Nonsedating antihistamines: pharmacology, clinical efficacy and adverse effects. 1992

M A Kaliner
National Institute of Allergy and Infectious Diseases, Bethesda, Maryland.

Antihistamines are effective therapy for histamine-mediated conditions, including seasonal and perennial allergic rhinitis and chronic urticaria. Until recently, all antihistamines produced some degree of drowsiness, as well as anticholinergic side effects. Several nonsedating antihistamines have been developed. Two of these antihistamines--terfenadine and astemizole--are commercially available. The lack of central nervous system effects is attributed to the inability of these drugs to penetrate the blood-brain barrier. They also have no appreciable binding to cholinergic receptors. Clinical trials have demonstrated that the newer agents are as effective as classic antihistamines and that they have no greater incidence of central nervous system or anticholinergic side effects than placebo.

UI MeSH Term Description Entries
D006969 Hypersensitivity, Immediate Hypersensitivity reactions which occur within minutes of exposure to challenging antigen due to the release of histamine which follows the antigen-antibody reaction and causes smooth muscle contraction and increased vascular permeability. Atopic Hypersensitivity,Hypersensitivity, Atopic,Hypersensitivity, Type I,IgE-Mediated Hypersensitivity,Type I Hypersensitivity,Atopic Hypersensitivities,Hypersensitivities, Atopic,Hypersensitivities, IgE-Mediated,Hypersensitivities, Immediate,Hypersensitivities, Type I,Hypersensitivity, IgE-Mediated,IgE Mediated Hypersensitivity,IgE-Mediated Hypersensitivities,Immediate Hypersensitivities,Immediate Hypersensitivity,Type I Hypersensitivities
D003533 Cyproheptadine A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. Antergan,Dihexazin,Periactin,Peritol,Viternum
D006634 Histamine H1 Antagonists Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. Antihistamines, Classical,Antihistaminics, Classical,Antihistaminics, H1,Histamine H1 Antagonist,Histamine H1 Receptor Antagonist,Histamine H1 Receptor Antagonists,Histamine H1 Receptor Blockaders,Antagonists, Histamine H1,Antagonists, Histamine H1 Receptor,Antihistamines, Sedating,Blockaders, Histamine H1 Receptor,First Generation H1 Antagonists,H1 Receptor Blockaders,Histamine H1 Blockers,Receptor Blockaders, H1,Antagonist, Histamine H1,Classical Antihistamines,Classical Antihistaminics,H1 Antagonist, Histamine,H1 Antagonists, Histamine,H1 Antihistaminics,Sedating Antihistamines
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D016589 Astemizole Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects. Alermizol,Astemina,Astemizol Alonga,Astemizol Ratiopharm,Astesen,Emdar,Esmacen,Fustermizol,Hismanal,Histaminos,Hubermizol,Laridal,Paralergin,R-43-512,Retolen,Rifedot,Rimbol,Romadin,Simprox,Urdrim,Alonga, Astemizol,R 43 512,R43512,Ratiopharm, Astemizol
D016593 Terfenadine A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME. Balkis Saft Spezial,Cyater,Hisfedin,RMI-9918,Rapidal,Seldane,Teldane,Terfedura,Terfemundin,Terfenadin AL,Terfenadin Heumann,Terfenadin Stada,Terfenadin Von Ct,Terfenadin-Ratiopharm,Terfenidine,Ternadin,Triludan,alpha-(4-(1,1-Dimethylethyl)phenyl)-4-(hydroxydiphenylmethyl)-1-piperdinebutanol,RMI 9918,RMI9918,Terfenadin Ratiopharm
D017336 Loratadine A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness. 4-(8-Chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-1-piperidinecarboxylic Acid Ethyl Ester,Alavert,Claritin,Clarium,Sch-29851,Sch 29851,Sch29851

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