5.ANTIMYCOBACTERIALS

BYBY
Dr.Dr. SAMINATHAN KAYAROHANAMSAMINATHAN KAYAROHANAM
M.PHARM, M.B.A, PhDM.PHARM, M.B.A, PhD
ANTIMYCOBACTERIALS
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NUM CONTENT SLIDE
1 INTRODUCTION TO MYCOBACTERIUM 4
2 OVERVIEW OF TUBERCULOSIS 5-9
3 TUBERCULOSIS-PREVALENCE(WHO-2009) 10
4 SYMPTOMS OF TUBERCULOSIS 11
5 OVERVIEW OF TO LEPROSY 12-21
6 LEPROSY-PREVALENCE(WHO-2004) 22
7 CLASSIFICATION OF ANTIMYCOBACTERIALS 23
8 MECHANISM OF ANTIMYCOBACTERIALS 25,26
9 MECHANISM OF ISONIAZID 27
10 MECHANISM OF RIFAMYCINS 28
11 SOME CHARACTERISTICS OF FIRST-LINE DRUGS
USED IN TREATING TUBERCULOSIS
29
12 CHEMOTHERAPY LEPROSY PATIENT 30
13 CHEMOTHERAPY TUBERCLOSIS PATIENT 31
14 TREATMENT GUIDELINES FOR TUBERCLOSIS 32-34
15 COMMON SIDE EFFECTS OF TUBERCLOSIS DRUGS 35-37
16 TREATMENT GUIDELINES FOR LEPROSY 38

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LEARNING OUTCOME
1. Describe and understand the tuberculosis and leprosy.
2. List the dug classification to treat tuberculosis and
leprosy.
3. Understand the symptoms of tuberculosis and leprosy.
4. Abele to demonstrate the general mechanism of drugs
used to treat tuberculosis and leprosy.
5. Able to describe the common tuberculosis and leprosy
drugs adverse effects.
6. Able to understand the therapeutic application of
tuberculosis and leprosy drugs.

4
Mycobacterium tuberculosis complex refers to a group
of Mycobacterium species that can cause tuberculosis in
humans.
1. INTRODUCTION TO MYCOBACTERIUM
 Mycobacterium is a genus of Actinobacteria,
given its own family, the Mycobacteriaceae.To
cause serious diseases in mammals.
1. Tuberculosis (Mycobacterium Tuberculosis)
2. Leprosy
(Mycobacterium Leprae,
Mycobacterium lepromatosis)
 Mycobacteria are aerobic and nonmotile
bacteria
(except for the species mycobacterium marinum)
 That are characteristically acid-alcohol-fast.
•Mycobacterium
tuberculosis
•Mycobacterium
africanum
•Mycobacterium bovis
•Mycobacterium microti
•Mycobacterium canettii
•Mycobacterium caprae
•Mycobacterium
pinnipedii
•Mycobacterium mungi
Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

5
2.OVERVIE OF TUBERCULOSIS
Tuberculosis, or TB, is an infectious bacterial
disease caused by Mycobacterium tuberculosis,
which most commonly affects the lungs.
It is transmitted from person to person via
droplets from the throat and lungs of people with
the active respiratory disease.
Today, these new and dangerous forms of the
disease -- resistant to some of the commonly used
drug treatments -- have created a public health
crisis in many large cities worldwide

6
Mycobacterium tuberculosis, one of a number of
mycobacteria, can lead to serious infections of the lungs,
genitourinary tract, skeleton, and meninges.
Treating tuberculosis as well as other mycobacterial
infections presents therapeutic problems.
The organism grows slowly; thus, the disease may have to
be treated for 6 months to 2 years. Resistant organisms
readily emerge, particularly in patients who have had prior
therapy or who fail to adhere to the treatment protocol.
It is currently estimated that about one-third of the world's
population is infected with M. tuberculosis, with 30 million
people having active disease. Worldwide, 8 million new cases
occur, and approximately 2 million people die of the
disease each year.

Dr.K.Saminathan.M.Pharm(Ph.D) , M.B.A (Ph.D)
7

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10
3.TUBERCULOSIS-PREVALENCE(WHO-2009)

11
4.SYMPTOMS OF TUBERCULOSIS

12
Leprosy, also known as Hansen's disease (HD), is a chronic
infection caused by the bacterium Mycobacterium leprae and
Mycobacterium lepromatosis.
Leprosy takes its name from the Latin word Lepra, which means
"scaly", while the term "Hansen's disease" is named after the
physician Gerhard Armauer Hansen. It is primarily a
granulomatous disease of the peripheral nerves and mucosa of
the upper respiratory tract; skin lesions are the primary external
sign.
Left untreated, leprosy can be progressive, causing permanent
damage to the skin, nerves, limbs and eyes. Contrary to
folklore, leprosy does not cause body parts to fall off, although they
can become numb or diseased as a result of secondary infections;
these occur as a result of the body's defenses being compromised
by the primary disease.
5.OVERVIEW OF TO LEPROSY

13
•Initially, infections are without symptoms and typically remain
this way for 5 to as long as 20 years.
•Symptoms that develop include granulomas of the nerves,
respiratory tract, skin, and eyes.
•This may result in a lack of ability to feel pain and thus loss
of parts of extremities due to repeated injuries. Weakness and
poor eyesight may also be present
• Until 1941, there was no cure. Even today, in some areas,
leprosy is still a significant, public-health problem.
•Socially, leprosy isolated someone from the community.
•The World Health Organization recommends the triple-drug
regimen of dapsone, clofazimine, and rifampin for 6 to 24
months.

