3. Antihypertensive drugs of peripheral neurotropic action. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

Classification:

ganglion blockers (benzohexonium, pentamine, arfonade, hygronium);

sympatholytics (octadine, reserpine);

α-blockers (phentolamine, tropafen, prazosin);

β-blockers (anaprilin, talinolol, metoprolol, atenolol);

α-β-blockers (labetalol).

Ganglion blockers- effects: ↓ VD, return of blood to the heart. For the treatment of hypertension, they are rarely used, because have many side effects (block both sympathetic and parasympathetic ganglia) - orthostatic collapse, constipation, intestinal obstruction, ↓ bladder tone, impaired accommodation, dry mouth, addiction. It is used for controlled hypotension during operations, with pulmonary and cerebral edema.

Sympatholytics (octadine)- mechanism: ↓ transport to oxoplasm and granule, ↓ release of norepinephrine from the depot (the depot is depleted). When administered intravenously, the action is in 2 phases: ↑ BP, then ↓ BP due to depot depletion (2-3 days). Effects: ↑ vein tone, ↓ strength and heart rate, does not pass through the blood-brain barrier. Side effects: orthostatic collapse, drowsiness, weakness, varicose veins in the extremities, diarrhea. Aid measures: atropine, bandaging of limbs, inject lying down. Octadine is more effective than reserpine.

Adrenoblockers:phentolamine - vasodilation, ↓ blood pressure, especially diastolic. (orthostatic collapse). With hypertensive crises. Quickly addictive. Side effects: tachycardia, nausea, diarrhea.

Anaprilin - mechanism ↓ blood pressure, ↓ release of renin by juxtaglomerular kidney cells, ↑ activity of the paraventricular depressor nucleus of the hypothalamus, excite α-receptors of the medulla oblongata. Gradual ↓ BP, maximum for 2-3 weeks. ↓ strength and heart rate. Side effects: narrowing of the bronchi. Used for hypertension.

Labetalol - ↓ TPR and BP, does not affect cardiac output, ↓ HR and renin production.

Prescribed for hypertension. Side effects: dizziness, orthostatic collapse. Prazosin - acts postsynaptically, there is no tachycardia, ↓ BP and OPSS, does not affect renin. The action develops after 4 hours and lasts 10 hours. With hypertension. Side effects: headache, palpitations, drowsiness, edema, orthostatic collapse.

4. Anti-tuberculosis drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Anti-tuberculosis drugs - Chemotherapeutic substances that suppress the vital activity and growth of acid-resistant mycobacteria - the causative agents of tuberculosis.

Classification

I SERIES (basic drugs)	II ROW (reserve drugs)
Isonicotinic acid hydrazide derivatives 1. Isoniazid 2. Ftivazid 3. Opiniazide (Saluside) 4. Saluside soluble 5. Metazid	Antibiotics and fluoroquinolones 16. Cycloserine 17. Viomycin (Florimycin sulfate) 18. Capreomycin sulfate (Capastat) 19. Lomefloxacin (Maksavin)
Derivatives of para-aminosalicylic acid 6. PASK (Aminacil) 7. Calcium benzamidosalicylate (Bepask) Antibiotics 8. Rifampicin (Rifadin) 9. Rifabutin 10. Streptomycin sulfate 11. Kanamycin 12. Streptosaluside 13. Pasomycin	Preparations of different chemical groups 20. Ethambutol (Kombutol) 21. Pyrazinamide (Pizina) 22. Thioacetazone (Tibon)
Isonicotinic acid thioamide derivatives 14. Ethionamide 15. Prothionamide

Group 1 (A) - the most effective drugs (isoniazid and rifampicin);

Group II (B) - drugs of average efficiency [streptomycin sulfate, prothionamide, ethionamide, ethambutol, pyrazinamide, kanamycin sulfate, cycloserine, florimycin sulfate (viomycin)];

Group III (C) - drugs of the lowest efficiency [PASK-sodium, thioacetazone (tibon)].

Mechanism of action: Synthetic anti-tuberculosis drugs (most effective): the mechanism of their anti-tuberculosis action is not completely clear, but there are several points of view:

1. Derivatives of GINK bind important biochemical substances containing a carbonyl group (pyruvic acid, acetaldehyde, pyridoxal, etc.).

2. They inhibit the activity of microbial cell enzymes (catalase, transaminase, amino oxidase, etc.). The inhibition of enzyme activity comes from bacteriostatic concentrations. This is the leading point of view.

3. They are able to form complexes with substances containing metals, and metals are most often constituents of enzymes.

Synthetic anti-tuberculosis drugs of different chemical structure: It has a bacteriostatic effect, equally affecting the intra- and extracellular Mycobacterium tuberculosis. Acts mainly on multiplying mycobacteria. Drug resistance can develop very quickly during treatment.

Indications: Prevention and treatment of active tuberculosis of any localization - isoniazid;

Streptomycin is most effective in the treatment of newly diagnosed and especially fresh cases of tuberculosis;

Kanamycin sulfate is used to treat tuberculosis of the lungs and other organs with resistance to anti-tuberculosis drugs of the 1st and 2nd row (except for florimycin).

Contraindications: Kanamycin is contraindicated in inflammation of the auditory nerve, impaired liver and kidney function (with the exception of tuberculous lesions).

Individual intolerance to the drug.

Epilepsy.

Severe psychosis.

Tendency to seizures.

History of poliomyelitis.

History of toxic hepatitis due to taking GINK drugs.

Acute hepatic and renal failure.

An absolute contraindication to the appointment of streptomycin is the lack of sensitivity of Koch's bacilli to it.

Side effect:Dizziness, discomfort in the region of the heart, tinnitus, headache (often due to a decrease in blood pressure, mainly systolic). Anaphylactic shock, vestibular disorders, hearing loss, deafness, drug fever, skin rash, contact dermatitis, muscle weakness and joint pain, dizziness, tinnitus, palpitations and pain in the region of the heart. In severe cases, paresthesias, insomnia, memory loss, muscle twitching, polyneuritis, ataxia, convulsions occur (due to the developing deficiency of pyridoxine and thiamine chloride). Changes in blood are possible: agranulocytosis, eosinophilia. Convulsive states, lesions of the optic nerve and polyneuritis are also possible. Endocrine system disorders: gynecomastia in men, dysmenorrhea in women, "cushingoid", hyperglycemia.