Estrone: profile and news

Esterified Estrogen May Be Slightly Safer Than Conjugated Equine ... Mar 1, 2006
Dr. Rozenn N. Lemaitre and colleagues theorized that EE might be safer because it consists primarily of the sulfate esters of estrone and equilin, whereas CEE ... - Medscape (subscription)

(PZ) Manhattan Pharmaceuticals' President and CEO Named Panelist ... Feb 10, 2006
The session will highlight new advances in obesity drugs, including Oleoyl-estrone (OE), Manhattan Pharma's orally administered small molecule in development ... - Houston Chronicle,

Dietary Modification and Risk of Breast Cancer Feb 8, 2006
...findings have been reported for postmenopausal Japanese women 21 ; those with a high-fat intake had higher serum levels of estrone and dehydroepiandrosterone ... - Journal of American Medical Association (subscription),

Other information

Indication
For management of Menopausal and postmenopausal disorders

Pharmacology
Estrone, a synthetically prepared or naturally occurring steroidal estrogen obtained from pregnant equine urine, is the primary circulating estrogen after menopause. Estrone is naturally derived from the peripheral conversion of androstenedione by an aromatase enzyme found in adipose tissues and is converted to estradiol in peripheral tissues. Estropipate is piperazine-stabilized estrone sulfate. Estrone, and estropipate are used to treat abnormalities related to gonadotropin hormone dysfunction, vasomotor symptoms, atrophic vaginitis, and vulvar atrophy associated with menopause, and for the prevention of osteoporosis due to estrogen deficiency.

Mechanism Of Action
Estrogens enter the cells of responsive tissues (e.g., female organs, breasts, hypothalamus, pituitary) where they interact with a protein receptor, estrogen receptors, subsequently increasing the rate of synthesis of DNA, RNA, and some proteins. 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
Antineoplastic Agents; Osteoporosis Prophylactic; Anti-menopausal Agents; Estrogens; ATC:G03CA07; ATC:G03CC04

Brand Names/Synonyms
Aquacrine; CCRIS 285; Crinovaryl; Cristallovar; Crystogen; Destrone; Disynformon; Endofolliculina; Esterone; Estrin; Estrogenic Substance; Estrol; Estron; Estrona; Estrona [Inn-Spanish]; Estrona [Spanish]; Estrone; Estrone [Usan:Inn]; Estrone-A; Estronum [Inn-Latin]; Estrovarin; Estrugenone; Estrusol; Femestrone Inj.; Femestrone Injection; Femidyn; Fermidyn; Folikrin; Folipex; Folisan; Follestrine; Follestrol; Follicular Hormone; Folliculin; Folliculine; Folliculine Benzoate; Follicunodis; Follidrin; GSS 33; Glandubolin; HSDB 3324; Hiestrone; Hormestrin; Hormofollin; Hormovarine; Kestrone; Ketodestrin; Ketohydroxy-Estratriene; Ketohydroxyestrin; Ketohydroxyoestrin; Ketophydroxyestrin; Kolpon; Menagen; Menformon; Menformon A; Mestronaq; NSC 9699; OVEX; Oestrin; Oestroform; Oestrone; Oestrone [Steroidal Oestrogens]; Oestronum; Oestroperos; Ovifollin; Penncap M; Perlatan; Sinafid M-48; Solliculin; Theelin; Thelestrin; Thelykinin; Thynestron; Tokokin; Unden; Wynestron; Wynestronpencap M

Dosage Forms
Vaginal Cream; Vaginal Suppository; Patch; Skin Gel; Tablet; IM Injectable Suspension

Absorption
43%

Interactions
Drug Interactions -------------------------------------------------------------------------------- This medicine may be affected by the drug cholestyramine and should not be taken with any form of estrogen therapy. Talk to your pharmacist for more information. Drugs that may decrease the effects of this medicine include: Rifampin barbiturates phenytoin (Dilantin) carbamazepine (Tegretol) Estrogens may decrease the effects of benzodiazepines (lorezepam oxezepam temezepam). If you are taking these medicines together or you have further questions about drug interactions talk to your doctor or pharmacist. Consult your doctor or pharmacist if you are taking any of the following: seizure medications antibiotics warfarin medications to help you sleep

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

Chemical Formula
C18H22O2

Half Life
19 hours

Drug Type
Approved Drug

# Accession No
APRD00588

CAS Registry Number
53-16-7