Ticket 13

1. Pharmacological work of domestic physiologists and clinicians (IM Sechenov, IP Pavlov, SP Botkin, NI Pirogov)

2. Anticholinesterase drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. Cholinesterase reactivators. FOS poisoning, assistance measures.

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

4. Antimalarial drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

1. Pharmacological work of domestic physiologists and clinicians (im Sechenov, ip Pavlov, sp Botkin, ni Pirogov)

Sechenov - pharmacology of neurotropic drugs. In 1866, "Reflexes of the head of the brain."

Pavlov - the founder of psychopharmacology, began his activity in the field of pharmacology in the clinic of S.P. Botkin, where he headed the experimental laboratory for 11 years. There, under the leadership of Pavlov, cardiac glycosides, antipyretics, and a number of ions were studied. For the first time in the history of science, Pavlov and his colleagues studied the effect of substances (bromides, caffeine) on higher nervous activity in healthy animals and in experimentally induced neuroses. Pavlov also studied the effects of various substances - acids, alkalis, ethyl alcohol, bitterness - on digestion.

Botkin - studied cardiotropic drugs. In 1860 he founded a clinical experimental laboratory, where the first Russian studies on clinical pharmacology and a therapy experiment were carried out.

Pirogov - research of drugs for anesthesia. The first operation under anesthesia in 1847 on the battlefield.

2. Anticholinesterase drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. Cholinesterase reactivators. FOS poisoning, assistance measures.

Anticholinesterase drugs- indirect cholinomimetics. These substances do not act on cholinergic receptors, but block the enzyme acetylcholinesterase, as a result of which acetylcholine is less destroyed, accumulates and stimulates cholinergic receptors.

Mechanism of action:Anticholinesterase agents inhibit acetylcholinesterase, an enzyme that hydrolyzes acetylcholine in the synaptic cleft and blood plasma cholinesterase (butyrylcholinesterase, pseudocholinesterase, pseudocholinesterase). Inhibition of acetylcholinesterase in cholinergic synapses leads to an increase in the concentration of acetylcholine in the synaptic cleft, as a result of which the action of acetylcholine is significantly enhanced and lengthened. Thus, all the effects of anticholinesterase drugs are due to endogenous acetylcholine.

Classification: Reversible cholinesterase blockers

Tertiary amines: Physostigmine is an alkaloid of Calabar beans. Galantamine (nivalin) is an alkaloid of Voronov's snowdrops tubers.

Amiridine is a synthetic derivative of quinoline (it blocks potassium channels).

Tacrine is a synthetic derivative of acridine.

Quaternary amines:

Neostigmine is a simplified analogue of physostigmine.

Pyridostigmine bromide (Kalimin) is a proserin derivative with a longer lasting effect.

D ystigmina

bromide (ubretide) symmetric bisammonium compounds, according to

Oksazil

Quinotilin activities are superior to proserin.

Irreversible action: Phosphacol, Armin, FOS (phosphorus-organic compounds).

Indications: Glaucoma (increased IOP) using eye drops or ointments

• Atony of the gastrointestinal tract, biliary, urinary tract,

uterus;

• Myasthenia gravis;

• Paresis, paralysis after suffering strokes, brain trauma, neuroinfections, neurosurgical interventions;

• To eliminate the effects of antidepolarizing muscle relaxants;

• Alzheimer's disease (TACRIN, RIVASTIGMINE);

• In case of poisoning with M-anticholinergics, as physiological antagonists.

Side effects: Involuntary twitching of small muscle groups (face, neck, tongue);

Increased irritability, tremors, insomnia;

• Visual impairment in the distance;

• Decreased AV conduction, bradycardia;

• Bronchospasm, bronchorrhea;

• Increased sweating;

• Hypersalivation;

• Spasm of the stomach, intestines, biliary tract;

• Spasms of the urinary tract;

• Strengthening of intestinal motility, diarrhea;

• Increased tone of the uterus;

Contraindications: • Epilepsy

• insomnia

• Heart rate <60 beats per minute, AV blockade

• Myocardial infarction with impaired conduction

• Bronchial asthma

• Peptic ulcer, hyperacid forms of gastritis

• Spasms of the gastrointestinal tract

• Cholelithiasis

• Urolithiasis disease

• Any acute inflammatory processes in the abdominal cavity

• Pregnancy (may cause miscarriage)

Comparative evaluation of drugs: Preparations from the group of tertiary amines are well absorbed from the gastrointestinal tract and penetrate well through the BBB, providing both peripheral and central effects

• Drugs from the group of quaternary amines are less absorbed from the gastrointestinal tract and poorly penetrate the BBB, providing mainly peripheral effects

• FOS do not have an ammonium structure, penetrate well through the BBB

Cholinesterase reactivators: Dipiroxime and isonitrazine. They interact with the residues of FOS associated with acetylcholinesterase, releasing the enzyme and restoring its physiological activity.

FOS poisoning, first aid:

Life-threatening symptoms:

• Severe bradycardia up to cardiac arrest

• Bronchospasm and bronchorrhea, impaired respiratory function

• Convulsions

Specific assistance measures:

• In case of an overdose of reversible drugs, a physiological antagonist is used - the M-anticholinergic antagonist ATROPIN

• In case of an overdose of irreversible drugs (including FOS), use the M-anticholinergic blocker ATROPIN + chemical antagonists (antidotes) - cholinesterase reactivators (DIPYROXIM, IZONITROSIN). Preference is given to ISONITROSINE, because it penetrates well into the central nervous system.