Drug for Tuberculosis

Isoniazid Rifampicin Pyrazinamide Ethambutol Streptomycin

General ~ Bactericidal – fast-dividing ~ Bactericidal – extra & intracellular ~ largely bacteriostatic ~ bacteriostatic on MTB ~ broad-spectrum
~ Bacteriostatic – slow-dividing bacilli ~ bacteriostatic on actively ~ poor penetration (extracellular
~ Penetrates cell wall – extra & intracellular ~ Broad-spectrum – gram +, gram - , replicating MTB bacilli only)
bacilli clamydiae
Pharmaco-kinetics ~ Oral or parenteral route ~ Oral ~ Oral ~ Oral ~ IM only
~ excreted in urine in 24h ~ excreted in feces ~ excreted in urine ~ excreted in urine ~ excreted in urine
Mode of Action Cell wall systhesis DNA transcription Synthesis of fatty acid Cell wall systhesis Protein synthesis

Major adverse ~ Neurotoxicity (pyridoxine deficiency) – ~ harmless – orange urine sweat ~ joint pain (arthralgia) ~ Retrobulbar neuritis (loss of ~ ototoxicity (hearing loss)
reactions paraesthesia, convulsion, ataxia ~ rash, fever, vomiting ~ hepatitis visual acuity & red-green clor ~ nephrotoxicity
~ Induced hepatitis (build up toxic ~ hepatitis ~ skin rash blindness)
acetylisoniazid) ~ nausea, vomiting, anorexia ~skin rash, pleuritis, joint pain
~ allergy: skin rash
Precaution Hepatic deficiency: ↓ dose
Ethanol: isoniazid hepatotoxicity

Ehambutol inhibits
X Mycobacterial
polymerization of
(encoded by pncA gene)
arabinosyltransferase
arqabinogalactan
X formation
(cell wall
of cell wall
component)
Streptomcin binds
X transcription to RNA & X to 16s rRNA of
X protein
synthesis
bacteria