3. Preparations of sex hormones and their antagonists. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Testosterone esters

Synthetic drugs

Combinations (mixture of testosterone esters)

- testosterone propionate (i / m 1 time in 2 days)

- testosterone enanthate (IM 1 time in 3-4 weeks.)

Produced in oil solutions for intramuscular injection (when taken orally

ineffective because quickly destroyed by the liver). Possess a pronounced androgenic

and anabolic effects.

- methyltestosterone (tablet form)

In terms of activity, it is several times inferior to testosterone, but unlike other androgens

effective when taken orally.

- omnadren

- testenat

- tetrasterone

The combination of testosterone esters with different absorption rates allows

provide a faster and longer (up to 4 weeks) effect with one injection of the drug.

Androgen receptor blockers

2. Inhibitors 5a-reductase

flutamide (niftholide, flulem, flutacan)

bicalutamide (bilumid, kalumid, casodex)

cyproterone acetate (androkur, ciproplex)

block the binding of androgens to specific receptors and prevent the manifestation of their biological effects

finasteride (proscar)

disrupts the restoration of testosterone to dihydrotestosterone, which leads to a decrease in the proliferation of prostate cells, has an antiandrogenic effect selectively only on those tissues whose function is associated with the action of dihydrotestosterone (prostate gland, external genital organs)

Indications for use

- palliative treatment of progressive prostate cancer;

- differential diagnosis of hypogonadism in men.

- severe hirsutism in women.

- benign prostatic hyperplasia.

Side effects

1. In men - gynecomastia, galactorrhea.

2. In women - oppression of ovulation, soreness in the area of ​​the mammary glands.

3. In large doses - impaired liver function, increased blood clotting, fluid retention in the body, osteoporosis.

Contraindications

1. Severe liver disease.

2. Increased blood clotting.

3. Severe forms of diabetes mellitus.

4. Pregnancy, lactation period.

5. Obstructive uropathy (finasteride).

6. Children's age (finasteride).

Ovarian follicular hormones

Semi-synthetic drugs

Synthetic non-steroidal compounds

- estrone (folliculin)

- estradiol esters (benzoate, propionate, valerate)

- estriol

- ethinyl estradiol (microfollin)

- mestranol

- sinestrol (hexestrol)

- sygetin

Mechanism of action:

They stimulate estrogen receptors in target organs (uterus, ovaries, vagina, mammary glands, pituitary gland, hypothalamus), which determines a wide biological spectrum of their effects:

1. Influence the development and functioning of the reproductive system (the growth of the oviducts and the uterus, the proliferation of the endometrium and uterine muscles, the contractile function of the uterus increases).

2. Promote the growth of bone mass, the closure of the epiphyseal growth zones.

3. Prevent the development of atherosclerosis (increase the level of HDL and reduce the content of LDL.

4. Increase blood clotting ability (stimulate the synthesis of fibrinogen and vitamin K-dependent factors of blood clotting in the liver).

5. Retain fluid in the body.

6. They have an anabolic effect on metabolism.

Indications for use

Among women:

• insufficiency of ovarian function (sexual underdevelopment, amenorrhea, dysmenorrhea, post-castration disorders);

• postpartum hemorrhage (to increase blood clotting);

• weakness of labor;

• climacteric disorders;

• breast cancer (over 60 years old);

• to suppress lactation in the postpartum period;

• for the purpose of contraception as part of combination drugs.

In men, prostate cancer.

Side effects:

1. Nausea, vomiting, diarrhea.

2. Dizziness

3. Swelling

4. Uterine bleeding

5. Thromboembolism

6. In men - signs of feminization, decreased libido and sexual potency.

Contraindications:

1. Tumors of the mammary glands.

2. Female genital organs in women under 60 years of age.

3. Endometritis.

4. Pregnancy.

5. Metrorrhagia.

6. Caution is required for liver and kidney diseases.