For D Pharmacy students

1. Presented by- Rahul Jadhav
Anusaya Institute of Pharmacy, Swami-
chincholi, Daund, Pune.

2. Tuberculosis:-
It is a Chronic Granulomatous disease and a major
health problem in a developing country.
 It is caused in humans by mycobacterium tuberculosis.
 It is characterized by inflammatory infiltration, tubercles
formation, fibrosis and calcification.
 It usually affects on the respiratory tract.

3.  The agent that is used in the treatment of tuberculosis, a disease
caused by Mycobacterium species ( M. Tuberculosis, M. Bovis,
M. Africanum ) characterized by formation of nodular bodies or
tubercles.
Classification:
1) P-amino salicylic acid derivative: e.g. PAS
2) Pyridine derivative: e.g. Isoniazid, Ethionamide
3) Pyrazine derivative: e.g. Pyrazinamide
4) Ethylene diamine derivative: e.g. Ethambutal
5) Antibiotics: e.g. Cycloserine, Streptomycin, Rifampicin

4. 1) First line drugs: e.g. Isoniazide, Rifampin, Ethambutol,
Pyrazinamide, Streptomycin.
2) Second line drugs; e.g Ethionamide, kanamycin, Cycloserin,
Capreomycin.
3) Third line drugs. e.g. Clarithromycin, Thioacetazone.

5. 1) ISONIAZID: (INH)
 Other names: Isonicotinic acid hydrazide, Isonicotino hydrazide,
Isonicotinyl hydrazide.
 Chemical name: pyridine-4-carbohydrazide.
 Physical Properties:
 Colourless crystals or white crystalline powder
 Odourless
 Sweet test followed by bitter test
 Soluble in water
 Chemical properties:
1) Isoniazid treated with bromine water in presence of HCL convert
into isonicotinic acid with liberation of N2 gas.

6. 2) Isoniazid treated with benzene sulphonyl chloride , convert into
its benzene sulphonyl derivative.
3) Isoniazid treated with isopropyl chloride, converted to N-
isonicotinyl, N- isopropile hydrazine which is also have
antitubercular activity.
 Stability and storage:
 Affected by light hence stored in tightly closed light resistant
containers.
 Uses:
1. Used in treatment of –
 Pulmonary tuberculosis
 Extrapulmonary lesions, including meningial and genito-
urinary infections.

7.  Lupus vulgaris.
2. As isoniazid develops resistance within a few weeks, it is given in
conjugation with ethambutal or rifampicin or streptomycin.
 Pharmaceutical Preparations:
 Isoniazid elixir, tablets, injection
 Sodium aminosalicylate and isoniazid Granules and Powers
 Isoniazid and ethambutal tablets
 Isoniazid and rifampicin tablets
 Brand Names: Cadizide, Isonex, Rimpazid, Isocadopas.

9. 3. To reduce gastric irritation produced by PAS when
given orally, it convert into-
a) ester by treating with alcohol in presence of dil.
H2So4
b) N-acetyl derivative when treated with benzoyl
chloride
4) It oxidized by air / oxygen with formation of black
or brown pigments.
• Stability and storage: It darkens when exposure to
air and light, stored in tightly closed light-
resistant containers.

11. • Chemical name: (+) N, N' Bis [(R)' - 1- hydroxy methyl
propyl] ethylenediamine.
• Physical properties: Its hydrocloric salt is yellow
crystalline powder, odourless, slightly soluble in
water.Its dextro isomer is more potent than laevo
isomer
• Chemical properties: aqueous solution of ehtambutal
hydrochloride when treated with copper sulphate and
solution made alkaline with NaOH, blue coloue is
produced

12. • Storage : stored in tightly closed containers.
• Uses:
 Used in treatment of tuberculosis.
 Used in combination with other AntiTB drugs.
• Pharmaceutical formulations :
 Ethambutol tablets, pawders
 Ethambutol and Isoniazid tablets.
• Brand names: Mymbutol, Albutol, Ly-butol

