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地氯雷他定的成人及儿童慢代谢者:药代动力学与安全性评估

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

作者信息

Prenner Bruce, Kim Kenneth, Gupta Samir, Khalilieh Sauzanne, Kantesaria Bhavna, Manitpisitkul Prasarn, Lorber Richard, Wang Zaiqi, Lutsky Barry

机构信息

Allergy Associates Medical Group, San Diego, CA 92120, USA.

出版信息

Expert Opin Drug Saf. 2006 Mar;5(2):211-23. doi: 10.1517/14740338.5.2.211.

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.

摘要

抗组胺药被广泛用于治疗成人和儿童的过敏性鼻炎(AR)和慢性特发性荨麻疹(CIU)。地氯雷他定是一种每日口服一次的抗组胺药,具有良好的镇静作用,已被批准用于治疗AR和CIU。已观察到地氯雷他定代谢存在表型多态性,即一些个体形成地氯雷他定主要代谢产物3-羟基地氯雷他定的能力下降;这些个体被称为“地氯雷他定代谢缓慢者”。本综述描述了地氯雷他定代谢缓慢者的患病率,量化了地氯雷他定代谢缓慢者对地氯雷他定的暴露量,并证明以适合年龄的剂量给药时,地氯雷他定代谢缓慢者的暴露量增加与年龄无关。此外,本综述表明,地氯雷他定代谢缓慢者对地氯雷他定的暴露量增加与地氯雷他定的安全性和耐受性概况的任何变化无关,包括心血管安全性。

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