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Updated: Dec 20 2019

H2 Blockers

  • 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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