8/3/2019 Anti-Mycobacteria Drugs

1/1

Barry Park, CRRAB2, PBL#4

Antituberculosis Agents

Drug MOA & Static or Cidal Selective Toxicity Pharmacokinetics Resistance Mechanism Toxicities Unique Properties

Isoniazid I/H synth of mycolicacidscell wall

component cidal of actively growing

bacilli

penetrates macrophages active against extra- &

intracellular organisms

-cidal Most effective

forM.

tuberculosis &M. ansasii

Not for atypicalmycobacteria

Diffuses readily, even in CNS life: 1-3 hours

distribution: nearly 100% elimination: liver- fast and

slow acetylators of littleclinical consequence

muts resulting in: overexpression of inhA

mut/del of kagG mut of ahpC (virulence

factor)

mut of kasA

Occl fever or skin rash Drug-induced hepatitis (1%)

DISCONTINUE! Benign increase (3-4X) in

liver aminotransferass (20-30%)

Others (25%) Peripheral neuropathy

CNS dysfunction (depression,psychosis)

Co-administer withpyridoxine to preventneuro S/E

Aminoglycosides

streptomycin 30s ribosomal subunitI/Hdecreased proteinsynth

-cidal distribution: poor, activemainly extracellularly

elimination: renal ribosomal structure

muts

ototoxic nephrotoxic dose-related

Only IV administered Used in severe, life-

threatening disease

Useful in resistantdisease