Demulen: profile and news

Burbs: Feeling flush, companies buy their stock May 28, 2005
...of Pomona said the Food and Drug Administration has approved its application to make and market a generic version of Pfizer's Demulen oral contraceptive. ... - The Journal News.com,

Other information

Indication
For treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive.

Pharmacology
Ethinyl estradiol is a synthetic derivative of the natural estrogen estradiol. It is one of two estrogens currently used in oral contraceptive pills. The other, mestranol, is converted to ethinyl estradiol before it is biologically active. Ethinyl estradiol and norethindrone are used together as an oral contraceptive agent.

Mechanism Of Action
Estrogens diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. 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. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).

Drug Category
Estrogens; ATC:G03CA01

Brand Names/Synonyms
17?-Ethynylestradiol; 17alpha-Ethinylestradiol; 17alpha-Ethynylestradiol; 17alpha-Ethynyloestradiol; Aethinyloestradiolum; Aethinyoestradiol [German]; Alesse; Alora; Amenoron; Amenorone; Anovlar; BRN 2419975; Binovum; Brevicon; Brevinor; CCRIS 286; CHEMBANK1139; Climara; Conceplan; Cyclosa; Demulen; Desogen; Dicromil; Diognat-E; Diogyn E; Diogyn-E; Diprol; Dyloform; EE; EE2; EO; ETHINYLESTRADIOL; Ertonyl; Esclim; Esteed; Estigyn; Estinyl; Eston-E; Estopherol; Estoral; Estoral {[Orion]}; Estorals; Estrace; Estraderm; Estradiol; Estring; Estrogel; Estrogen; Ethidol; Ethinoral; Ethinyl Estradiol; Ethinyl-Oestranol; Ethinylestradiolum [Inn-Latin]; Ethinylestriol; Ethinyloestradiol; Ethy 11; Ethynylestradiol; Ethynyloestradiol; Eticyclin; Eticyclol; Eticylol; Etinestrol; Etinestryl; Etinilestradiol [Inn-Spanish]; Etinilestradiolo [Dcit]; Etinoestryl; Etistradiol; Etivex; Feminone; Fempatch; Follicoral; Genora; Ginestrene; Gynodiol; Gynolett; HSDB 3587; Halodrin; Inestra; Innofem; Jenest; Kolpolyn; Levlen; Linoral; Lo/Ovral; Loestrin; Logynon; Lynoral; Marvelon; Menolyn; Menostar; Mercilon; Microfollin; Microgynon; Mircette; Modicon; NEE; NSC-10973; Necon; Nelova; Neo-Estrone; Neocon; Nogest-S; Norcept; Nordette; Norethin 1/35 E; Norimin; Norinyl; Norlestrin; Novestrol; Oradiol; Orestralyn; Orestrayln; Ortho Tri-Cyclen; Ortho-Cept; Ortho-Cyclen; Ortho-Novum; Ovcon; Ovex; Oviol; Ovral; Ovran; Ovranette; Ovysmen; Palonyl; Perovex; Primogyn; Primogyn C; Primogyn M; Progynon C; Progynon M; Prosexol; Spanestrin; Stediril; Synphase; Tetragynon; Thiuram E; Thiuranide; Tri-Levlen; Tri-Norinyl; Trinordiol; Trinovum; Triphasil; Vagifem; Varnoline; Vivelle; Ylestrol

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

Absorption
Rapid and complete absorption follows oral intake of ethinyl estradiol (bioavailability 43%).

Interactions
Drug Interactions for Ethinyl Estradiol:

Certain endocrine and liver function tests may be affected by estrogen-containing oral contraceptives. The following similar changes may be expected with larger doses of estrogen:

Increased sulfobromophthalein retention; increased prothrombin and factors VII, VIII, IX, and X; decreased antithrombin 3; increased norepinephrine-induced platel et aggregation; increased thyroid binding globulin (TBG) leading to increased circulating total thyroid hormone, as measured by PBI, T₄ by column, or T₄ by radioimmunoassay. Free T₃ resin uptake is decreased, reflecting the elevated TBG; free T₄ concentration is unaltered: impaired glucose tolerance; decreased pregnanediol excretion; reduced response to metyrapone test; reduced serum folate concentration; increased serum triglyceride and phospholipid concentration.

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

Chemical Formula
C20H24O2

Half Life
36 +/- 13 hours

Drug Type
Approved Drug

# Accession No
APRD00691

CAS Registry Number
57-63-6