Pharm mycobacterial drugs

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Pharm mycobacterial drugs
2012-05-05 21:16:32
mycobacterial drugs

mycobacterial drugs
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  1. Isoniazid
    • Uses: clinically manifest disease; prophylaxis
    • Mechanism: inhibits synthesis of mycolic acids
    • Pharmacokinetics: readily absorbed in GI tract; effective intracellularly and extracellularly; good CNS penetration; inactivated by acetylation (population variability)
    • Adverse effects: peripheral and central neurotoxicity (prevented by coadministration of B6); hepatotoxicity
  2. Rifampin
    • Uses: First line in combo; can be used as prophylaxis against other infections
    • Mechanism: inhibits bacterial DNA dependent RNA polymerase
    • Pharmacokinetics: well absorbed from GI tract; excreted into bodily fluids, turning them orange-red
    • Adverse effects: usually well tolerated but can cause jaundice, rash, thrombocytopenia, nephritis, & hepatotoxicity
  3. Ethambutol
    • Uses: First line in combo
    • Mechanism: inhibits synthesis of arabinogalactan
    • Pharmacokinetics: readily absorbed from GI tract; excreted in urine; does not cross blood-brain barrier
    • Advere effects: few side effects; optic neuritis; try to avoid in children
  4. Pyrazinamide
    • Uses: short term therapy in combo
    • Mechanism: inhibits mycobacterial fatty acid synthase I gene (involved in mycolic acid synthesis)
    • Pharmacokinetics: readily absorbed in GI tract and mostly excreted in the urine
    • Adverse effects: hepatotoxicity; contraindicated in patients with severe liver disease or gout