Benedetti Margherita Strolin, Whomsley Rhys, Poggesi Italo, Cawello Willi, Mathy François-Xavier, Delporte Marie-Laure, Papeleu Peggy, Watelet Jean-Baptiste
UCB Pharma SA, Belgium.
Drug Metab Rev. 2009;41(3):344-90. doi: 10.1080/10837450902891295.
In this article, aspects of absorption, distribution, metabolism, and excretion have been described bearing in mind the pathogenesis of allergic diseases and their possible therapeutic opportunities. The importance of the routes of administration of the different therapeutic groups has been emphasized. The classical aspects of drug metabolism and disposition related to oral administration have been reviewed, but special emphasis has been given to intranasal, cutaneous, transdermal, and ocular administration as well as to the absorption and the subsequent bioavailability of drugs. Drug-metabolizing enzymes and transporters present in extrahepatic tissues, such as nasal mucosa and the respiratory tract, have been particularly discussed. As marketed antiallergic drugs include both racemates and enantiomers, aspects of stereoselective absorption, distribution, metabolism, and excretion have been discussed. Finally, a new and promising methodology, microdosing, has been presented, although it has not yet been applied to drugs used in the treatment of allergic diseases.
在本文中,我们在考虑过敏性疾病的发病机制及其可能的治疗机会的情况下,描述了吸收、分布、代谢和排泄等方面。强调了不同治疗组给药途径的重要性。回顾了与口服给药相关的药物代谢和处置的经典方面,但特别强调了鼻内、皮肤、透皮和眼部给药,以及药物的吸收和随后的生物利用度。特别讨论了存在于肝外组织(如鼻黏膜和呼吸道)中的药物代谢酶和转运蛋白。由于市售的抗过敏药物包括外消旋体和对映体,因此讨论了立体选择性吸收、分布、代谢和排泄等方面。最后,介绍了一种新的、有前景的方法——微剂量给药,尽管它尚未应用于用于治疗过敏性疾病的药物。