The basic meaning of diethylstilbestrol

Diethylstilbestrol (stilbestrol) is a synthetic non-steroidal estrogenic substances, can produce all the same with the natural estradiol pharmacological and therapeutic effects. Mainly used for estrogen and hormone balance disorders caused by functional bleeding, amenorrhea, can also be used for stillbirth before induction of labor, in order to improve myometrial sensitivity to oxytocin.

(1) for the Qi derivatives of a group of synthetic estrogen hormone substances in general. The efficiency is very strong, and steroidal substances different, almost insoluble in water, in order not to be damaged by the liver, by oral, diethylstilbestrol, hexestrol, hexestrol, estrone, etc. has been widely used clinically .

(2) diethyl diethylstilbestrol for short.

(3) i.e. 3,4-bis (p-hydroxyphenol) -3-hexene. Can be a single female estrone. Abbreviated as DES, is not a steroid skeleton synthesis of female hormones one. And estrogen-17β can be the same significant estrogen effect. Because oral effective, so in addition to estrogen therapy, but also for the treatment of benign prostatic hyperplasia.

Drug preparation of diethylstilbestrol

Phenol as the starting material, polyphosphoric acid (PPA) as the catalyst, and n-propionic acid by Firedd, C- Crafts.JM reaction of a hydroxy acetophenone, and then acetic anhydride reaction, phenolic hydroxyl esterification protection, Then in tetrahydrofuran solution with TiCl4 / Zn reduction of a coupling, and then hydrolysis of potassium hydroxide, the removal of acetate, the final acidification by hydrochloric acid, derived products.

Contraindication of diethylstilbestrol

1, during pregnancy do not use estrogen, systemic medication may lead to fetal malformations, vaginal medication should also be noted. After administration of female fetuses can occur reproductive tract abnormalities, adolescent suffering from vaginal adenosis, rare cases in the reproductive age of vaginal cancer or cervical cancer; male fetuses feminine, testicular dysplasia. Estrogen can enter the milk through the breast and discharge, and inhibition of lactation, breast-feeding women disabled.

2, the following conditions should be banned: 1). known or suspected of having breast cancer, as the treatment of advanced metastatic breast cancer exception; 2). known or suspected of suffering from estrogen-dependent tumors; 3). acute thrombophlebitis or thromboembolism ; 4). the use of estrogen in the past, had associated with thrombophlebitis or thromboembolism, for the treatment of advanced breast cancer and prostate cancer exception; 5). cholestatic jaundiced iethylstilbestrol standard history of veterinary drugs; 6). not a clear diagnosis of irregular vaginal bleeding.

3, the following conditions should be used with caution in estrogen: 1). asthma; 2). cardiac insufficiency; 3). epilepsy; 4). depression: 5). migraine; 6). renal insufficiency, estrogen can increase water retention; 7). diabetes; 8). benign breast disease ; 9). cerebrovascular disease; 10). coronary artery disease; 11). endometriosis; 12). gallbladder disease or gallbladder history, especially gallstones; 13). liver dysfunction; 14). hypercalcemia, associated with tumor or metabolic bone 15). the history of jaundice or jaundice during pregnancy, estrogen to promote the risk of liver damage recurrence; 16). acute, intermittent or complex liver glucosidase; 17). renal dysfunction; 18). thyroid disorders; 19). uterus Fibroids. Liver and kidney disease patients and pregnant women disabled.

Drug interactions of diethylstilbestrol

1, Anticoagulant with the use of estrogen can reduce the anticoagulant effect, must be used with the time, should adjust the anticoagulant dosage. The combination of carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, etc., can reduce the estrogen effect, which is due to induction of liver microsomal enzymes, increased estrogen metabolism.

2, Tricyclic antidepressants used at the same time, a large number of estrogen can enhance the adverse effects of antidepressants, while reducing its due effect. And antihypertensive drugs at the same time, can reduce the role of antihypertensive. Reduce the therapeutic effect of tamoxifen. Increase the absorption of calcium.

Environmental hazards of diethylstilbestrol

Diethylstilbestrol sodium diethylstilbestrol in the seventies and eighties as an estrogen-like drugs are widely used in oral contraception, and to prevent abortion. It can promote the normal development of female sexual organs and secondary sexual characteristics, endometrial hyperplasia and vaginal epithelial hyperkeratosis, reduce women after menopause or gynecological surgery due to gonadal insufficiency caused by endocrine disorders, increased uterine contraction, increased uterine oxytocin Of the sensitivity.

Like the notorious thalidomide (thalidomide), diethylstilbestrol has received a lot of popularity since it first appeared. Many people do not have to worry about the birth of a child, and the child can not be born. However, just as thalidomide, when people did not realize its dangers.

Until a large number of use of diethylstilbestrol that generation of female children after birth, the problem occurred, and more concentrated in their puberty after the serious performance:

Taking diethylstilbestrol in the life of the girl, the vagina and cervical cells have varying degrees of disease. Studies have shown that vaginal clear cell adenocarcinoma in recent years, girls and young women in the incidence of an increasing trend. According to the survey, these patients were born before the impact of diethylstilbestrol. Fetal exposure to diethylstilbestrol in women, age to 24 years of age the cumulative risk of this disease is 0.14% to 1.4%. There are a lot of people have benign cervical and vaginal tissue changes, known as adenomatosis. By fetal exposure to diethylstilbestrol in the routine examination of women found that about 1/3 of these abnormalities.

In infants exposed to diethylstilbestrol, the incidence of abnormal reproductive system is also high, 4.33% of testicular abnormalities, 3% of testicular hypoplasia, 2.1% of cryptorchid history, 1.1% of testicular induration. These patients had a significantly increased incidence of testicular abnormalities compared with those of the same age group who had not been exposed to diethylstilbestrol during the fetal period. The patient's semen examination showed decreased sperm count and decreased sperm motility, indicating that the patient's fertility damage may be the application of diethylstilbestrol after treatment of another consequence.

These cases, we call it "DES syndrome."

At the same time, during pregnancy, diethylstilbestrol can also cause fetal malformations, so that women masculine, feminine male, hypospadias, epididymis, testicular and sperm abnormalities, and even cause hydrocephalus, meningoencephalic and so on. At the same time, pregnant women may also cause liver and kidney damage, the incidence of asthma increased significantly, but also may lead to the formation of bile cholesterol saturation stones, induced pancreatitis and thromboembolic disease.

At this time it was discovered that diethylstilbestrol is an environmental hormone, and estrogen receptor binding will interfere with the human endocrine, induced genital lesions and tumors.

However, as in the history of many "drug accident", want to make up, it is too late.