Physiological effects of hormones and pharmacological effects of their preparations

1. Effect on thermoregulation:

– increased oxygen consumption and heat production by all tissues, with the exception of the brain, genitals and lymphoid tissue.

2. Effect on growth and differentiation of tissues.

3. Effects on metabolic processes:

– in addition to the fact that these hormones promote growth, they also contribute to the synthesis of proteins (anabolic effect);

– in high doses catabolic effect;

– the rate of cholesterol catabolism increases;

– influence on water and electrolyte metabolism

(for example, in hypothyroidism – retention of water and electrolytes).

4. Effect on the cardiovascular system:

– there is a stimulation of the speed and strength of myocardial contractions, increased cardiac output.

5. Effect on the central nervous system:

– increases myelination of nerve fibers.

6. Effect on blood:

– with hypofunction of the thyroid gland anemia develops.

The clinic can meet the state of the hypo – and hyperfunctions of the thyroid gland. Hypothyroidism (hypothyroidism) causes three forms of pathology:

1) myxedema (in adults);

2) cretinism (in children);

3) endemic simple goiter (primary hypothyroidism).

The following drugs are used to treat all three forms of hypothyroidism:

I. TYREOIDIN ( Thyreoidinum; vol. In powders and tablets of 0, 05 and tablets, coated in 0, 1 and 0, 2).

The drug is available, cheap. Powder is obtained from dried, defatted thyroid glands of slaughter cattle. The effect of this drug is due to the presence of two hormones in it : thyroxine and triiodothyronine. Thyroidin is most effective in myxedema, when, thanks to the use of this drug, it has been possible to achieve a good clinical effect for years.

Indications for use:

1. Cretinism (it is desirable that treatment should be started as early as possible, since brain development basically ends by the third year of a person’s life).

2. When treating patients with thyroid cancer before removing the tumor.

3. With great care, the drug is used in patients with atherosclerosis.

Side effects:

– allergic reactions;

– thyrotoxicosis phenomena (in case of overdose): tachycardia, sweating, weakness, worsening of the course of ischemic heart disease, worsening of the course of diabetes, etc.

Ii. TRIYODTIRONINA HYDROCHLORIDE (available in tab. 0, 02 and 0, 05).

This drug is a synthetic agent, corresponding in structure and action to the natural thyroid hormone. The drug is absorbed faster, has a faster effect and acts as a whole quickly, but shortly. Onset of action – after 4-8 hours, the maximum effect develops after 24 hours. The effect of the drug gradually decreases during the week (half- elimination period is two days).

The drug is used for the same indications as thyroidin, but mainly in subacute conditions.

Indications for use:

1. Primary hypothyroidism and myxedema, cretinism (more appropriate is the use of the drug in the first stage of treatment).

2. In partial adenoectomy of the thyroid gland with its hyperfunction.

3. For thyroidin resistance.

4. With myxedema coma and psychosis (most effective).

Side effects are the same as thyroidin.

Iii. LEVOTIROXIN (L-thyroxin) is a synthetic analogue of thyroxin. Available in tablets of 25, 50, 75, 100, 125, 150, 200 micrograms.

It differs from previous preparations in that it is slowly absorbed, slowly excreted, the therapeutic effect is observed after 7-12 days. Prescribe the drug once a day.

The indications and side effects are the same.

Iv. Synthetic combination drugs:

– TYREOKOMB (contains T3, T4 and potassium iodide);

– TYREOT (contains T3 and T4).

In addition, with thyrotoxicosis, beta-blockers ( anaprilin, metaprolol) are used to reduce tachycardia, etc.


In this condition, a clinical picture of diffuse toxic goiter of varying severity develops. Thyrotoxicosis is realized by exophthalmos, tachycardia, sweating, increased metabolism, etc.

In general, there are two groups of antithyroid drugs.

