Diethylilstilbestrol (Diethilstilboestrolum, list B ) is a synthetic estrogenic preparation of a nonsteroidal structure. Estrogenic activity is superior to estrone (folliculin). In 1 mg of diethylstilbestrol contains 20,000 units. It is used for ovarian failure due to the same indications as other estrogens (see Folliculin ), and also for prostate and breast cancer. Higher doses of diethylstilbestrol for adults: a single dose of 0.001 g, a daily 0.003 g; intramuscularly in the form of 0.1% oil solution, single 1 ml, daily 3 ml, and malignant tumors to 2 ml 3% solution. Diethylstilbestrol propionate (Diethylstilboestroli propionas) has a longer action; intramuscularly administered 1 ml of 0.1 and 0.5% oil solution 1 time in 2 days. Forms of production of diethylstilbestrol - tablets of 0.001 g and ampoules of 1 ml of 0.1% or 3% solution in oil; diethylstilbestrol-propionate - ampoules of 1 ml of 0.1% or 0.5% solution in oil. Keep in the dark place.
Diethylstilbestrol. Propionate of diethylstilbestrol (Diaethylstilboestrolum Diaethylstilboestrolum dipropionicum). Diethylstilbestrol - 4,4'-dihydroxy-γ-Δ-diethylstilbene. Diethylstilbestrol-dipropionate is its dipropionic ether.
Diethylstilbestrol is a white, fine crystalline powder, easily soluble in alcohol, ether, chloroform, liquid oils, dilute alkali solutions, poorly soluble in water. The melting point is 168-171 °.
Diethylstilbestrol-dipropionate is a crystalline powder. Soluble in alcohol, ether, chloroform, almost insoluble in water. The melting point is 104-107 °.
Preparations are synthetic analogues of folliculin. They differ from it in structure, but are similar to it in terms of biological and therapeutic properties. Twice as high as folliculin and synestrol. In 1 mg diethylstilbestrol contains 20,000 units, diethylstilbestrol more often than synestrol, causes nausea and vomiting.
Pharmacological action . Activates the processes of proliferation of the endometrium, promotes the development of primary and secondary sexual characteristics. A great advantage of the drug is its ability to maintain its healing properties and when applied inside. The action of diethylstilbestrol-propionate is longer than the action of diethylstilbestrol.
Indications . Menopause disorders. Hypogenitalism. Primary and secondary amenorrhea. Starch and gonorrhoid vaginitis. Prostate cancer.
With physiological menopause at the age of 36-58 years, diethylstilbestrol removes or softens dizziness, hot flushes, headaches, insomnia, nervousness, irritability, fatigue, fatigue, depression , impotence.
Similar results are observed when the drug treats menopausal symptoms in women after surgical or roentgenologic intervention on the sex glands.
In the case of atrophic changes in the mucous membranes of female genital organs (senile vaginitis, postoperative menopause, gonorrhagic vaginitis) under the influence of diethylstilbestrol, the vaginal epithelium and the various degrees of endometrial hyperplasia occur. In most cases, the state of the endometrium after treatment with diethylstilbestrol is similar to that of healthy women on the 12-14th day of the menstrual period.The
In infantile girls and in cases of meager and rare monthly diethylstilbestrol normalizes them and promotes the development of genital organs and mammary glands.
Diethylstilbestrol is used after birth to suppress lactation.
The total dose of diethylstilbestrol on the course of treatment should not exceed 25-30 mg when taken orally, and both drugs with intramuscular injection, 15-20 mg.
Treatment should be carried out under close medical supervision. Too large doses of drugs can cause secondary proliferation of the endometrium with abundant bloody discharge, cystic degeneration, liver damage.
In the treatment of prostate cancer, it is necessary to surgically enucleate the testicle parenchyma before surgery, during the first course of treatment, 2 ml of a 3% solution of the drug is injected intramuscularly each day before the appearance of a painful swelling of the mammary glands, but at least a month.
After the disappearance of soreness and a decrease in swelling in the mammary glands proceed to the second course. This is based on the size of the prostate gland, the presence of the patient's metastases and related pain.
The second course consists of daily injections into the muscles for 30-40 days 1 ml of a 3% solution of diethylstilbestrol.
After the second course of treatment, depending on the patient's condition, treatment is stopped or diethylstilbestrol is given in tablets of 10 mg per day.
Ampules of diethylstilbestrol should be heated before use.
Adverse events . Nausea, vomiting, pain in the epigastric region, headaches, itching in the mammary glands, tenderness and swelling of them, loss of appetite, a feeling of squeezing in the stomach.
When these phenomena appear, the dose of the drug is reduced or abolished.
Contraindications . Tumors of the mammary glands and uterus. Tendency to uterine bleeding. Diseases of the liver and kidneys.
|Indications||Diethylstilbestrol in tablets||Diethylstilbestrol in ampoules||Diethyl-stilbestrol dipropionate in ampoules|
|Menopause disorders||0.5-1 mg per day||1 mg after 1-2 days (8-12 injections)||1 mg in 4-6 days|
|Treatment is carried out by courses for 2-3 weeks, in the presence of indications, a second course of treatment is carried out after a 3-4-week break|
|Hypogenitalism, primary amenorrhea||1-2 mg per day||1 mg per day||1 mg per day or every other day; 5 mg every 3-4 days|
|Treatment is carried out 3-4 pedules, after which progesterone is prescribed at 5 mg per day or pregnin at 30 mg per day for 6-8 days|
|Ovarian hypofunction, secondary amenorrhea||1 mg per day||1 mg per day||1 mg every other day|
|Treatment is carried out for 2-3 weeks, after which progesterone is prescribed at 5 mg per day or pregnin at 30 mg per day for 6-8 days|
|Ovarian hypofunction, uterine underdevelopment, hypo-oligomenorrhoea||0.5-1 mg per day||1 mg in 1-2 days||1 mg in 2-3 days|
|Treatment is carried out during the expected phase of proliferation|
|Older vaginitis||0.1-1 mg per day for 1-4 weeks||0.5-2 mg 2-3 times a week for 1-4 weeks|
|Gonorrhoid vaginitis||2 mg per day for 1-3 weeks||Not recommended|
|To suppress lactation||5 mg 1-3 times a day for 2-4 days||5 mg 1-2 times a day for 2-4 days|
|Menopause||1 mg per day for 15-20 days||0.5 mg 2-3 times a week for 15-20 days (course of 8-12 injections)|
Form of issue . Diethylstilbestrol is available in the form of tablets of 1 mg (20,000 units) and in ampoules of 1 mg (20,000 units). Diethylstilbestrol dipropionate is available in ampoules of 1 and 5 mg (20,000 units and 100,000 units, respectively). Both preparations are stored with caution. Belong to the list B. Store in sealed ampoules or in closed glass jars in a dark place protected from light.
Rp. Diaethylstilboestroli 0.001. D. td N. 20 in tabulettis. S. 1 tablet once a day.
Rp. Sol. Diaethylstilboestroli oleosae 0, l% 1.0. D. td N. 5 in ampulis. S. 1 ml per muscle 1 time per day.
Rp, Sol. Diaethylstilboestroli propionici oleosae 0.1% 1.0. D. td N. 5 in ampulis. S. 1 ml per muscle every 2 days.
Rp. Sol Diaethylstilboestroli 3% 1.0. D. td N. 10 in ampulis. S. 1 ml 2 times a day (with prostate cancer).