Tuberculosis- causative agent Anti-Tubercular Agents- definition, classification [Study of the following category of medicinal compounds with respect classification, chemical name, chemical structure (compounds with * mark), uses, stability and storage conditions, different types of formulation & their popular brand names] INH*, Ethambutol, Para Amino Salicylic Acid, Pyrazinamide, Rifampicin, Bedaquiline, Delamanid, Pretomanid*

1. Presented by:- Shalini N. Barad
Lecturer,
Appasaheb Birnale College of
Pharmacy
TUBERCULOSIS

2. Index
 Tuberculosis- causative agent
 Anti-Tubercular Agents- definition, classification
[Study of the following category of medicinal compounds
with respect classification, chemical name, chemical
structure (compounds with * mark), uses, stability and
storage conditions, different types of formulation & their
popular brand names]
1) INH*,
2) Ethambutol,
3) Para Amino Salicylic Acid,
4) Pyrazinamide,
5) Rifampicin,
6) Bedaquiline,
7) Delamanid,

3.  Mycobectrium tuberculosis, the causative agent
for tuberculosis (TB)
 Mycobacteria are transition forms between bacteria
and fungi.
 Mycobacteria are characterized by nonmotile,
nonsporulating rods that resist decolorization with
acidified organic solvents (acid fast bacteria).
 Tuberculosis (TB) is an acute or chronic
communicable disease.
 It is caused in humans mycobacterium tuberculosis
of homonis type, but can also be caused by bovine
type.
 It is characterised by inflammatory infiltrations,
tubercle formation, fibrosis and calcification affects

4.  Extrapulmonary TB is more common in
patients suffering AIDS (i.e. HIV infected
patients).
 The primary tuberculosis spreads through
blood stream mainly meninges, bones and
genito-urinary tract.
 Post primary tuberculosis leads to
necrosis, ulceration and cavitation to give
extensive lesions.

6.  Anti-tubercular drugs are agents used for
the treatment of parasitic diseases caused
by Mycobacteria tuberculosis.

7.  Classification
 According their clinical utility the anti-TB drugs
can be divided into:
A. First line drugs: Highly effective bactericidal
agents, with an acceptable degree toxicity.
These drugs have high antitubercular efficacy
as well low toxicity; used routinely.
 Isoniazid,
 Rifampin,
 Ethambutol,
 Streptomycin,
 Pyrazinamide

8. B. Second line drugs: These drugs have
either low antitubercular efficacy or high
toxicity or both; are used in special
circumstances only.
 For antimicrobial resistance or patient
related factors.
 Combinations drugs necessary treat
tuberculosis prevent development of
resistant bacilli.
1. Amikamycin 5. Cycloserine
2. Ethionamide 6. Capreomycin,
3. P-amino salicylic acid 7. THioacetazone

11.  Isoniazid
 Stability and Storage: It is affected by light and
hence it is stored in tightly-closed light-resistant
containers.
 Uses:
1. It used in treatment of:
 i)pulmonary tuberculosis
 (ii) extrapulmonary lesions, including meningeal
and genito-urinary infections
 (iii) lupus vulgaris.
2. As isoniazid develops resistance within a weeks,
it given conjunction ethambutol or rifampicin or
streptomycin.

13.  Pharmaceutical Formulations:
1. Isoniazid elixir (syrup).
2. Isoniazid tablets IP.
3. Sodium aminosalicylate and Isoniazid
granules.
4. Sodium aminosalicylate and Isoniazid
powder.
5. Isoniazid and ethambutol tablets.
6. Isoniazid and rifampicin tablets.
7. Isoniazid injection.
 Brand Names: Cadizide, Isonex, Rimpazid,

14.  Para-Amino salicylic acid (PAS)
 Chemical Structure:
 Chemical Name: 4-amino, 2-hydroxy,
benzoic acid.
 Stability and Storage : It darkens on
exposure to air and light. Hence, it is
stored in tightly-closed, light containers.

15.  Uses:
1) It is used in the treatment of tuberculosis.
2) It is generally given in combination with isoniazid
and streptomycin. It is now replaced by more
effective and well tolerated antitubercular agents
like rifampicin, ethambutol
 Pharmaceutical Formulations:
(1) Amino salicylic acid tablets.
(ii) Amino salicylate sodium tablets.
(iii) Amino salicylate potassium tablets.
(iv) Amino salicylate calcium capsules.
(v) Amino salicylate calcium tablets.
(vi) Benzoyl PAS calcium tablets.
 Brand Name: Idipas, Isopar, Benzapas, Pacser,

16.  Ethambutol Hydrochloride:
 Storage: It is stored in tightly-closed containers.
 Uses:
1) It is used in the treatment of tuberculosis.
2) IT is given in conjunction with other
antitubercular drugs.
3) It is also active against the strains which are
resistant to other antitubercular drugs.
 Pharmaceutical Formulations :
1) Ethambutol tablets.
2) Ethambutol powder.
3) Isoniazid and ethambutol tablets.
4) Brand Names: Myambutol, Albutol, Ly-Butol.

17.  Rifampicin or Rifampin:
 Stability and Storage :it is stored in tightly-
closed light-resistant containers in an
atmosphere of nitrogen and at a temperature
not exceeding 15°C.
 Rifampin is unstable in moisture and hence
desiccant, silica gel, should be included
rifampin capsule container.
 Uses :It is a broad spectrum antibiotic.
1) It is mainly used to treat tuberculosis. It is
useful when resistance to other develops. It
is given in conjunction with other
antitubercular agents like Isoniazid,
ethambutol, streptomycin.
2) It is also used to treat biliary infections.

18.  Pharmaceutical Formulation :Rifampicin
capsules IP.
 Brand Names: Rimpin, Rimpacin.

19.  Pyrazinamide:
 Storage: It is stored in tightly-closed
containers.
 Uses:
1) It is used as a tuberculostatic agent.
2) It is active against the strains which are
resistant to other antitubercular agents.
 Pharmaceutical Formulation
:Pyrazinamide tablets IP.
 Brand Names: Zinamide, Pyride, Pyrina -
500.

20.  Bedaquiline:
 Storage: It is stored in tightly-closed
containers protected from light and
moisture
 Uses:
1) As part of combination therapy in adults (
≥ 18 years) with pulmonary multi-drug
resistant tuberculosis (MDR-TB).
 Pharmaceutical Formulation:
Bedaquiline Tablet IP.
 Brand Names: Sirturo.

21.  Delamanid:
 Storage: It is stored in tightly-closed
container protected from light and
moisture.
 Uses:
1) Multidrug-resistant tuberculosis may also
require more than 2 years of
chemotherapy and second-line therapies
with narrow therapeutic index.
 Pharmaceutical Formulation :
1) Delamanid Tablet IP.
 Brand Name: Deltyba.

22.  Pretomanid:
 Chemical Name: (6S)-2-nitro-6-[[4-(trifluoro
methoxy)phenylmethoxyl-6, 7-dhys 5H-
imidazo[2, 1-b][1, 3]oxazine
 Structure:

23.  Uses:
 It is used to treat following disease
conditions:
1) Non-responsive pulmonary multidrug-
resistant (MDR) tuberculosis (TB).
2) Pulmonary extensively drug resistant
(XDR)
3) Treatment-intolerant Pulmonary TB
 Pharmaceutical Formulation:
Pretomanid Tablet IP.
 Brand Name: Dovprela.