Updated: 12/20/2019

H2 Blockers

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Introduction
  • Other agents: cimetidine, famotidine, and nizatidine 
  • Mechanism 
    • indirectly inhibit proton pump by blocking stimulation via H2 receptors on parietal cells and ECL cells
      • leads to ↓ H+ secretion by parietal cells
    • no effect on gastic emptying time
  • Clinical use
    • peptic ulcer
    • gastritis
    • GERD
    • Zollinger-Ellison syndrome
  • Toxicity
    • cimetidine
      • potent inhibitor of P-450 
      • antiandrogenic effects 
        • results in gynecomastia, impotence, and ↓ libido in males
      • crosses blood-brain barrier
        • results in confusion, dizziness, and headaches
        • avoid in the elderly and mentally unstable
      • crosses placenta
    • cimetidine and rantidine ↓ creatinine clearance
    • other H2 blockers have fewer side effects
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