14
Historical of Leprosy:
Norwegian physician Gerhard Armauer Hansen discovered the
Mycobacterium Leprae in 1876. He was searching in the skin of
patients with leprosy and discovered this bacterium.
Leprosy was recognized in many ancient civilizations like China,
Egypt, and India dating all the way back to 600 BC.
1921, the U.S established that nations first leprosarium in
Louisiana in order to institutionalize patients with leprosy for
experiments and further research.

15
Common Symptoms:
Skin lesions
•Numbness
•Muscle Weakness
•Lesions have decreased sensation to touch, pain, or heat.
•The lesions are lighter than your skin color.
5. OVERVIEW OF TO LEPROSY

16

Dr.K.Saminathan.M.Pharm(Ph.D) , M.B.A (Ph.D)
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Dr.K.Saminathan.M.Pharm(Ph.D) , M.B.A (Ph.D)18

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6. LEPROSY-PREVALENCE(WHO-2004)

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7. CLASSIFICATION OF ANTIMYCOBACTERIALS
Con…Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

7. CLASSIFICATION OF ANTIMYCOBACTERIALS
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0
20
40
60
80
100
120
一月二月三月四月
亚洲区
欧洲区
北美区
8. MECHANISM OF ANTIMYCOBACTERIALS
1425

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8. MECHANISM OF ANTIMYCOBACTERIALS

27
Isoniazid, the hydrazide of isonicotinic acid, is a synthetic
analog of pyridoxine.
Isoniazid, often referred to as INH, is a prodrug that is
activated by a mycobacterial catalase-peroxidase (KatG).
Genetic and biochemical evidence has implicated at least
two different target enzymes for isoniazid within the unique
Type II fatty acid synthase system involved in the production
of mycolic acids.
The targeted enzymes are enoyl acyl carrier protein
reductase (InhA) and a ketoacyl-ACP synthase (KasA). The
activated drug covalently binds to and inhibits these
enzymes, which are essential for the synthesis of mycolic
acid.
9.MECHANISM OF ISONIAZID

28
Rifampin, rifabutin, and rifapentine are all
considered to be rifamycins, a group of
structurally similar macrocyclic antibiotics, which are
first-line drugs for tuberculosis. Any of these
rifamycins must always be used in conjunction with
at least one other antituberculosis drug to which the
isolate is susceptible.
Rifampin blocks transcription by interacting with the
subunit of bacterial but not human DNA-dependent
RNA polymerase.
[Note: The drug is thus specific for prokaryotes.]
Rifampin inhibits mRNA synthesis by suppressing
the initiation step.
10. MECHANISM OF RIFAMYCINS

29
11. SOME CHARACTERISTICS OF FIRST-LINE DRUGS
USED IN TREATING TUBERCULOSIS

30
12.CHEMOTHERAPY LEPROSY PATIENT

31
13. CHEMOTHERAPY FOR TUBERCLOSIS PATIENT

32
14. TREATMENT GUIDELINES FOR TUBERCLOSIS

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14.TREATMENT GUIDELINES FOR TUBERCLOSIS

34Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

Dr.K.Saminathan.M.Pharm(Ph.D) , M.B.A (Ph.D) 35
15. COMMON SIDE EFFECTS OF TUBERCLOSIS DRUGS

Dr.K.Saminathan.M.Pharm(Ph.D) , M.B.A (Ph.D) 36Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

37 Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

Dr.K.Saminathan.M.Pharm(Ph.D) , M.B.A (Ph.D)38
16.TREATMENT GUIDELINES FOR LEPROSY

40
MYCOBACTERIUM BACTERIA
ACID-FAST MYCOBACTERIALEPROMATOUS LEPROS
MYCOBACTERIUM TUBERCULOSIS
INFECTION OF LUNG
MYCOBACTERIUM TUBERCULOSIS

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Bacillus Calmette–Guérin (historically Vaccin Bilié de Calmette et
Guérin commonly referred to as Bacille de Calmette et Guérin or BCG)
is a vaccine against tuberculosis that is prepared from a strain of the
attenuated (virulence-reduced) live bovine tuberculosis
bacillus, Mycobacterium bovis, that has lost its virulence in humans by
being specially subcultured in a culture medium, usually Middlebrook 7H9
BCG vaccine

5.ANTIMYCOBACTERIALS

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5.ANTIMYCOBACTERIALS