Department of Medicine.
J Asthma Allergy. 2008 Sep 19;1:19-29. doi: 10.2147/jaa.s3092.
Fexofenadine is a selective, non-sedating H1 receptor antagonist, marketed in the United States since 2000. The FDA approved an oral suspension in 2006, for the treatment of seasonal allergic rhinitis and chronic idiopathic urticaria in children. The tablet, capsule, and oral suspension are bioequivalent. Although fexofenadine does not use P450 CYP 3A4 it does interact with a number of drugs at P-glycoprotein and organic anion transporter polypeptides. The risk of toxicity from other drugs may increase with the administration of fexofenadine. Orange and grapefruit juices reduce the bioavailability of fexofenadine. Fexofenadine has been shown to have an impact on inflammatory mediators, other than histamine, such as decreasing the production of LTC(4), LTD(4), LTE(4), PGE(2), and PGF(2α); inhibiting cyclo-oxygenase 2, thromboxane; limiting iNOS generation of NO; decreasing cytokine levels (ICAM-1, ELAM-1, VCAM-1, RANTES, I-TAC, MDC, TARC, MMP-2, MMP-9, tryptase); and diminishing eosinophil adherence, chemotaxis, and opsonization of particles. These effects may provide benefit to some of the inflammatory responses of an acute allergic reaction and provide a basis for future development of H1 antagonists with stronger anti-inflammatory effects. These studies also support the contention that fexofenadine is effective for the treatment of allergic rhinits and chronic idiopathic urticaria.
非索非那定是一种选择性、非镇静的 H1 受体拮抗剂，自 2000 年以来在美国上市。2006 年，FDA 批准了其口服混悬剂，用于治疗儿童季节性过敏性鼻炎和慢性特发性荨麻疹。片剂、胶囊和口服混悬剂具有生物等效性。虽然非索非那定不使用 P450 CYP 3A4，但它确实与许多药物在 P-糖蛋白和有机阴离子转运多肽上相互作用。与非索非那定联合使用可能会增加其他药物的毒性风险。橙汁和葡萄柚汁会降低非索非那定的生物利用度。非索非那定已被证明除了组胺之外，对其他炎症介质也有影响，如减少 LTC(4)、LTD(4)、LTE(4)、PGE(2)和 PGF(2α)的产生；抑制环氧化酶 2、血栓素；限制 iNOS 生成 NO；降低细胞因子水平（ICAM-1、ELAM-1、VCAM-1、RANTES、I-TAC、MDC、TARC、MMP-2、MMP-9、胰蛋白酶）；并减少嗜酸性粒细胞的黏附、趋化性和颗粒的调理作用。这些作用可能对急性过敏反应的一些炎症反应有益，并为未来开发具有更强抗炎作用的 H1 拮抗剂提供了依据。这些研究也支持了非索非那定对过敏性鼻炎和慢性特发性荨麻疹治疗有效的观点。
