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Anti tubercular drugs
TONYSCARIA 2010 KMC
First line
• Isoniazid
• Rifampicin
• Ethambutol
• Streptomycin
• Pyrazinamide
Second line
• Cycloserine
• Kanamycin
• Amikacin
• Ciprofloxacin
• Ofloxacin
• Clarithromycin
TONYSCARIA 2010 KMC
INH
• Drug of choice for TB
• Inhibit synthesis of mycolic acid
• DOC for prophylaxis of TB
TONYSCARIA 2010 KMC
TONYSCARIA 2010 KMC
TONYSCARIA 2010 KMC
INH
• Most effective antitubercular drug against intracellular & extracellular
organism
• Penetrates in to caseous material & perisist in therapeutic
concentration
TONYSCARIA 2010 KMC
INH
• Metabolised by acetylation
• Metabolism is under genetic control
• Fast acetylation
• Slow acetylation
TONYSCARIA 2010 KMC
s/e of INH
• Peripheral neuritis
• Transient memory loss
• Psychosis
• Hepatitis
• Optic neuritis
TONYSCARIA 2010 KMC
Rifampicin
TONYSCARIA 2010 KMC
Rifampicin
• Tuberculocidal for both dividing & nondividing bacteria
• Inhibiting beta subunit of DNA dependant rna polymerase
• bactericidal for both intracellular and extracellular mycobacteria,
including M.tuberculosis, and atypical mycobacteria, such as M.
kansasii
• Only bactericidal drugs active against dormant bacilli in caseous lesions
TONYSCARIA 2010 KMC
• Also used in
• Meningococcal prophylaxis
• Staphylococcal carrier state
• Treatment of leprosy
TONYSCARIA 2010 KMC
• Rifampin is well absorbed after oral administration and excreted
mainly through the liver into bile. It then undergoes enterohepatic
recirculation, with the bulk excreted as a deacylated metabolite in
feces and a small amount in the urine.
• Dosage adjustment for renal or hepatic insufficiency is not necessary
TONYSCARIA 2010 KMC
• s/e
• Orange discolouration of urine & other secretion
• Flu like syndrome
• Hepatitis
TONYSCARIA 2010 KMC
Rifampicin is an enzyme inducer
Rifampicin  induces metabolism of
antiretrovirals hence in AIDS patients with TB
rifabutin is used
TONYSCARIA 2010 KMC
Rifabutin
• derivative of rifampin,
• less potent inducer of cytochrome P450 enzymes.
• preferred drug for use in tuberculosis-infected patients with the human
immunodefciency virus (HIV), who are concomitantly treated with protease
inhibitors or nonnucleoside reverse transcriptase inhibitors
• Rifabutin has adverse effects similar to those of rifampin, but can also
cause uveitis, skin hyperpigmentation, and neutropenia
• No dose adjustment needed in hepatic or renal failure
TONYSCARIA 2010 KMC
Ethambutol
• Only first line tuberculostatic drug
• Fast multiplying bacilli are more susceptible
• does not cross BBB
TONYSCARIA 2010 KMC
Ethambutol inhibit arabinosyl transferase 
inhibit mycolic acid synthesis
TONYSCARIA 2010 KMC
S/E
• Retrobulbar neuritis
• Red green colour blindness
• Hyperuricemia
• Peripheral neuritis ‘
TONYSCARIA 2010 KMC
Pyrazinamide
• Tuberculocidal drug
• Acts by inhibiting mycolic acid synthesis
• active against slowly dividing organisms
• Active drug against intracellular bacteria
• Pyrazinamide is active against tubercle bacilli in the acidic environment of
lysosomes, as well as, in macrophage
TONYSCARIA 2010 KMC
• S/E
• Arthralgia
• Hyperuricemia
• MOST HEPATOTOXIC ANTITUBERCULAR DRUG
TONYSCARIA 2010 KMC
Ethionamide
• Develops cross resistance to INH
• S/E
• Optic neuritis
• Optic neuritis hypothyroidism
TONYSCARIA 2010 KMC
TONYSCARIA 2010 KMC
Active against
extracellular
mycobacteria
•Rifampicin
•INH
•Streptomycin
Active against
intracellular
mycobacteria
•Rifampicin
•INH
•Pyrazinamide
TONYSCARIA 2010 KMC
No dose adjustment in renal failure
• Rifapentine
• Rifabutin
• Rifamycin
TONYSCARIA 2010 KMC
Hypothyroidism can be caused by
• PAS
• Ethionamide
TONYSCARIA 2010 KMC
Hyperuricemia caused by
• Pyrazinamide
• Ethambutol
TONYSCARIA 2010 KMC
TONYSCARIA 2010 KMC
TONYSCARIA 2010 KMC
TONYSCARIA 2010 KMC
NIKSHAY- A web based solution for
monitoring of TB patients
• SMS services have been used effectively for communication with
patients and monitoring the programme on day to day basis.
TONYSCARIA 2010 KMC

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