Analyzing the clinical efficacy and safety of levocetirizine based on its receptor occupancy, intraclass comparison and role in the treatment of CSU: an AROG consensus statement.

IF 3.6 3区 医学 Q2 PHARMACOLOGY & PHARMACY Expert Review of Clinical Pharmacology Pub Date : 2024-09-12 DOI:10.1080/17512433.2024.2401093
Kabir Sardana, C R Srinivasan, Mukesh Girdhar, Neirita Hazarika, Krina Patel, Narayan Rao, Akshay Jain, Jaspriya Sandhu, Shivani Bansal, Sunil Ghate, Rizwan Haq, Dhruv Premy Agarwal
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Abstract

Introduction: Chronic spontaneous urticaria (CSU) is characterized by urticaria persisting for more than 6 weeks. Antihistamines, notably sgAH (second generation antihistamines) are the first line of treatment for CSU.

Areas covered: This consensus aimed to review the existing research on receptor occupancy of antihistamines, including levocetirizine, and translate its implications in the treatment of CSU. The consensus deliberations were under the banner of the Antihistamine Receptor Occupancy Group (AROG) from India, an expert panel of 12 dermatologists with a mix of institutional and practitioner backgrounds. This group analyzed the existing translational research on the receptor occupancy of levocetirizine to establish the clinical efficacy and safety of levocetirizine in the treatment of CSU using the grading of recommendations assessment, development, and evaluation (GRADE) method vis-a-vis the varied SGAH.

Expert opinion: SGAH constitute the first step in the therapeutic ladder for managing CSU. Levocetirizine has high bioavailability, high affinity and occupancy of the H1 receptor, rapid onset of action, limited distribution and minimal hepatic metabolism. It exhibits significant anti-inflammatory effects at clinically relevant concentrations. The marked receptor occupancy translates to enhanced efficacy as compared to similarly dosed SGAH with the lower cost making it an appropriate drug for chronic use. Receptor occupancy should be the basis of intra-class head-to-head trials in CSU.

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根据左西替利嗪的受体占据率、类内比较和在 CSU 治疗中的作用分析其临床疗效和安全性:AROG 共识声明。
导言:慢性自发性荨麻疹(CSU)的特征是荨麻疹持续6周以上,并导致严重的发病率。抗组胺药,尤其是第二代抗组胺药(sgAH)是治疗 CSU 的一线药物:本共识旨在回顾有关抗组胺药(包括左西替利嗪)受体占用的现有转化研究,并确定其在 CSU 治疗中的作用。该共识由来自印度的抗组胺药受体占位小组(AROG)牵头,该小组由来自不同地区的十二名皮肤科专家组成,他们具有不同的机构和从业背景。该共识分析了现有关于左西替利嗪受体占位的转化研究,采用建议评估、开发和评价分级(GRADE)方法,与不同的SGAH.专家意见相比,确定了左西替利嗪治疗CSU的临床疗效和安全性:第二代抗组胺药是治疗CSU的第一步。左西替利嗪的生物利用度高,对H1受体的亲和力和占据率高,起效迅速,分布有限,肝脏代谢极少。在临床相关浓度下,它具有明显的抗炎作用。与类似剂量的 SGAH 相比,其明显的受体占有率可转化为更好的疗效,而且分子成本较低,适合长期使用。受体占用率应作为 CSU 类内头对头试验的基础。
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来源期刊
Expert Review of Clinical Pharmacology
Expert Review of Clinical Pharmacology PHARMACOLOGY & PHARMACY-
CiteScore
7.30
自引率
2.30%
发文量
127
期刊介绍: Advances in drug development technologies are yielding innovative new therapies, from potentially lifesaving medicines to lifestyle products. In recent years, however, the cost of developing new drugs has soared, and concerns over drug resistance and pharmacoeconomics have come to the fore. Adverse reactions experienced at the clinical trial level serve as a constant reminder of the importance of rigorous safety and toxicity testing. Furthermore the advent of pharmacogenomics and ‘individualized’ approaches to therapy will demand a fresh approach to drug evaluation and healthcare delivery. Clinical Pharmacology provides an essential role in integrating the expertise of all of the specialists and players who are active in meeting such challenges in modern biomedical practice.
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