Antihistamines: pharmacology and clinical use

Drugs. 1976;12(4):258-73. doi: 10.2165/00003495-197612040-00002.


Antihistamines are a diverse group of drugs which possess the ability to inhibit various histaminic actions. By and large, they bear a certain structural resemblance to histamine, and act principally to prevent histamine-receptor interaction through competition with histamine for histamine receptors. Consequently, they are helpful therapeutically in preventing, rather than reversing, histaminic actions. Individual antihistaminic drugs act to inhibit histaminic action at one or another histamine receptor (H1 or H2-receptor), but not at both receptors. The large number of antihistaminics which have been available for many years and employed chiefly as 'antiallergic' drugs are classified as H1-receptor inhibitors; they are most effective therapeutically in inhibiting manifestations of histamine-induced wheal and erythema formation and pruritus. H2-receptor inhibitors, agents which are able to inhibit histamine-induced gastric acid secretion, have been developed more recently. Antihistaminics in general and H1-receptor inhibitors in particular, exert a wide variety of pharmacological activities. Their use is frequently accompanied by undesirable side-effects, notably CNS depression, dryness of mucous membranes, and gastrointestinal effects. Used judiciously and in proper dosage, antihistaminic drugs are helpful in the control of allergic disorders, allergic rhinitis and urticaria in particular; newly developed H2-receptor inhibitors show therapeutic promise in the treatment of peptic ulceration.

Publication types

  • Review

MeSH terms

  • Administration, Topical
  • Anaphylaxis / drug therapy
  • Asthma / drug therapy
  • Conjunctivitis / drug therapy
  • Drug Interactions
  • Drug Tolerance
  • Edema / drug therapy
  • Female
  • Histamine H1 Antagonists / administration & dosage
  • Histamine H1 Antagonists / adverse effects
  • Histamine H1 Antagonists / metabolism
  • Histamine H1 Antagonists / pharmacology*
  • Histamine H1 Antagonists / therapeutic use
  • Humans
  • Pregnancy
  • Pruritus / drug therapy
  • Rhinitis, Allergic, Seasonal / drug therapy
  • Structure-Activity Relationship
  • Time Factors
  • Urticaria / drug therapy


  • Histamine H1 Antagonists