I. A group of drugs used in hyperthyroidism – hormone synthesis inhibitors ( tiamazole, synonym: mercazole).

TIAMAZOL ( Thiamazole ; issue in tab. On 0, 005) – synthetics, easily soluble in alcohol and water. The drug causes a decrease in the synthesis of thyroxin in iron by suppressing the enzyme oxidase. Reduced basal metabolism. The drug accumulates for a long time in the gland, and therefore has a long latent period, and the clinical effect develops in 1-2 weeks, and the maximum effect – within 4-8 weeks. Therefore, the drug is usually prescribed for a long period – an average of one year or more, since it is simply impossible to prescribe a drug for a shorter period.

Side effects :

1. Inhibition of blood formation (leukopenia, anemia, agranulocytosis ).

2. Skin rash (the drug affects nucleic acid metabolism).

3. Lymphadenopathy.

3. The drug penetrates the placenta, causing inhibition of fetal development.

4. Easily penetrates the mother’s breast milk.

5. Goiter (thyroid hyperplasia in response to active synthesis of TSH by the adenohypophysis – implementation of the feedback effect: mercazole causes a decrease in gland hormone synthesis, resulting in an increase inrelease releasing hormones, which leads to an increase in TSH release and, as a result, proliferation thyroid gland.

Ii. The second group of antithyroid drugs used in the treatment of patients with hyperfunction of the thyroid gland is the IODINE PREPARATIONS (iodides ).

This is the oldest group of drugs used to treat patients with thyroid dysfunction. First of all, it should be said about preparations containing elemental iodine. These are Lugol solution (5% iodine solution in 10% potassium iodide solution) and inorganic iodides (potassium and sodium iodides). The idea of ​​prescribing these drugs is that the content of iodine in them significantly exceeds the physiological needs of the body. However, tissue receptors do not react to hormone molecules, but to iodine, which is part of them. At high dosages of iodine, the receptors are deceived, which leads to a decrease in the production of releasing hormones. This, in turn, leads to a decrease in TSH production, iron decreases, its atrophy sets in, its vascularization decreases sharply .

Drugs act quickly, and the effect is manifested after 24 hours from the moment of the start of treatment. The maximum clinical effect is observed in 10-14 days. However, after a certain period of time, the therapeutic effect is significantly reduced. With long-term treatment with these drugs, the patient’s condition may even return to the original or even worse. Thus, these drugs are not suitable for long-term treatment and are used only for one indication – in preparing patients for thyroid surgery, in order to reduce vascularization .

Side effects

– iodism (runny nose, cough, conjunctivitis );

– irritation of the gastric mucosa.


The pituitary gland consists of three lobes – anterior, intermediate, and posterior, each of which is essentially an endocrine gland. The anterior lobe, purely glandular in structure , is called an adenohypophysis . Adenohypophysisconsists of three types of cells:

– the main ( chromophobic ) cells;

– acidophilic cells producing somatotropic hormone and prolactin;

– basophilic cells producing adrenocorticotropic, thyroid-stimulating and gonadotropic (follicle-stimulating and luteinizing ) hormones.

Hormone intermediate pituitary is intermedin or melanocyte-stimulating hormone.

Preparations of the anterior and intermediate lobes of the pituitary gland, as a rule, are obtained from the pituitary glands of cattle and are usually used for the purpose of replacement therapy according to appropriate indications.

Of great importance are preparations of the posterior lobe of the pituitary gland, which is called the neurohypophysis . Two hormones are secreted from the posterior lobe of the pituitary:

1) antidiuretic hormone (vasopressin);

2) oxytocin.

The mechanism of action of antidiuretic hormone is associated both with increased water reabsorption by the walls of the collecting tubules of the kidneys, and with a reduction in vascular smooth muscle, which leads to an increase in blood pressure (meaning large doses).

The second hormone of the neurohypophysis , oxytocin, stimulates the contraction of the smooth muscles of the uterus, especially at the end of pregnancy, and also affects the separation of milk.

Due to the fact that oxytocin is currently used mainly in obstetrics, it seems necessary to know the means that affect the tone of the uterus.


