2. Ganglion blocking agents. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of the drug.

Ganglion blockers - These are drugs that selectively block the H-cholinergic receptors in the autonomic ganglia (sympathetic and parasympathetic). In addition, ganglion blockers block the H-cholinergic receptors of the chromaffin cells of the adrenal medulla (reducing the release of catecholamines), as well as the H-cholinergic receptors reflex arousal of respiratory and vasomotor)

Classification: 1. Short-acting: Gigronium (12-20 min.), Arfonad (15-20 min.), Imekhin (4-10 min.); 2. Average duration: Pentamin (1-2 hours), benzohexonium (2-4 hours), Pachikarpin (4-6 hours); 3. Long-term action: Camphonium (6-8 hours), Pyrylene (8-12 hours) - an adverse effect on the central nervous system.

Mechanism of action: Ganglion blockers block sympathetic and parasympathetic ganglia, as well as n-cholinergic receptors of the cells of the adrenal medulla and the carotid glomerulus, they are referred to as antidepolarizing substances.

Pharmacological effects: sedative effect on the central nervous system, dilated pupil, decreased IOP, tachycardia, dilates blood vessels, lowers blood pressure, dilated bronchi, decreased tone of smooth muscles and peristalsis in the gastrointestinal tract, decreased tone of the bladder.

Indications: "Controlled" hypotension, hypertensive crisis, pulmonary and cerebral edema, trophic ulcers, burns, bedsores, open-angle glaucoma, peptic ulcer disease, bronchospasm.

Side effects: 1. Orthostatic collapse; 2.Hypotension; 3.Tachycardia; 4.Reduction of intestinal motility; 5.Photophobia; 6. Atonic constipation.

Contraindications: 1. BP less than 100/60 mm Hg; 2. Atony of the gastrointestinal tract; 3. Atony of the urinary tract; 4. Angle-closure glaucoma; 5.Adenoma of the prostate; 6.Myocardial infarction.

Pyrylene is well absorbed from the gastrointestinal tract, well penetrates the blood-brain barrier, has a stimulating effect on the myometrium. Pentamine - high activity, pronounced selectivity, poorly absorbed in the gastrointestinal tract, so it is advisable to administer it intravenously.

3. Means that reduce the secretion of gastric glands. Classification. Mechanism of action. Indications for use. Side effects. Contraindications. Comparative evaluation of drugs.

Hyperacidity, increased activity of pepsin and lack of mucin predispose to the development of diseases such as gastric ulcer and duodenal ulcer, erosive gastritis, etc. The main tactic of treatment for such a pathology is a decrease in the secretory activity of the gastric glands and an increase in cytoprotective mechanisms.

Classification:

1) M-anticholinergics: non-selective: atropine, platifilin, metacin.

Selective: pirenzepine, telenzepine

Mechanism of action: block the M-cholinergic receptors of the parasympathetic ganglia of the stomach, reduce the secretion of hydrochloric acid and pepsinogen, have a cytoprotective effect on the gastric mucosa.

2) blockers of H2 - histamine receptors; 1st generation: cimetidine; 2nd generation: ranitidine; 3rd generation: famotidine; 4th generation: nizotidine; 5th generation: roxatidine

Mechanism of action: competitively blocks H2 - histamine receptors of parietal cells of the gastric mucosa

3) proton pump inhibitors: omeprazole, pantoprazole, lansoprazole, rabeprazole, esomeprazole.

Mechanism of action: a proton pump is an enzymatic protein located on the apical membrane of the parietal cells that exchanges hydrogen ions for potassium ions, inhibitors suppress HCI secretion, reduce the total volume of gastric juice and inhibit the release of pepsinogen.

4) prostaglandins, their synthetic derivatives and somatostatin: misoprostol

Mechanism of action: they have an antisecretornone effect by inhibiting adenylate cyclase.

5) antagonists of gastrin receptors;

Indications - gastric ulcer and duodenal ulcer, peptic ulcerative esophagitis, hypergastrinemia, reflux esophagitis, duodenitis, erosive gastritis.

1) Blockers of histamine H2-receptors - histamine antagonists, reduce the secretion of hydrochloric acid, pepsinogen. The volume of gastric juice is reduced. They do not penetrate into the central nervous system. Ranitidine - duration 8-12 hours, side effects - headache, rash, diarrhea. Famotidine is more active than ranitidine, it lasts longer.

2) Proton pump inhibitors - omeprazole - selectively acts on parietal cells, reduces the secretion of hydrochloric acid and pepsinogen, reduces the volume of gastric juice, has gastroprotective activity, and has a long-term effect. Side effects - diarrhea, nausea, intestinal colic, headache.

3) Blockers of cholinergic receptors - block the M1-cholinergic receptors of the parasympathetic ganglia of the stomach. Pirenzepine - does not pass through the BBB, reduces the secretion of hydrochloric acid and pepsinogen. Has gastroprotective activity. Reduces the secretion of the salivary glands.

4) Prostaglandins - have an antisecretory effect by inhibiting adenylate cyclase, do not have gastroprotective activity.

Side effects - diarrhea, nausea, swelling, drowsiness, anorexia, flatulence, abdominal pain, allergy, convulsions, candidiasis

Contraindications - pregnancy, breastfeeding, severe renal failure.

4. Antibiotics of the tetracycline and chloramphenicol group. Classification. Mechanism of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation.

Classification: Tetracyclines: natural (tetracycline) and semi-synthetic (doxycycline, morphocycline, metacyclin). Levomycetin belongs to nitrobenzenes.

Mechanism: inhibit protein synthesis.

Mode of action: bacteriostatic.

Spectrum: wide - gram (+) (-), suppresses aerobic and anaerobic bacteria, actinomycetes, legionella, spirochetes, leptospira, mycoplasma, ureaplasma, reketsia, plasmodia; levomycetin has a bacteriostatic effect on streptococci, gonococci, pneumococci, clostridia, anthrax pathogens, diphtheria, plague, whooping cough, salmonella, shigella, brucella.

Indications: rickettsiosis, chlamydial infections, pneumonia, bronchitis, sinusitis, syphilis, leptospirosis, brucellosis, tularemia, cholera, plague, anthrax, typhoid fever, meningitis caused by Haemophilus influenzae.

Side effects: a decrease in hematopoiesis to agranulocytosis, irritate the gastrointestinal tract, teratogenic (tetracyclines), allergies, dysbiosis, candidiasis.

Contraindications: liver, kidney, blood diseases, pregnancy, children under 8 years old.

Doxycycline and metacyclin last longer (up to 12 hours). All are reserve antibiotics (very toxic).

Tetracyclines are very toxic, therefore they are rarely used in children, especially those for 3-5 years. Levomycetin in children under 3 years of age is used to a limited extent, because toxic effects may occur