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Estradiol
drug data and news
Estradiol drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Estradiol | ||
| Brand Names/Synonyms | ?-ESTRADIOL; Aerodiol; Agofollin; Alora; Altrad; Amnestrogen; Aquadiol; Bardiol; Beta-Estradiol; Cis-Estradiol; Cis-Oestradiol; Climaderm; Climara; 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; 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; Estrovite; Evex; Evorel; Extrasorb; Femestral; Femestrol; Feminone; Femogen; Fempatch; Femring; Femtrace; Femtran; Follicyclin; Ginedisc; Ginosedol; Gynergon; Gynestrel; Gynodiol; Gynoestryl; Gynpolar; Innofem; Lamdiol; Lynoral; Macrodiol; Macrol; Menest; Menorest; Menostar; Microdiol; NSC-9895; Nordicol; Oestergon; Oestradiol; Oestradiol R; Oestrogel; Oestroglandol; Oestrogynal; Ovahormon; Ovasterol; Ovastevol; Ovociclina; Ovocyclin; Ovocycline; Ovocylin; Perlatanol; Primofol; Profoliol; Profoliol B; Progynon; Progynon Dh; Progynon-Dh; Ricifon; Ritsifon; Sandrena Gel; Sisare Gel; Sk-Estrogens; Soldep; Sotipox; Syndiol; Systen; Theelin, Dihydro-; Tradelia; Trial Sat; Trocosone; Vagifem; Vivelle; Zerella; Zumenon; Ô-Estradiol | ||
| Indication | 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). | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Estradiol News (When available) |
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| Dosage Forms | DISC (SUSTAINED-RELEASE); GEL; IMPLANT; LIQUID; PATCH; RING (SLOW-RELEASE); SOLUTION; TABLET | ||
| Drug_Category | Anti-menopausal Agents; Anticholesteremic Agents; Estrogens; ATC:G03CA01; ATC:G03CA03; ATC:L02AA02; ATC:L02AA03 | ||
| Absorption | 43% | ||
| Interactions |
-->Interactions for Estradiol: 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. | ||
| Toxicity | Can cause nausea and vomiting, and withdrawal bleeding may occur in females. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol | ||
| Chemical Formula | C18H24O2 | ||
| Molecular Weight | 272.382 g/mol | ||
| Smiles String | CC12CCC3C(C1CCC2O)CCC4=C3C=CC(=C4)O | ||
| Melting Point | 173-179 °C | ||
| Water Solubility | 3.6 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 3.511 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estrogens are partially metabolized by cytochrome P450. | ||
| Half Life | 36 hours | ||
| Protein Binding [%] | >95% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Estradiol.html http://www.rxlist.com/cgi/generic3/estrogel.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00311 | ||
| CAS Registry Number | 50-28-2 | ||
| KEGG Compound ID | C00951 | ||
| PubChem ID | SID:148536 | ||
| PharmGKB ID | PA449503 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2246969 |
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