13. • Physical properties : Yellow crystals or crystalline
powders, odourless, tasteless, slightly soluble in
water.
• Chemical properties :
1. When solution in 6N NaOH is boiled with lead
acetate sol. for 1 min., produce black ppt of lead
sulphate.
2. Hydrolysis and Diazotization reaction: solution
boiled with 1 N HCL and treated with NaNo2 and
HCL gives diazo compound. This compound with

14. • Stability and storage: Affected by light, stored in
air-tight, light resistant containers.
• Uses:
1. In treatment of tuberculosis and leprosy.
2. Used in combination with streptomycin and
Isoniazid.
• Pharmaceutical formulations : Thiacetazone tablet
• Brand names: Thiopramizone, Decetazone

15. • Physical properties: Yellow crystalline powder,
slight odourl, unpleasant sulphurous taste,
insoluble in water
• Chemical properties :
1. When heated with sodium hydroxide, ammonia
gas evolves.
2. When heated with HCL, H2S gas evolves.
• Stability and storage: Affected by light, hence
stored well closed, light-resistant containers.

16. • Uses: used to treat pulmonary tuberculosis.
• Pharmaceutical formulations : Ethionamide tablet
• Brand names: Ethynex, Trescalyl
6) Pyrazinamide:
• Chemical name: Pyrazine-2- carboxamide
• Physical properties: White crystalline powder,
odourless, slight bitter taste. Sparingly soluble in
water and suluble in ether and chloroform.

17. • Stability and storage: Stored in tightly closed
containers.
• Uses:
 Used as tuberculostatic agent.
 Active against strains which are resist to other
AntiTB drugs
• Pharmaceutical formulations : Pyrazinamide tablet
• Brand names: Zinamide, Pyride, Pyrina-500

18. • Chemistry: Low molecular weight hydrophilic
antibiotic obtained from Streptomyces
orchidaceus / S. garyphatus.
• Physical properties : White / pale yellow
crystalline powder, Odourless and slight bitter
taste. It is hygroscopic, soluble in water and
dextro rotatory.
• Storage and Stability: It is hygroscopic & affected
by heat, hence stored in tightly closed containers
temperature not exceeding 25° c.

19. • Category: Antibacterial ( Tuberculostatic)
• Uses:
 In treatment of pulmonary tuberculosis.
 As Antibacterial agent. Used when Streptomycin is
not effective.
 In treatment of urinary tract infection.
• Pharmaceutical formulations :
 Cycloserin tablet & capsule.
• Brand names: Cycosin, Themiserin.

21. • Stability and storage : Affected by moisture and
heat, hence stored in well closed containers at
temp. not exceeding 30°c and protected from
moisture.
 If intended for parenteral container should be
sterile and sealed.
• Uses: It is broad spectrum antibiotics and
antibacterial.
 Orally, in intestinal infection of large intestine.
 Intramuscularly, to treat all form of tuberculosis.

22.  Non tubercular infection like cholecystisis,
peritonitis.
• Pharmaceutical formulations :
 Streptomycin tablet, Injection.
• Brand names : Chlorostrep, Enterostrep,
Lykastrep, Streptomax.
9) Rifampicin / Rifampin:
• Physical properties : Brick-red / reddish-brown
colour, odourless. It is very soluble in water and
alcohol, soluble in chloroform. It is Unstable in

23. • Chemical properties :
1. In alkaline medium it oxidised to quinone.
2. Hydrolysed in acidic medium to give 3- formyl
Rifampicin.
3. Ester group slowly Hydrolysed in neutral medium.
4. Aq. solution is treated with ammo. presulphate at
pH 7.4, colour changes from orange-yellow to
violet-red.
• Stability and storage : Unstable in moisture, affected
by light and air, hence stored in tightly closed light-
resistant containers in atmosphere of nitrogen and
temp. not exceeding 15° c.

24. • Uses: Broad spectrum antibiotics.
1. Used to treat TB.
2. Used to treat biliary infection.
3. Used to treat meningitis.
• Pharmaceutical formulations :
• Rifampicin capsules.
• Brand names : Rimpin, Rimpacin.