Diethylstilbestrol-estrogens,progestins and contraceptives and its pharmacology.

DESCRIPTION  :

A  synthetic nonsteroidal estrogen used in the treatment of monopausal and post menopausal disordereds.it was also used formely as a growth promoter in animals.According to the fourth annual report on carcinogen,diethylstilbesterol has been listed as a known carcinogen.This compound belongs to the class of organic compound known as stilbenes .These are organi compound containing a 1,2-diphenylethylene moiety.Stilbenes are derived from the common pheny propene skeleton building block .The introduction of one or more hydroxyl group to a phenyl ring lead to stilbenoids.

CATEGORY  :

            Anti-neoplastic agent

            Carcinogens

PHARMACODYNAMICS :

 It is a synthetic estrogen that was developed to supplement a woman's natural estrogen production. In 1971 ,the food and drug administration issued a drug bulletin advising physician to stop prescribing DES to pregnant woman because it was linked to a rare vaginal cancer in female offspring.

MECHANISM OF ACTION :  

Estrogens diffuse into their target cells and interact with a protein receptor,the estrogen receptor,.Target cell includes the female reproductive tract, the mammary glands ,the hypothalamus and the effect of estrogen binding their receptor causes downstream increase the hepatic synthesis of sex hormone binding globulin ,thyroid binding globulin and other serum protein and suppress follicle ,stimulating hormones from the anterior pituiatory .The combination of an estrogen with a progestin suppress the hypothalmic pituitary system decreasing the secretion of gonadotropin releasing hormone.

PHARMACOKINETIC PROPERTY :

Metabolism :Hepatic

THERAPEUTIC USES :

   In the treatment of -

               prostat cancer

               prevention of miscarries or pre mature delivery

               Hormone replacement therapy

               Delayed puberty ingirls

SIDE EFFECTS :

              Gynacomastia

              Migrane

              Epilepsy

              Endometriosis

DRUG -DRUG INTERACTION :

                        Diethylstilbestrol  + carbidopa  =decrease metabolism of diethylstilbestrol

                        Diethylstilbestrol  + Levodopa  = decrease metabolism of diethylstilbestrol

                        Diethylstilbestrol  + entacapone =decrease the metabolism of diethylstilbasterol

                        Diethylstilbesterol +tolcapone = decrease the metabolism of diethylstilbesterol

REFERENCE:-Tripathi K D"Essential of medical pharmacology",7th edition ,page no. 306, 308, 309.