Adult and paediatric poor metabolisers of desloratadine: an assessment of pharmacokinetics and safety.

Abstract

Antihistamines are widely used to treat allergic rhinitis (AR) and chronic idiopathic urticaria (CIU) in adults and children. Desloratadine is a once-daily oral antihistamine with a favourable sedation profile that is approved for the treatment of AR and CIU. Phenotypic polymorphism in the metabolism of desloratadine has been observed, such that some individuals have a decreased ability to form 3-hydroxydesloratadine, the major metabolite of desloratadine; such individuals are termed 'poor metabolisers of desloratadine'. This review describes the prevalence of poor metabolisers of desloratadine, quantifies the exposure to desloratadine in poor metabolisers and demonstrates that the increased exposure in poor metabolisers is independent of age when administered at age-appropriate doses. Furthermore, this review demonstrates that the increased exposure to desloratadine in poor metabolisers is not associated with any changes in the safety and tolerability profile of desloratadine, including cardiovascular safety.

• Authors: Bruce Prenner, Kenneth Kim, Samir Gupta, Sauzanne Khalilieh, Bhavna Kantesaria, Prasarn Manitpisitkul, Richard Lorber, Zaiqi Wang, Barry Lutsky
• Journal: Expert opinion on drug safety (Expert Opin Drug Saf) Vol. 5 Issue 2 Pg. 211-23 (Mar 2006) ISSN: 1744-764X [Electronic] England
• PMID: 16503743 (Publication Type: Journal Article, Review)

Chemical References

• Histamine H1 Antagonists, Non-Sedating
• Loratadine
• desloratadine

Topics

• Administration, Oral
• Age Factors
• Dose-Response Relationship, Drug
• Electrocardiography
• Histamine H1 Antagonists, Non-Sedating (adverse effects, metabolism, pharmacokinetics, therapeutic use)
• Loratadine (adverse effects, analogs & derivatives, metabolism, pharmacokinetics, therapeutic use)
• Rhinitis, Allergic, Seasonal (drug therapy)
• Urticaria (drug therapy)