Jan 1, 1976

Antihistamines: pharmacology and clinical use

D S Pearlman


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...Continue Reading

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Mentioned in this Paper

Structure-Activity Relationship
Drug Tolerance
Administration, Topical
Antihistamines, Classical
Drug Interactions

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