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5 Cards in this Set
- Front
- Back
1st Line Agents for TB
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INH (isoniazide), RMP (rifampin), PZA (pyrazinamide), EMB (Ethambutol)
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Rifampin
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bactericidal
MOA: Inhibits bacterial DNA dependant RNA polymerases (DDRP) ADRs: discolor bodily fluids, cause liver toxicity, induce CYP450 => DDI |
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Insoniazide
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activated by catalase-peroxidase enzyme (katG) to an acylating residue
MOA: covalently react with NADH (=> inhib reduction of unsaturated fatty acids to saturated fatty acids => inhib synthesis of mycolic acid); inhibition in the transport of precursor fatty acids (of mycolic acid) to the cell envelope ADRs: Basic –NH2, can cause problems in metabolism (Fast/slow metabolizers, e.g. acetyl transferases) and also tends to react with pyridoxal phosphate (PLP, the activated form of Vit B6) => deplete PLP => ↓GABA synthesis => ↑ CNS side-effects (e.g. seizures) usually used with Vit B6 supplements; GI upset, jaundice, hepatotoxicity |
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Pyrazinamide
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POA provides an acidic environment => ↓ in membrane potential of the mycobacteria => ↓ in the energetics of the cell and membrane transport => cell death
ADRs: hyperuricemia, hepatotoxicity |
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Ethambutol
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MOA: inhibitor of arabinosyl transferase and arabinosyl polymerization
ADRs: optic neuritis => ↓ visual acuity - inability to distinguish red-green |