Antihistaminesin Skin Disease and Care

  • Competitive inhibitor (reversible) of histamine at tissue receptor sites; H1 and H2 blockers
  • H1 antihistamines divided into first and second generation
  • First generation: diphenhydramine, promethazine, cyproheptadine, chlorpheniramine, hydroxyzine
    • SE: drowsiness and anticholinergic symptoms (blurry vision, urinary retention, dry mouth, constipation)
    • Cyproheptadine: treatment of choice for cold urticaria
    • Chlorpheniramine: safest in pregnancy
    • Hydroxyzine: side effects include EKG changes, arrhythmias
  • Second generation: fexofenadine, loratidine, cetirizine, levocetirizine
    • SE: drowsiness and anticholinergic symptoms
    • Fexofenadine: few sedative effects, few to no anticholinergic symptoms, category C
    • Loratidine: long-acting, minimally sedating, category B
    • Cetirizine: low sedation, metabolite of hydroxyzine, ± anticholinergic effect, category B
  • H2 antihistamines (cimetidine, ranitidine)
    • Cimetidine: competitively inhibits DHT at androgen receptor site (side effects include gynecomastia, impotence, loss of libido)
  • Others
    • Doxepin: tricyclic antidepressant, H1/H2 antihistamine, inhibits histamine and acetylcholine, anticholinergic, cardiotoxic (may prolong QT interval); side effects: conduction disturbances, seizure disorder, urinary retention
    • Amitryptaline: tricyclic antidepressant with some H1 blocking activity, side effects include anticholinergic symptoms and risk of cardiac arrhythmias
    • Cromolyn sodium: blocks mast cell degranulation
    • Montelukast, zafirlukast: leukotriene receptor antagonist
    • Zileuton: inhibitor of 5-lipoxygenase, which subsequently inhibits leukotriene formation