anti tuberculosis drugs
TRANSCRIPT
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Anti Tuberculosis Drugs
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TUBERCULOSIS ?
Chronic granulomatous disease caused by Mycobacterium tuberculosis.
Tuberculosis typically attacks the lungs, but can also affect other parts of the body.
It is spread through the air when people who have an active TB infection cough, sneeze, or otherwise transmit respiratory fluids through the air.
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Symptoms
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Sites of extra-pulmonary tuberculosis
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Chemotherapy of
tuberculosis
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Dru
gs u
sed
in T
B
Firs
t line
Secon
d lin
e
Isoniazid Rifampicin Pyrazinamide Ethambutol Streptomycin
Ethionamide Thiacetazone Para Aminosalicylic acid (PAS) Amikacin Capreomycin Cycloserine Ciprofloxacin Kanamycin Rifabutin Rifapentine
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Based
on
An
ti – TB
activ
ity
tub
erc
ulo
cid
al
tub
erc
ulo
sta
tic
Isoniazid Streptomycin Capromycin Ciprofloxacin Rifampicin Pyrazinamide Kanamycin
Ethambutol Thiacetazone PAS Ethionamide Cycloserine
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Isoniazid (INH)
Most effective and cheapest primary anti tubercular drug.
Effective in both acidic and alkaline medium
Tuberculocidal for rapidly multiplying bacilli Tuberculostatic for resting bacilli
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Mechanism of action Mycolic acids
synthesizes
Isoniazid inhibits
this synthesis
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Adverse effects
Peripheral neuritis Hepatitis Psychosis Seizures Anorexia GIT discomfort Fever Allergic reactions
Less common
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Rifampicin
Semisynthetic derivative of rifamycin , am anitibiotic obtained from streptomyces mediterranei.
Highly effective tuberculocidal Acts on both intra and extracellular organisms. It is called a sterilizing agent.
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Mechanism of action
Rifampicin binds to beta subunit of DNA dependant RNA polymerase and inhibits RNA synthesis in bacteria.
It cannot bind to human RNA polymerase, thus selectively destroying the bacteria.
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Adverse effects
Hepatotoxicity GIT disturbances Flu-like syndrome CNS symptoms – drowsiness, ataxia,
confusion, peripheral neuropathy etc Hypersensitivity reactions Staining of secretions
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Uses
TB & atypical mycobacterial infections
Leprosy Prophylaxis
in H. influenza
Resistant staph
infections
Brucellosis
Pneumococcal meningitis
To eradicate carrier state
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Pyrazinamide
Analog of nicotinamide Tuberculocidal Requires acidic pH for its activity Mechanism of action not clearly known. HEPATOTOXICITY is theMost common adverse effect
May inhibit
synthesis of mycolic
acids
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Streptomycin
Tuberculocidal Acts only against extracellular
organisms Has to be given IM When used alone resistance develops. Least preferred first line drug.
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Ethambutol
Tuberculostatic Also effective against atypical mycobacteria. Well absorbed on oral administration Dose should be reduced in renal failure Optic neuritis is an important adverse
effect which needs withdrawal of the drug. It decreases the renal excretion of uric
acid and enhances plasma urate levels.
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Relative activity of first line drugs
INH: potent bactericidal Rifampicin: potent bactericidal
Pyrazinamide: weak bactericidal Ethambutol: bacteriostatic Streptomycin: bactericidal
Synergistic effect
NEVER USE A SINGLE DRUG FOR CHEMOTHERAPY IN TUBERCULOSIS, A
COMBINATION OF 2 OR MORE IS ALWAYS BETTER
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Second line drugs in TB
Less effective More toxic Used only if organism is resistant to
first line drugs Ethionamide , PAS, cycloserine :
bacteriostatic Amikacin, capromycin,
fluoroquinolones are used in Multi Drug Resistant TB
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Phases of chemotherapy
Phase I
• 1-3 months• Rapidly kills
bacilli• Symptomatic
relief
Phase II
• 4-6 months• Eliminates
remaining bacilli• Prevents relapse
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Conventional drug regimen
1. INH+S+T daily for 2 months2. INH+T daily for 10 months
INH – isoniazidS – StreptomycinT - Thiacetazone
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Short term regimans
1. INH+R+Z+E/S daily or thrice a week for 2 months followed by:
2. INH+R daily or thrice a week for 4 months
3. INH+R+Z trice a week for 2 months followed by
4. INH+R daily for 7 months.
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TH
AN
K Y
OU