New oral H1 antihistamines in children: facts and unmeet needs

• Published in: Allergy 2008-10, Vol.63 (10), p.1395-1404
• Main Authors: de Benedictis, F.M, de Benedictis, D, Canonica, G.W
• Format: Article
• Language: English
• Subjects: Administration, Oral; antihistamines; Child; children; Children & youth; Evidence-Based Medicine; Histamine; Histamine H1 Antagonists, Non-Sedating - administration & dosage; Histamine H1 Antagonists, Non-Sedating - adverse effects; Histamine H1 Antagonists, Non-Sedating - pharmacokinetics; Histamine H1 Antagonists, Non-Sedating - therapeutic use; Humans; Hypersensitivity - drug therapy; Hypersensitivity - metabolism; Infant; Kinetics; Pharmacology; Receptors, Histamine H1 - genetics; Receptors, Histamine H1 - metabolism; Side effects
• ISSN: 0105-4538; 1398-9995; 0108-1675
• DOI: 10.1111/j.1398-9995.2008.01771.x

Second-generation antihistamines differ from first-generation ones because of their elevated specificity and affinity for peripheral H1-receptors and because of their lower penetration to the central nervous system, having fewer sedative effects as a result. Over the last few years, new compounds with different pharmacokinetic properties have been synthesized. More recent improvements of the molecules, generally in the form of active metabolites, led to the synthesis of new-generation antihistamines. Recommendations on the minimum criteria that would have to be met for compounds to be classified as new-generation antihistamines have been recently established by a consensus statement. In the past, the pharmacokinetics and pharmacodynamics of H1 antihistamines have not been optimally investigated in the pediatric population, especially in infants and young children. The pharmacology of second-generation H1 antihistamines has been investigated relatively deeper than old antihistamines in children. In the pediatric population, clinical studies with new-generation antihistamines are still limited in number and, with rare exceptions, of brief duration. Comparative trials on the efficacy and safety between different compounds are also lacking. Properly designed, long-term trials with new-generation H1 antihistamines need to be performed in single age groups, in order to better define the effects of these drugs in all pediatric population.