indication

Used in the treatment of prostate cancer. Previously used in the prevention of miscarriage or premature delivery in pregnant women prone to miscarriage or premature delivery.

pharmacology

Diethylstilbestrol is a synthetic estrogen that was developed to supplement a woman's natural estrogen production. In 1971, the Food and Drug Administration (FDA) issued a Drug Bulletin advising physicians to stop prescribing DES to pregnant women 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 cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. The effect of Estrogen binding their receptors causes downstream increases 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. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).

toxicity

Symptoms of overdose include nausea and vomiting, and withdrawal bleeding may occur in females.

biotransformation

Hepatic.

drug interactions

Amobarbital: The enzyme inducer, amobarbital, decreases the effect of the hormone agent, diethylstilbestrol.

Aprobarbital: The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, diethylstilbestrol.

Butabarbital: The enzyme inducer, butabarbital, decreases the effect of the hormone agent, diethylstilbestrol.

Butalbital: The enzyme inducer, butalbital, decreases the effect of the hormone agent, diethylstilbestrol.

Butethal: The enzyme inducer, butethal, decreases the effect of the hormone agent, diethylstilbestrol.

Ethotoin: The enzyme inducer, ethotoin, decreases the effect of the hormone agent, diethylstilbestrol.

Fosphenytoin: The enzyme inducer, fosphenytoin, may decrease the therapeutic effect of diethylstilbestrol.

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

Heptabarbital: The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, diethylstilbestrol.

Hexobarbital: The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, diethylstilbestrol.

Mephenytoin: The enzyme inducer, mephenytoin, decreases the effect of the hormone agent, diethylstilbestrol.

Methohexital: The enzyme inducer, methohexital, decreases the effect of the hormone agent, diethylstilbestrol.

Methylphenobarbital: The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, diethylstilbestrol.

Pentobarbital: The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, diethylstilbestrol.

Phenobarbital: The enzyme inducer, phenobarbital, may decrease the therapeutic effect of diethylstilbestrol.

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

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

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

Primidone: The enzyme inducer, primidone, may decrease the effect of the hormone agent, diethylstilbestrol.

Raloxifene: Association not recommended

Secobarbital: The enzyme inducer, secobarbital, decreases the effect of the hormone agent, diethylstilbestrol.

Talbutal: The enzyme inducer, talbutal, decreases the effect of the hormone agent, diethylstilbestrol.

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

Ursodeoxycholic acid: Estrogens decreases the effect of ursodiol