Season 6

1. Formation and development of the Department of Pharmacology of the Kuban State Medical University (P.P. Avrorov, I.E. Akopov, A.I. Ostroumov, etc.)

The department was founded in 1922. The first head was Professor P.P. Aurov is an outstanding scientist, widely known for his works on the study of the effect on the body of complete starvation, alcohol, as well as on the cultivation of tissues outside the body. P.P. Avrorov pays much attention to the pharmacodynamic study of the Psekup mineral springs in the town of Goryachy Klyuch and others. He carried out a lot of work to improve the methods of experimental research. He organized the Department of Experimental Hygiene, which he headed for 8 years.

After the death of P.P. Avrorov since 1940, the department was headed by Associate Professor Ya.L. Levin. He proposed a number of improvements in pharmaceutical research methods.

Since 1958, the department was headed by Professor Ivan Emmanuilovich Akopov. During this period, the main scientific problem of the department was "Pharmacology of the process of blood coagulation and hemostasis".

The result of his research is the introduction into medicine of drugs intoxicating logachilus. Under the leadership of I.E. Akopov in the Kuban, the organization of an allergological service to combat ragweed polynosis began.

Since 1974, the department has been headed by Professor Arkady Ivanovich Ostroumov. The main problem of the department is pharmacotherapy of allergic diseases and the study of the pharmacology of blood coagulation and hemostasis.

In 1980 - 1981 the head was Professor Vera Mikhailovna Yadrova. Work was carried out on the topic "Pharmacology of blood coagulation and hemostasis".

In 1981, Professor Pavel Aleksandrovich Galenko-Yaroshevsky was elected to the post of head. The staff of the department is developing a scientific direction for the creation of neuro-, cardio- and dermatotropic drugs. The drugs sufan, rihlokain and baliz-2 have been created (in co-authorship) and introduced into practice.

In 1995 P.A. Galenko-Yaroshevsky was elected a corresponding member of the Russian Academy of Sciences (RAS), and in 1996 - an academician of a number of foreign academies.

47. Beta-blockers. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Classification:

1. Cardioselective (acting mainly on _one-receptors of the heart)

1. with SMA:

-acebutolol, praktolol, celiprolol

2. without MCA:

-metoprolol, talinolol, atenolol, bisoprolol, nebivolol

2. Noncardioselective (acting equally as on _oneand on ₂-receptors)

1. with SMA:

-pindolol, oxprenolol, alprenolol, bopindolol

2. without MCA:

–Anaprilin, timolol, sotalol, nadolol

Mechanism of action:

• a heart: blockade of beta1 receptors leads to a decrease in heart rate, contractility, excitability, conductivity, automatism, stroke and minute blood volumes, a slowdown in metabolic processes in the myocardium and a decrease in its oxygen demand, which is important in terms of treating coronary heart disease. Coronary vessels are somewhat narrowed, mainly reflexively, due to a decrease in the work of the heart and to a small extent due to blockade₂-receptors of these vessels.

• Vessels: by blocking beta2 receptors of JGA cells, the drugs reduce the secretion of renin and this leads to a decrease in systemic vascular resistance at the beginning of treatment, which, with an initially increased tone of arterioles, sometimes even cause peripheral circulatory disorders. With a long course appointment-blockers (on average after a month) OPSS returns to the initial one and even decreases. This is due to the entry into force of the "antirenine mechanism". Nebivolol immediately reduces OPSS, since it dilates blood vessels, stimulating the production of NO in the endothelium.

• Arterial pressure: Decreases, especially with prolonged course use. The leading mechanism of the hypotensive effect is a decrease in cardiac output, i.e. decrease in blood pressure is mainly due to the systolic fraction. In this case, the OPSS at the beginning of treatment increases. Another mechanism, realized on average after a month of treatment, is the suppression of renin secretion, especially in patients with its initial hypersecretion.

• Bronchi: the tone is increased due to the blockade of beta2 receptors.This is a side effect that limits the use of non-selective drugs in patients with broncho-obstructive diseases. The least dangerous are the most highly selective (nebivolol, bisprolol and betaxolol).

• Eye: decrease in IOP by reducing the production of intraocular fluid

• uterus: increased tone. The use of β-blockers during pregnancy can cause intrauterine fetal hypoxia and even miscarriage

• blood: -blockers inhibit an increase in fibrinolytic activity and an increase in platelet aggregation under stress loads

Indications: Ischemic heart disease, hypertension, tachyarrhythmia, hyperthyroidism, open-angle glaucoma

Side effects: bronchospasm, weakening of heart contractions, decreased heart rate, impaired AV conduction, withdrawal syndrome, hypo- or hyperglycemia, weakness, lethargy, decreased potency, impaired peripheral circulation.

Contraindications: broncho-obstructive diseases, sinus bradycardia (<50 / min), hypotension, atherosclerosis, diabetes mellitus and hypoglycemic conditions, pregnancy, congestive circulatory failure, peripheral circulatory disorders (Raynaud's disease, obliterating endarteritis)

Anaprilin - reduces heart rate and strength of heart contractions, increases bronchial tone, can provoke bronchospasm. Blocks the metabolic effects of catecholamines.

Oxprenolol - rarely causes bronchospasm.

Metoprolol - affects mainly the beta1-adrenergic receptors of the heart, is used orally for arterial hypertension.

Talinolol - does not affect the bronchi, does not cause orthostatic collapse.

88. Inhibitors of fibrinolysis. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Fibrinolysis inhibitors - these are synthetic substances and substances of animal origin with antienzyme activity that reduce the fibrinolytic activity of blood and tissues.

Classification:

1.synthetic: aminocaproic acid, tranexamic acid, aminomethylbenzoic acid.

2.animal origin: APROTININ (high molecular weight polypeptides secreted from various tissues and slaughter cattle: from the pancreas (gorodoks), parotid glands (trasilol), lungs (contrikal); aprotinin is the general name of drugs).