Cetirizine: more than an antihistamine? 1991

J Bernheim, and C Arendt, and C de Vos
UCB Pharmaceutical Sector, R & D, Chemin du Foriest, Braine l'Alleud, Belgium.

Cetirizine, a metabolite of hydroxyzine, is an antihistamine with as distinguishing features: 1) exquisite anti-H1 specificity: cetirizine appears unique in being devoid of action on receptors other than the H1 receptor; 2) potency: at unit dose it is the most potent antihistamine in the skin and the lung; 3) absence of metabolism. These three characteristics suggest that cetirizine be considered the choice H1 antagonist for experiments on the immediate allergic reaction. Cetirizine additionally in vitro inhibits the migration of eosinophils, and in vivo, in the skin, the infiltration by eosinophils that is characteristic for the late phase allergic reaction. Other antihistamines are less active or inactive with respect to this property. According to several lines of evidence, the effect of cetirizine on eosinophils is unlikely to be due to H1 antagonism, but is more likely a novel property of the compound.

UI MeSH Term Description Entries
D006967 Hypersensitivity Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen. Allergy,Allergic Reaction,Allergic Reactions,Allergies,Hypersensitivities,Reaction, Allergic,Reactions, Allergic
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D006633 Histamine Antagonists Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only. Antihistamine,Antihistamines,Histamine Antagonist,Antagonist, Histamine,Antagonists, Histamine
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
D006919 Hydroxyzine A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative. 2-(2-(4-((4-Chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)ethanol,Atarax,Durrax,Hydroxyzine Dihydrochloride,Hydroxyzine Hydrochloride,Hydroxyzine Pamoate,Orgatrax,Vistaril,Pamoate, Hydroxyzine
D000485 Allergens Antigen-type substances that produce immediate hypersensitivity (HYPERSENSITIVITY, IMMEDIATE). Allergen
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001249 Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL). Asthma, Bronchial,Bronchial Asthma,Asthmas
D015444 Exercise Physical activity which is usually regular and done with the intention of improving or maintaining PHYSICAL FITNESS or HEALTH. Contrast with PHYSICAL EXERTION which is concerned largely with the physiologic and metabolic response to energy expenditure. Aerobic Exercise,Exercise, Aerobic,Exercise, Isometric,Exercise, Physical,Isometric Exercise,Physical Activity,Acute Exercise,Exercise Training,Activities, Physical,Activity, Physical,Acute Exercises,Aerobic Exercises,Exercise Trainings,Exercise, Acute,Exercises,Exercises, Acute,Exercises, Aerobic,Exercises, Isometric,Exercises, Physical,Isometric Exercises,Physical Activities,Physical Exercise,Physical Exercises,Training, Exercise,Trainings, Exercise

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