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氯雷他定:对其药理特性及在过敏性疾病治疗应用的重新评估

Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders.

作者信息

Haria M, Fitton A, Peters D H

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1994 Oct;48(4):617-37. doi: 10.2165/00003495-199448040-00009.

DOI:10.2165/00003495-199448040-00009
PMID:7528133
Abstract

Loratadine is a long-acting antihistamine agent, exhibiting partial selectivity for peripheral histamine H1-receptors. To date, loratadine has been evaluated in allergic rhinitis, urticaria and, to a limited extent, in asthma. In several large controlled comparative clinical studies, loratadine was superior to placebo, faster acting than astemizole and as effective as azatadine, cetirizine, chlorpheniramine (chlorphenamine), clemastine, hydroxyzine, mequitazine and terfenadine in patients with allergic rhinitis and chronic urticaria. The clinical effectiveness of loratadine in asthma is at present unclear. Loratadine is well tolerated. At dosages of 10 mg daily, commonly reported adverse events were somnolence, fatigue and headache. Sedation occurred less frequently with loratadine than with azatadine, cetirizine, chlorpheniramine, clemastine and mequitazine. Serious ventricular arrhythmias, as reported with some other second generation histamine H1-receptor antagonists, have not been observed with loratadine to date. Thus, loratadine, with its attributes of once daily administration, fast onset of action and essentially nonsedating properties, would appear to be an appropriate first-line agent for the treatment of allergic rhinitis or urticaria.

摘要

氯雷他定是一种长效抗组胺药,对外周组胺H1受体具有部分选择性。迄今为止,已对氯雷他定在过敏性鼻炎、荨麻疹以及在一定程度上在哮喘中的应用进行了评估。在几项大型对照比较临床研究中,在过敏性鼻炎和慢性荨麻疹患者中,氯雷他定优于安慰剂,起效比阿司咪唑快,且与阿扎他定、西替利嗪、氯苯那敏、氯马斯汀、羟嗪、美喹他嗪和特非那定效果相当。氯雷他定在哮喘中的临床疗效目前尚不清楚。氯雷他定耐受性良好。每日剂量为10毫克时,常见的不良事件为嗜睡、疲劳和头痛。氯雷他定引起的镇静作用比阿扎他定、西替利嗪、氯苯那敏、氯马斯汀和美喹他嗪少见。迄今为止,尚未观察到氯雷他定出现一些其他第二代组胺H1受体拮抗剂所报道的严重室性心律失常。因此,氯雷他定具有每日一次给药、起效快且基本无镇静作用的特点,似乎是治疗过敏性鼻炎或荨麻疹的合适一线药物。

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Duration of effect of loratadine and terfenadine administered once a day for one week on cutaneous and inhaled reactivity to histamine.每日一次服用氯雷他定和特非那定一周对皮肤和吸入组胺反应性的作用持续时间。
Chest. 1993 Mar;103(3):777-81. doi: 10.1378/chest.103.3.777.
2
Mechanism of the cardiotoxic actions of terfenadine.特非那定心脏毒性作用的机制。
JAMA. 1993;269(12):1532-6.
3
[Effectiveness of loratadine vs. placebo in the treatment of urticaria-angioedema syndrome in patients with food allergy].氯雷他定与安慰剂治疗食物过敏患者荨麻疹-血管性水肿综合征的疗效对比
氯雷他定作为一种抗艰难梭菌毒素B的抗炎剂。
J Infect Dis. 2024 Sep 23;230(3):545-557. doi: 10.1093/infdis/jiae021.
4
Cationic amphiphilic drugs induce accumulation of cytolytic lysoglycerophospholipids in the lysosomes of cancer cells and block their recycling into common membrane glycerophospholipids.阳离子两亲性药物诱导溶酶体中细胞毒性溶血甘油磷脂在癌细胞中的积累,并阻止它们循环回常见的膜甘油磷脂中。
Mol Biol Cell. 2024 Mar 1;35(3):ar25. doi: 10.1091/mbc.E23-06-0263. Epub 2023 Dec 20.
5
Solubility and Physical Stability Enhancement of Loratadine by Preparation of Co-Amorphous Solid Dispersion with Chlorpheniramine and Polyvinylpyrrolidone.通过与氯苯那敏和聚乙烯吡咯烷酮制备共无定形固体分散体提高氯雷他定的溶解度和物理稳定性
Pharmaceutics. 2023 Oct 31;15(11):2558. doi: 10.3390/pharmaceutics15112558.
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A systematic review and meta-analysis of loratadine combined with montelukast for the treatment of allergic rhinitis.氯雷他定联合孟鲁司特治疗变应性鼻炎的系统评价和Meta分析
Front Pharmacol. 2023 Oct 17;14:1287320. doi: 10.3389/fphar.2023.1287320. eCollection 2023.
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Simultaneous Determination of Loratadine and Its Metabolite Desloratadine in Beagle Plasma by LC-MS/MS and Application for Pharmacokinetics Study of Loratadine Tablets and Omeprazole‑Induced Drug-Drug Interaction.LC-MS/MS 法同时测定比格犬血浆中氯雷他定及其代谢物去氯雷他定浓度及其在氯雷他定片和奥美拉唑诱导的药物相互作用中的药代动力学研究。
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Comparative study of the efficacy and safety of loratadine syrup and terfenadine suspension in the treatment of chronic allergic skin diseases in a pediatric population.氯雷他定糖浆与特非那定混悬液治疗儿童慢性过敏性皮肤病的疗效及安全性比较研究
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Effect of loratadine on human eosinophil function in vitro.氯雷他定对人嗜酸性粒细胞体外功能的影响。
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