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Home / Drugs / Starting with E / Estrone
 
Estrone
 

Estrone, one of the major mammalian estrogens, is an aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone. It is produced in vivo from androstenedione or from testosterone via estradiol. It is produced primarily in the ovaries, placenta, and in peripheral tissues (especially adipose tissue) through conversion of adrostenedione. Estrone may be further metabolized to 16-alpha-hydroxyestrone, which may be reduced to estriol by estradiol dehydrogenase.
BrandsAquacrine
Crinovaryl
Cristallovar
Crystogen
Destrone
Disynformon
Endofolliculina
Esterone
Estrin
Estrogenic Substance
Estrol
Estron
Estrona
Estrona [INN-Spanish]
Estrona [Spanish]
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
Glandubolin
Hiestrone
Hormestrin
Hormofollin
Hormovarine
Kestrone
Ketodestrin
Ketohydroxy-Estratriene
Ketohydroxyestrin
Ketohydroxyoestrin
Ketophydroxyestrin
Kolpon
Menagen
Menformon
Menformon A
Mestronaq
Oestrin
Oestroform
Oestrone
Oestrone [Steroidal Oestrogens]
Oestronum
Oestroperos
OVEX
Ovifollin
Penncap M
Perlatan
Sinafid M-48
Solliculin
Theelin
Thelestrin
Thelykinin
Thynestron
Tokokin
Unden
Wynestron
Wynestronpencap M
CategoriesAntineoplastic Agents
Estrogens
Osteoporosis Prophylactic
Anti-menopausal Agents
ManufacturersWyeth ayerst laboratories
Watson laboratories inc
Parkedale pharmaceuticals inc
PackagersCarlisle Laboratories Inc.
Clint Pharmaceutical Inc.
Consolidated Midland Corp.
Gallipot
Martin Surgical Supply
Medisca Inc.
Merit Pharmaceuticals
National Pharmaceuticals
North America Genescience LLC
Primedics Laboratories

indication

For management of perimenopausal and postmenopausal symptoms.

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. The estrogenic potency of estrone is one third that of estradiol. 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 estrogen receptors. Hormone-bound estrogen receptors dimerize, translocate to the nucleus of cells and bind to estrogen response elements (ERE) of genes. Binding to ERE alters the transcription rate of affected genes. 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) release from the anterior pituitary.

toxicity

Symptoms of overdose include nausea and vomiting. Estrogen related side effects include nausea, breast tenderness, fluid retention and edema, headaches and/or migraines, chloasma and poor contact lens fit. Estrogen hormone deficiency is associated with breakthrough bleeding, hypomenorrhea, irritability, depression and menopausal symptoms. Withdrawal bleeds may occur in females.

biotransformation

Hepatic.

absorption

43%

half life

19 hours

drug interactions

Fosphenytoin: The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estrone.

Griseofulvin: The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, estrone.

Phenobarbital: The enzyme inducer, phenobarbital, decreases the effect of the hormone agent, estrone.

Phenytoin: The enzyme inducer, phenytoin, decreases the effect of the hormone agent, estrone.

Prednisolone: The estrogenic agent, estrone, may increase the effect of the corticosteroid, prednisolone.

Prednisone: The estrogenic agent, estrone, may increase the effect of corticosteroid, prednisone.

Primidone: The enzyme inducer, primidone, decreases the effect of the hormone agent, estrone.

Tipranavir: Estropipate may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Estropipate. Monitor for estrogen deficiency during concomitant therapy.