This PPT covers drug therapy for tuberculosis. It includes classification of antitubercular drugs. First line agents like Rifampin/Rifampicin Isoniazide Pyrazinamide Ethambutol Streptomycin Second line agents Para amino-salicyclic acid Kanamycine Cycloserine Ethidnamide

1. Antitubercular Agents
Pyrizinamide
Para Amino salicylic acid
Presented By: Priyanka N.Deshmukh
M.Pharm(Q.A)

2. 1. Tuberculosis(TB): Infectious disease caused by Mycobacterium
tuberculosis.
2. Site of primary infections- lungs
3. Anti-tubercular agents: The agents which are used in the treatment or
prophylaxis of tuberculosis.

3. First line agents
More effective
Less toxic
 Rifampin/Rifampicin
 Isoniazide
 Pyrazinamide
 Ethambutol
 Streptomycin
Second line agents
Less effective
More toxic
 Para amino-salicyclic acid
 Kanamycine
 Cycloserine
 Ethidnamide

4. Isoniazid (INH)
 INH- Isonicotinic acid hydrazide.
 Used for treatment of tuberculosis.
 Used in combination with rifampicin, pyrazinamide, and either sterptomycin
or ethambutol.
 MOA: Inhibits the formation of the mycobacterial cell wall by inhibition of
biosynthesis of mycolic acids.
Chemical Name: Pyridine-4- carbohydrazide
Pyridine
CONHNH2
Pyridine-4- carbohydrazide

5. Physical Properties:
1. Colourless crystals or white crystalline powder.
2. Odourless.
3. Has sweet taste followed by bitter taste.
4. It is soluble in water.
Chemical Properties:
Isoniazid treated with bromine water in the presence of HCl, formation of iso
nicotinic acid with the liberation of N2 gas.
CONHNH2
+ 2Br2 H2O + N2 + 4HBr
+
Isoniazid Isonicotinic acid

6.  Stability and storage:
Stored in tightly- closed, light- resistant containers.
 Pharmaceutical preparation:
1. Isoniazid elixir
2. Isoniazid Tablets I.P
3. Isoniazid And ethambutol Tablets
4. Isoniazid And rifampicin Tablets
5. Isoniazid Injection
 Uses:
1. In pulmonary tuberculosis.
2. In extra pulmonary tuberculosis.
3. In lupus valgaris(Tuberculosis of skin).
Dose: 5mg/kg
Brand Name:
1. Isonex
2. Rimpazid
3. Cadizide

7. Ethambutol
Chemical Name: Ethylene diamino-di-1-butanol
Physical Properties
1. White crystalline powder
2. Odourless
3. Freely soluble in water
4. More effective in combination with isoniazid Or rifampicin.

8. Storage:
Stored in tightly- closed containers.
Uses:
1. Bacteriostatic agents and
2. Treatment of TB
 Pharmaceutical preparation:
1. Ethambutol powder
2. Ethambutol Tablets
3. Isoniazid and ethambutol tablets
Dose: 15 mg/kg
Brand Name:
1. Albutol
2. Myambutol
3. Ly- butol
MOA:
Inhibition of arabinosyl transferase an enzyme that required for
arabinogalactan a Mycobacterial cell wall constituent.

9. Pyrazinamide
Chemical Name: Pyrazine-2-carboxamide
Physical Properties
1. White crystalline powder
2. Odourless
3. Sparingly soluble in water
4. Has bitter taste.
5. Soluble in ether and chloroform.
Storage:
Stored in tightly- closed containers.
Uses:
1. Bacteriostatic agents and
2. Treatment of TB
Dose: 25 mg/kg
Pharmaceutical Formulation :pyrazinamide tablet
Brand name: pyride
Pyrina-500
Zinamide

10. Chemical name: 4 –amino- 2 -hydroxy benzoic acid
PAS: Para Amino salicylic acid
Physical Properties
1. White or yellowish white crystal.
2. Odourless
3. Slightly soluble in water
4. Has slightly acid taste.
5. Soluble in alkalies and in dil. Dil.nitric acid.
Chemical properties
2-Hydroxy benzoic acid
2-Hydroxy 4-nitrobenzoic acid Para Amino salicylic acid

11. Stability and storage:
Stored in tightly- closed, light- resistant containers.
Uses:
1. To treat tuberculosis.
2. Used in combination with isoniazid Or
Streptomycin
Formulation:
1. Amino salicylic acid tablets.
2. Amino salicylate sodium tablets.
3. Amino salicylate Potassium tablets.
4. Amino salicylate Calcium tablets.
5. Amino salicylate Calcium Capsules.
Dose: 10-12 mg per day in divided
doses.
Brand name: paser, monopas,
Idipas, Benzapas

12. Rifampicin or Rifampin
Physical Properties
1. Reddish - brown crystalline powder
2. Odourless
3. Very Slightly soluble in water and alcohol
4. Soluble chloroform
Chemical properties:
1. In acidic medium: it is hydrolysed to give 3-formyl rifampicin.
2. In alkaline medium: it is oxidized to give quinone.
3. In neutral medium: ester group of rimpicin is slowly hydrolysed.

13. Uses
1. Broad spectrum antibiotics.
2. Used to treat bililary infection.
3. Used in the treatment of meningitis.
4. Used to treat TB.
Pharmaceutical Formulations:
Rifampicin capsules
Brand Name:
1. Rimpin
2. Rimpacin
Stability and storage:
Stored in tightly- closed, light- resistant containers in an atmosphere of
nitrogen

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