Classification of uterine products

I. Funds stimulating myometrium

A: Means stimulating rhythmic contractions of the uterus

1. Preparations of the oxytocin group:

– oxytocin ( syn .: syntocinone );

– methyloxytocin ;

– sandopart ( demoxytocin );

– pituitrin;

– mammofizin .

2. Preparations of prostaglandins:

– dinoprost ( enaprost F, prostin F2-alpha);

– dinoprostone ( E2 prostin ).

B: Means stimulating tonic contractions of the uterus

1. Ergot preparations:

– methylergometrine ( syn .: metergin , methylergobrevin );

– ergometrine ( syn .: panergal );

– ergotamine ( syn .: ginofort , kornutyamin );

– ergotal.

Ii. Means, relaxing myometrium ( tocolytics )

1. Preparations of beta-2 adrenomimetics:

– partusisten ( syn .: fenoterol);

– Salbupart ( salbutamol );

– ginipral ( hexoprenaline );

– bricanil ( terbutaline );

– pre-steam ( ritodrin ).

2. Preparations of different groups:

– means for anesthesia (ether for anesthesia, etc.)

– myotropic antispasmodics (magnesia sulfate, no-spa, etc.).

By means of stimulating the myometrium , enhancing its rhythmic contractions, are drugs of the oxytocin group.

OXYTOCIN ( Oxytocinum ; vol . 1 ml each (5 U) in amp ., ” Gedeon Richter”, Hungary) – neurohypophysis hormone . Currently received its synthetic counterpart. The sensitivity of the uterus at the beginning of pregnancy to this hormone and its synthetic analogs is very low, however, by the end of pregnancy, this sensitivity rises sharply. In this regard, the hormone is a regulator of labor.

When applied, the main pharmacological effect is an increase in the contraction of the uterine muscles, while the contraction of the myometrium is connected with:

1) with an increase in the amplitude of muscle contraction;

2) with an increase in the frequency of contractions of the uterus.

Thus, the contractions of the uterus continue to remain rhythmic, that is, after the contraction of the myometrium , its complete relaxation occurs. The latter makes it possible to restore the placental blood circulation, which preserves the physiology of the contractile activity of the myometrium .

Oxytocin also increases milk secretion, increasing the production of lactogenic hormone by the anterior pituitary gland.

Oxytocin drug is released as an officinal drug in 1 ml ampoules (5 U in 1 ml). The drug is administered intravenously, previously diluted in 500 ml of isotonic solution, drip at a certain speed.

Indications for use:

1) induction of labor activity (2-5 units to dilute in 500 ml of 5% glucose solution, enter drip );

2) stimulation of labor during prolonged labor, their arrest or inertia of the uterus (the drug is most effective in case of premature discharge of water);

3) to stop hypotonic uterine postpartum bleeding, as in large doses the drug increases the tone of the uterus. In this case, the drug is administered intramuscularly (or subcutaneously), since in this case it has a less dramatic effect;

4) in case of complicated pregnancy (II-III trimester) with the aim of artificially induction of labor (enter 20-30 U units into a vein, intramuscularly or subcutaneously ).

So far, PITUITRIN, an old drug that is a water extract from the hind lobes of the cat hypophysis, has been used. This is not a very good drug, it has uterine, vasopressor and antidiuretic activity (contains oxytocin and vasopressin ).

Pituitrin is used for the same indications as oxytocin, as well as for the normalization of uterine involution in the postpartum, post-abortion periods.

PAHIKARPIN – ganglioblokator , which increases the tone and strengthens the contraction of the muscles of the uterus. This is an old drug, but is still used to enhance labor.

Of the newer means of this group, it is necessary to say about the preparations of prostaglandins (local, tissue hormones). These are short – lived compounds. The most widely used two drugs:

Prostaglandin F2-alpha under the international name DINOPROST ( Di – noprost ; prostin F2-alpha; in Hungary it is produced under the name enzaprost F); Vol. in amp . 4 ml and 8 ml (5 mg of prostaglandin F2-alpha in 1 ml)).The drug has a pronounced stimulating effect on the smooth muscles of the uterus.

