Adult and paediatric poor metabolisers of desloratadine: an assessment of pharmacokinetics and safety.
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.
Prenner
Bruce
B
Allergy Associates Medical Group, San Diego, CA 92120, USA. prenner@aaamg.com
Kim
Kenneth
K
Gupta
Samir
S
Khalilieh
Sauzanne
S
Kantesaria
Bhavna
B
Manitpisitkul
Prasarn
P
Lorber
Richard
R
Wang
Zaiqi
Z
Lutsky
Barry
B
D000284:Administration, Oral; D000367:Age Factors; D004305:Dose-Response Relationship, Drug; D004562:Electrocardiography; D039563:Histamine H1 Antagonists, Non-Sedating / Q000009:adverse effects / Q000378:metabolism* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D017336:Loratadine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use; D006255:Rhinitis, Allergic, Seasonal / Q000188:drug therapy; D014581:Urticaria / Q000188:drug therapy
D039563:Histamine H1 Antagonists, Non-Sedating; D017336:Loratadine; C121345:desloratadine