is increased by application of sunscreen. Transdermal patch may contain conducting metal (e.g. aluminum). Estrogens with or without progestin should be used for the shortest duration possible at the lowest effective dose consistent with treatment goals. Use caution applying topical products to severely atrophic vaginal mucosa.