Dienestrol-estrogen,progestins and contraceptives and its pharmacology

DESCRIPTION 

 It is a synthetic ,non-steroidal estrogen it is a estrogen recepor agonist .Estrogens work partly by increasing a normal discharge from the vagina and making the value and urethra healthy .Using or applying on estrtogen relieves or lessens :dryness and soreness of the  vulva .condition that are treated with vaginal and inflammation of the urethra .The compound belongs to  the class of organic compound containing a 1,2-diphenyethylene moiety .Stilbenes are derived from the common phenylpropene skeleton building block .The introduction of one or more hydroxy groupto a phenyl ring to stilbenoinds.

CATEGORY : 

                 Non-steroidal

                 synthetic estrogen

PHARMACODYNANICS :

  Estrogen diffuse into their target cells and intract with a protein receptor . Target cells and interact a protein receptor . target cells includes  the female reproductive tract ,the mammary gland ,the hipothalamus and the pituitary .Estrogens increases th hepatic synthesis of sex hormone binding  globulin  ,thyroid -binding globulin ,and other serum proteins and suppress follicle -stimulating hormone from the anterior pituitary .the combination  of an estrogen with a progestin suppresses the hypothalmic -pituitary system ,decreasing the secretion of gonadotropin releasing hormone .

MECHANISM OF ACTION  :

 Dienestrol is asynthetic ,non steroidal estrogen .estrogen passively diffuse into target cell of responsive tissues ,complex with the estrogen  receptor and enter the cell nucleus to initiate or enhance gene transcription of protein synthesis after binding to DNA.

PHARMACOKINETIC PROPERTY :

Absorption : estrogen diffuse into their target cells and interact with protein receptor .Target cells include the female reproductive tract ,the mammary gland,the hypothalamus and the pituitary. Estrogen increase the hepatic synthesis of sex hormone binding globulin,thyroid binding globulin The combination of an estrogen with a progestin suppress the hypothalmic pituitary system decreasing the secretion of gonadotropin releasing hormones.

Protein Binding : 50 -80 %

Metabolism - Hepatic

ADVERSE EFFECT :

                        nausea

                        vomiting

                        withdrawal bleeding

THERAPEUTIC USES : 

                 In the treatment of- Atropic vaginitis

                 kraurosis vulvae

DRUG -DRUG INTERACTION :

                Dienestrol  + Carbidopa  = Decrease the metabolism of  dienestrol.

                Dienestrol  + Entacapone = Decrease the metabolism of  dienestrol.

                Dienestrol  + Tolcapone  = Dicrease the metabolism of  dienestrol.

                Dienestrol  + Levodopa  = Decrease the metabolism of dienestrol.

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