Depending on the dosage, dinoprost is used for the following indications:

1) stimulation and stimulation of the contractile action

the presence of the uterus at different periods of pregnancy;

2) causing abortion.

The second drug is DINOPROSTON ( Dinoproston ( syn .: prostin E2; Vol. in tab. on 0, 00005 and in amp . on 0, 75 ml). Prostaglandin preparations are administered intravenously, intraamnally , intravaginally , and also orally.

The principal difference between prostaglandin drugs is that the uterus is sensitive to them at any time during pregnancy. The effectiveness of these drugs (expelled ovum) is very high (about 90%).

Complications while taking prostaglandins (nausea, vomiting, etc.) are found in 90% of cases.

Ergot preparations (ergot is the resting stage of the fungus, parasitizing on rye), stimulating tonic contractions are widely used for the following indications:

1) uterine atony and uterine bleeding associated with it (the hemostatic effect is associated with the contraction of the vessel walls with contractions myometrium );

2) acceleration of the reverse development (involution) of the uterus in the postpartum period;

3) with menstrual bleeding.

The most commonly used drugs are ergot:

1) ERGOTAMIN ( Ergotaminum ; issue in tab. On 0, 001, in amp . 1 ml of 0.05% solution, in vials of 10 ml 0, 1% solution);

2) ergometrine (Ergometrinum;.. No. in the table on 0, 0002, in ampoules to 0, 5 ml and 1 ml 0, 02% solution)..

Ergometrine is one of the main ergot alkaloids. It acts stronger and faster on the muscles of the uterus, increasing its tone and increasing the frequency of contractions.

These drugs, unlike oxytocin, primarily increase the tone of the myometrium . Thus, ergot drugs do not cause rhythmic contractions of the myometrium , pinch the vessels of the uterus.

These drugs are contraindicated to stimulate labor. When using large doses, poisoning is possible (spasms of peripheral vessels, nausea, vomiting, tachycardia, mental disorders, etc.).

A group of tools that relax the muscles of the uterus – TOKOLITIKI. The inhibitory effect on the myometrium has various means. Until recently, there was practically no means of relaxing the myometrium during an excessively stormy labor. There were extreme measures:

1) general anesthesia;

2) the use of ethyl alcohol.

Currently, according to this indication, various means are used, which is associated with the detection of tissue alpha and beta adrenoreceptors in the uterus.

Excitation of alpha- adrenoreceptors leads to uterine contraction (adrenaline, norepinephrine). This explains the occurrence of contractions (labor) in pregnant women during anxiety.

Beta-2-adrenoretseptory are inhibitory, they are in the uterus and bronchi. Stimulation of beta- adrenoreceptors leads to a decrease in myometrial tone . For this purpose, you can use izadrin , however, it is a non-selective betaadrenergic mimetic , therefore it is better to use selective agents: salbutamol , berotek , fenoterol. The berotec used for this indication is known as Partusisten . This drug is effective for threatening preterm labor and does not have an oriental effect on the fetus. The drug is prescribed either intravenously or orally.

Similar in structure and action to beroteka is RITODRIN. Side effects: tachycardia, hand tremor, muscle weakness, low blood pressure, sweating, nausea, vomiting.

DRUGS OF SEXUAL HORMONES (their derivatives, synthetic substitutes and antagonists)


In the ovaries, hormones are produced by follicles (estrogens) and yellow body cells (progestogens).

The main follicular hormone is estradiol, produced during the development of egg cells. Estrone and estriol are formed from estradiol in the body (they can be found in the blood and urine ).

Estrogens ensure the development of sexual organs and secondary sexual characteristics. In addition, under their influence, proliferation of the endometrium occurs in the first half of the menstrual cycle. As a result of ovulation, a corpus luteum is formed, the main hormone of which is progesterone. Progestins contribute to the further proliferation of the mucous membrane of the uterus in the second half of the menstrual cycle, and during fertilization of the egg – the formation of the decidual membrane and placenta. This is a pregnancy hormone.

The production of gonadal hormones by gonadotropic hormones of the anterior pituitary gland is regulated.

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