Indian Journal of Dermatology
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SYMPOSIUM
Year : 2013  |  Volume : 58  |  Issue : 3  |  Page : 219-224

Pharmacology of antihistamines


1 Allergie Centrum Charité/ECARF, Charité Universitätsmedizin Berlin, Germany
2 Highlands Medical Centre, Fareham, Hampshire, Germany

Correspondence Address:
Martin K Church
Department of Dermatology and Allergy, Charité Universitätsmedizin Berlin, Charitéplatz 1, D 10117 Berlin
Germany
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Source of Support: Martin Church has been a speaker or consultant for Almirall, FAES Pharma, Menarini, MSD, UCB Pharma, Sanofi-Aventis, and Uriach. Diana Church has no conflict of interest., Conflict of Interest: None


DOI: 10.4103/0019-5154.110832

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H 1- antihistamines, the mainstay of treatment for urticaria, were developed from anticholinergic drugs more than 70 years ago. They act as inverse agonists rather than antagonists of histamine H 1 -receptors which are members of the G-protein family. The older first generation H 1- antihistamines penetrate readily into the brain to cause sedation, drowsiness, fatigue and impaired concentration and memory causing detrimental effects on learning and examination performance in children and on impairment of the ability of adults to work and drive. Their use should be discouraged. The newer second-generation H 1 -antihistamines are safer, cause less sedation and are more efficacious. Three drugs widely used for symptomatic relief in urticaria, desloratadine, levocetirizine and fexofenadine are highlighted in this review. Of these levocetirizine and fexofenadine are the most potent in humans in vivo. However, levocetirizine may cause somnolence in susceptible individuals, whereas fexofenadine has a relatively short duration of action and may be required to be given twice daily for all round daily protection. Although desloratadine is less potent, it has the advantages of rarely causing somnolence and having a long duration of action.


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