An exogenous agent that inhibits the release of histamine, the amino acid derivative that stimulates vasodilation and permeability under many circumstances, particularly tissue irritation. The most common type of antihistamine, the H1 receptor antagonist, produces many moderate side effects, and the H2 receptor antagonist cimetidine is even more problematic. That they are so commonly used can lull both physician and patient into trivializing their iatrogenic potential. Histamines, which are most abundant in the skin, respiratory, and GI tract mucus membranes, help heal; using antihistamines to inhibit the healing response for the whole body simply in order to lessen the acute but physiologically superficial symptoms of something like hay fever is to risk many subtle side effects.
n. a drug that inhibits the action of *histamine by blocking specific histamine receptors. Four histamine receptors have been identified (H1 to H4). H1-receptor antagonists are used for symptomatic relief of allergic conditions, such as hay fever, pruritus (itching), and urticaria (nettle rash). Many H1-receptor antagonists, e.g. *cyclizine and *promethazine, also have a strong *antiemetic activity and are used to prevent motion sickness. The most common side-effect of these drugs, especially the older antihistamines (e.g. *alimemazine, promethazine), is drowsiness and because of this they are sometimes used for sedation. Newer antihistamines, e.g. cetirizine, loratidine, mizolastine, are less sedating. Other side-effects include dizziness, blurred vision, tremors, digestive upsets, and lack of muscular coordination.
H2 receptors are mainly found in the stomach, where stimulation by histamine causes secretion of acid gastric juice. H2-receptor antagonists (e.g. *cimetidine, *nizatidine, *ranitidine, and *famotidine) block these receptors and reduce gastric acid secretion; they are used in the treatment of functional dyspepsia, *peptic ulcers, and *gastro-oesophageal reflux disease. H3- and H4-receptor antagonists have yet to find a clinical role.
treats allergic conditions; counteracts effects of histamine (which produces capillary dilation and, in larger doses, haemoconcentration).