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Home / Drugs / Starting with E / Estriol 		 
Estriol
  

A hydroxylated metabolite of estradiol or estrone that has a hydroxyl group at C3-beta, 16-alpha, and 17-beta position. Estriol is a major urinary estrogen. During pregnancy, large amount of estriol is produced by the placenta. Isomers with inversion of the hydroxyl group or groups are called epiestriol. Though estriol is used as part of the primarily North American phenomenon of bioidentical hormone replacement therapy, it is not approved for use by the FDA or Health Canada. It is however available in the United States by prescription filled only by compounding pharmacies. It has also been approved and marketed throughout Europe and Asia for approximately 40 years for the treatment of post-menopausal hot flashes.
BrandsTrimesta
CategoriesEstrogens
PackagersJiangxi Yuneng Pharmchem Co. Ltd.
NutriScience Innovations LLC
Synonyms(16α,17β)-estra-1,3,5(10)-triene-3,16,17-triol
16-alpha-Hydroxyestradiol
16alpha-hydroxyestradiol
16α-hydroxyestradiol
Oestriol

indication

Used as a test to determine the general health of an unborn fetus.

pharmacology

Estriol (also oestriol) is one of the three main estrogens produced by the human body. It is only produced in significant amounts during pregnancy as it is made by the placenta. In pregnant women with multiple sclerosis (MS), estriol reduces the disease's symptoms noticeably, according to researchers at UCLA's Geffen Medical School.

mechanism of action

Estriol levels can be measured to give an indication of the general health of the fetus. DHEA-S is produced by the adrenal cortex of the fetus. This is converted to estriol by the placenta. If levels of "unconjugated estriol" are abnormally low in a pregnant woman, this may indicate a problem with the development of the child. The drug 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 estriol 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.

toxicity

ORAL (LD50): Acute: >2000 mg/kg [Rat].

drug interactions

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

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

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

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

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

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

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

Raloxifene: Association not recommended

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