Active ingredient: Estradiol - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Anti-menopausal Agents
• Anticholesteremic Agents
• Estrogens

Dosage Forms

• Disc (sustained-release)
• Gel
• Implant
• Liquid
• Patch
• Ring (slow-release)
• Solution
• Tablet

Brands / Synonyms

Activella; Aerodiol; Agofollin; Alora; Altrad; Amnestrogen; Angeliq; Apri; Aquadiol; Bardiol; Beta-Estradiol; Brevicon; Cis-Estradiol; Cis-Oestradiol; Climaderm; Climara; Climara PRO; Climarapro; Combipatch; Compudose; Compudose 200; Compudose 365; Corpagen; D-Estradiol; D-Oestradiol; Delestrogen; Depo-Estradiol; Dermestril; Dihydrofollicular Hormone; Dihydrofolliculin; Dihydromenformon; Dihydrotheelin; Dihydroxyesterin; Dihydroxyestrin; Dihydroxyoestrin; Dimenformon; Dimenformon Prolongatum; Diogyn; Diogynets; Divigel; Encore; Esclim; Estinyl; Estrace; Estraderm; Estraderm Tts; Estradiol Cypionate; Estradiol Valerate; Estradiol-17beta; Estradurin; Estraldine; Estrasorb; Estreva; Estrifam; Estring; Estring Vaginal Ring; Estroclim; Estroclim 50; Estrofem 2; Estrofem Forte; Estrogel; Estrogens, Esterified; Estrol; Estrostep FE; Estrovite; Evex; Evorel; Extrasorb; Femestral; Femestrol; Feminone; Femogen; Fempatch; Femring; Femtrace; Femtran; Follicyclin; Ginedisc; Ginosedol; Gynergon; Gynestrel; Gynodiol; Gynoestryl; Gynpolar; Innofem; Junel; Kelnor 1 / 35; Lamdiol; Levora; LOW-Ogestrel; Lunelle; Lynoral; Macrodiol; Macrol; Menest; Menorest; Menostar; Microdiol; Nordette; Nordicol; Nortrel 7 / 7 / 7; Oestergon; Oestradiol; Oestradiol R; Oestrogel; Oestroglandol; Oestrogynal; Ortho Evra; Ovahormon; Ovasterol; Ovastevol; Ovcon; Ovociclina; Ovocyclin; Ovocycline; Ovocylin; Perlatanol; Prefest; Primofol; Profoliol; Profoliol B; Progynon; Progynon Dh; Progynon-Dh; Reclipsen; Ricifon; Ritsifon; Sandrena Gel; Seasonique; Sisare Gel; Sk-Estrogens; Soldep; Sotipox; Syndiol; Systen; Theelin, Dihydro-; Tradelia; TRI-Norinyl; Trial Sat; Trivora; Trocosone; Vagifem; Vivelle; Vivelle-DOT; Zerella; Zovia; Zumenon

Indications

For the treatment of urogenital symptoms associated with post-menopausal atrophy of the vagina (such as dryness, burning, pruritus and dyspareunia) and/or the lower urinary tract (urinary urgency and dysuria).

Pharmacology

Estradiol, the principal intracellular human estrogen, is substantially more active than its metabolites, estrone and estriol, at the cellular level.

Mechanism of Action

Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.

Absorption

43%

Toxicity

Can cause nausea and vomiting, and withdrawal bleeding may occur in females.

Biotrnasformation / Drug Metabolism

Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estrogens are partially metabolized by cytochrome P450.

Contraindications

Estrogens should not be used in individuals with any of the following conditions:

1. Undiagnosed abnormal genital bleeding.

2. Known, suspected, or history of cancer of the breast.

3. Known or suspected estrogen-dependent neoplasia

4. Active deep vein thrombosis, pulmonary embolism, or history of these conditions.

5. Active or recent (e.g., within the past year) arterial thromboembolic disease (e.g., stroke, myocardial infarction).

6. Liver dysfunction or disease.

7. EstroGel therapy should not be used in patients with known hypersensitivity to its ingredients.

8. Known or suspected pregnancy. There is no indication for EstroGel in pregnancy. There appears to be little or no increased risk of birth defects in children born to women who have used estrogens and progestins from oral contraceptives inadvertently during early pregnancy.

Drug Interactions

D. Drug and Laboratory Test Interactions

1. Accelerated prothrombin time, partial thromboplastin time, and platelet aggregation time; increased platelet count; increased factors II, VII antigen, VIII antigen, VIII coagulant activity, IX, X, XII, VII-X complex, II-VII-X complex, and beta-thromboglobulin; decreased levels of anti-factor Xa and antithrombin III, decreased antithrombin III activity; increased levels of fibrinogen and fibrinogen activity; increased plasminogen antigen and activity.

2. Increased thyroid-binding globulin (TBG) leading to increased circulating total thyroid hormone levels, as measured by protein-bound iodine (PBI), T₄ levels (by column or by radioimmunoassay) or T₃ levels by radioimmunoassay. T₃ resin uptake is decreased, reflecting the elevated TBG. Free T₄ and T₃ concentrations are unaltered. Patients on thyroid replacement therapy may require higher doses of thyroid hormone.

3. Other binding proteins may be elevated in serum, i.e., corticosteroid binding globulin (CBG), sex hormone-binding globulin (SHBG), leading to increased total circulating corticosteroids and sex steroids, respectively. Free hormone concentrations may be decreased. Other plasma proteins may be increased (angiotensinogen/renin substrate, alpha-1-antitrypsin, ceruloplasmin).

4. Increased plasma HDL and HDL₂ cholesterol subfraction concentrations, reduced LDL cholesterol concentration, increased triglyceride levels.

5. Impaired glucose tolerance.

6. Reduced response to metyrapone test.