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- W2046236013 abstract "Ketotifen is an oral antiallergic drug developed in 1970 by Sandoz Pharmaceuticals of Switzerland. It is a benzocycloheptathiophene derivative and was initially marketed as an inhibitor of anaphylaxis. [1] Kamide R. Niimura M. Ueda H. et al. Clinical evaluation of ketotifen for chronic urticaria: multicenter double-blind comparative study with clemastine. Ann Allergy. 1989; 62: 322-325 PubMed Google Scholar The pharmacodynamic properties of ketotifen are many, because it is an inhibitor of the release and/or activity of mast cell and basophil mediators, including histamine, neutrophil, and eosinophil chemotactic factors, arachidonic acid metabolites, prostaglandins, and leukotrienes. [2] St-Pierre J.P. Kobric M. Rackham A. Effect of ketotifen treatment on cold-induced urticaria. Ann Allergy. 1985; 55: 840-843 PubMed Google Scholar Thus, it inhibits the bronchial response to inhaled histamine, allergen, or aspirin. In addition, the ocular, nasal, and dermal responses to applied allergen in sensitized patients are attenuated with use of ketotifen. [3] Grant S.M. Goa K.L. Fitton A. Sorkin E.M. Ketotifen. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma and allergic disorders. Drugs. 1990; 40: 412-448 Crossref PubMed Scopus (192) Google Scholar It also has been found to have some calcium antagonist activity and to inhibit responses to platelet-activating factor from proinflammatory cells, such as eosinophils. [2] St-Pierre J.P. Kobric M. Rackham A. Effect of ketotifen treatment on cold-induced urticaria. Ann Allergy. 1985; 55: 840-843 PubMed Google Scholar Additional possible modes of action include its ability to reverse β2-agonist–induced decreases in β-adrenoreceptor density and to alter the affinity of these receptors and increase intracellular concentrations of cyclic adenosine monophosphate. [3] Grant S.M. Goa K.L. Fitton A. Sorkin E.M. Ketotifen. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma and allergic disorders. Drugs. 1990; 40: 412-448 Crossref PubMed Scopus (192) Google Scholar Ketotifen has a chemical structure similar to some first-generation antihistamines, such as cyproheptadine and azatidene. [2] St-Pierre J.P. Kobric M. Rackham A. Effect of ketotifen treatment on cold-induced urticaria. Ann Allergy. 1985; 55: 840-843 PubMed Google Scholar With regard to the pharmacokinetic properties of ketotifen, it is readily absorbed from the gastrointestinal tract after oral administration and achieves peak plasma concentrations within 2 to 4 hours of administration. Clearance of the drug from plasma is biphasic, with a half-life of distribution of 3 hours and a half-life of elimination of 22 hours in adults. [3] Grant S.M. Goa K.L. Fitton A. Sorkin E.M. Ketotifen. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma and allergic disorders. Drugs. 1990; 40: 412-448 Crossref PubMed Scopus (192) Google Scholar However, the onset of action of ketotifen is slow, and it may take 4 to 6 weeks to achieve full prophylactic value under certain conditions. [4] Karaayvaz M. Calişkaner Z. Turan M. Akar A. Oztürk S. Ozangüç N. Levothyroxine versus ketotifen in the treatment of patients with chronic urticaria and thyroid autoimmunity. J Dermatol Treat. 2002; 13: 165-172 Crossref PubMed Scopus (10) Google Scholar" @default.
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- W2046236013 title "Ketotifen in the management of chronic urticaria: resurrection of an old drug" @default.
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