Diethylstilbestrol Usage: Its Interesting Past, Important Present, and Questionable Future

Abstract

Literature on the history metabolism and toxicology and therapeutic use of diethylstilbestrol (DES) is reviewed. DES was first synthesized in the 1930s and showed 5 times the potency of orally administered estradiol. The greater part of administered DES is excreted in the bile as glucurondie though very little is known about its actual metabolism even with the development of sophisticated detection techniques. There have been reports of sever liver toxicity in laboratory animals treated with DES. Reports of severe cardiovascular side effects with DES have become common. There is also evidence that DES may cause symptoms in acute intermittent porphyria. DES has lately been associated with the development of vaginal adenocarc inoma in female offspring of mothers treated with the drug during pregnancy. Hence the Food and Drug Administration has banned its use during pregnancy. Examination protocol for women with possible or definite exposure to DES during fetal life are outlined. DES has been found to have a pronounced effect on the reticuloendothelial system by greatly increasing the rate of phagocytosis of foreign material and to a lesser extent by increasing gamma-globulin. Generally DES affects the same determinations in laboratory tests that all other estrogens do. The therapeutic applications of DES include: 1) the suppression of lactation 2) control of menopausal symptoms 3) control of carcinoma of the breast and prostate 4) postcoital contraception and 5) treatment of severe acne. DES may also have application in the treatment of Duchennes muscular dystrophy.