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Updated: Oct 24 2018

H1 Blockers

  • Overview
    • Mechanism
      • reversible inhibition of H1 histamine receptors
  • 1st generation
    • Drugs
      • diphenhydramine (Benadryl)
      • dimenhydrinate (Dramamine)
      • chlorpheniramine
      • hydroxyzine
      • promethazine
        • abused as a recreational drug ("purple drank" or "sizzurp")
    • Clinical uses
      • allergy
      • motion sickness
      • sleep aid
    • Toxicity
      • antimuscarinic
      • anti-α-adrenergic
      • sedation (lipophilic and thus crosses brain barrier)
  • 2nd generation
    • Drugs
      • loratadine (Claritin)
      • fexofenadine (Allegra)
      • cetirizine (Zyrtec)
      • desloratadine
    • Clinical uses
      • allergy
    • Toxicity
      • decreased entry into CNS (lipophobic) makes this generation far less sedating
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