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.