Femring: profile and news

Breast Cancer: Topical Estrogen Risky Jan 26, 2006
...estrogen. Commonly used vaginal estrogen products include Estrace and Premarin creams, and Estring and Femring vaginal rings. "We ... - WebMD

Hormones given through the skin are worth a look 11 Dec 2005
...are also FDA-approved vaginal rings that deliver estradiol, one called Estring which only combats vaginal dryness; and another called Femring, which addresses ... - Boston Globe,

Galen Holdings PLC closes purchase of SarafemÂ® rights from Lilly Oct 3, 2005
...that there is opportunity for significant future growth of SarafemÂ®, complementing our pipeline of products developed in-house, such as FemringÂ®, which will ... - Biotechnology Investment Today (Press Release),

FDA Safety Labeling Changes: Crestor, Diamox Sequels, Femring Jun 8, 2005
On March 11, the FDA approved revisions to the safety labeling for an estradiol acetate vaginal ring (Femring, made by Galen Chemicals Inc.) to warn of the ... - Medscape (subscription)

Other information

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).

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.

Drug Category
Anti-menopausal Agents; Anticholesteremic Agents; Estrogens; ATC:G03CA01; ATC:G03CA03; ATC:L02AA02; ATC:L02AA03

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

Dosage Forms
DISC (SUSTAINED-RELEASE); GEL; IMPLANT; LIQUID; PATCH; RING (SLOW-RELEASE); SOLUTION; TABLET

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.

Chemical IUPAC Name
13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol

Chemical Formula
C18H24O2

Half Life
36 hours

Drug Type
Approved Drug

# Accession No
APRD00311

CAS Registry Number
50-28-2