Updated: 11/29/2021

Anti-Mycobacterials

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  • Introduction
    • Drugs
      • rifamycins
      • isoniazid
      • pyrazinamide
      • ethambutol
      • dapsone
      • clofazimine
      • streptomycin
    • Clinical use
      • Classic Treatment Paradigm for Mycobacteria
      • Organism
      • Prophylaxis
      • Treatment
      • Mycobacterium tuberculosis
      • Isoniazid
      • Active infection: RIPE therapy
      • Rifampin
      • Isoniazid
      • Pyrazinamide
      • Ethambutol
      • Latent infection:
      • isoniazid x 9 months
      • Mycobacterium avium-intracellulare
      • Azithromycin
      •  Rifabutin
      • Azithromycin + ethambutol
      •  Can also add rifabutin or ciprofloxacin
      • Mycobacterium leprae
      • Tuberculoid: dapsone + rifampin
      •  Lepromatous: dapsone + rifampin + clofazimine
    • Anti-Mycobacterial Medications
      DrugMechanism of Action
      Adverse Effects
      Notes

      Rifamycins (rifampin and rifabutin)

      • Inhibits DNA-dependent RNA polymerase
      • Hepatotoxicity
      • Red or orange body fluids
      • CYP450 inducer
      • Rifabutin has less CYP450 effect, thus favored for HIV patients
      • Mutations occur due to decreased binding to RNA polymerase
      • Resistance occurs rapidly if used as monotherapy
      Isoniazid
      • Inhibits synthesis of mycolic acids
      • Hepatotoxicity
      • Inhibits CYP450
      • Drug-induced systemic lupus erythematosus
      • Vitamin B6 deficiency
        • peripheral neuropathy
        • sideroblastic anemia
        • co-administer with pyridoxine (B6) to reduce side effects
      • May be used as monotherapy for prophylaxis and latent TB
      • Mutations occur due to underexpression of enzyme required to convert drug into active metabolite
      Pyrazinamide
      • Unknown but may work through host phagolysosomes
      • Hepatotoxicity
      • Hyperuricemia
      -
      Ethambutol
      • Inhibits arabinosyltransferase and disrupts cell wall
      • Optic neuropathy
        • red-green color blindness
      -
      Dapsone
      • Inhibits dihydropteroate synthesis (anti-folate)
      • Methemoglobinemia
      • Hemolysis (G6PD deficiency patients)
      -
      Clofazimine
      • Disrupts DNA
      • Gastrointestinal upset
      • Dry skin
      • Pink/brown skin and body fluid dyspigmentation
      -
      Streptomycin
      • Interacts with 30S ribosomal subunit
      • Tinnitus
      • Vertigo
      • Ataxia
      • Renal toxicity
      • Second-line treatment forM. tuberculosis
      • Anti-Mycobacterial Medications
      • Drug
      • Mechanism of Action
      • Adverse Effects
      • Notes

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