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泊马昔布:新型非甾体抗炎药治疗骨关节炎的综述

Polmacoxib: A Review of the Newer Non-steroidal Anti-inflammatory Drug in Osteoarthritis.

作者信息

Easwaran Raju, Mistry Urvi K, Bhole Milind, Peethambaran Kartik

机构信息

Orthopaedics and Traumatology, Shree Meenakshi Orthopaedics and Sports Medicine Clinic, New Delhi, IND.

Established Pharmaceuticals Division, Abbott Healthcare Pvt. Ltd., Mumbai, IND.

出版信息

Cureus. 2024 Apr 17;16(4):e58446. doi: 10.7759/cureus.58446. eCollection 2024 Apr.

Abstract

Osteoarthritis represents a huge socioeconomic burden and has a significant impact on daily life and productivity. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used in the management of osteoarthritis to curb inflammation, pain, and stiffness and improve physical function. However, due to the various side effects, most healthcare professionals avoid using NSAIDs for a long period. Nonselective cyclooxygenase (COX) inhibitors and cyclooxygenase-1 (COX-1) inhibitors are associated with increased gastrointestinal adverse effects due to the inhibition of prostaglandins, which are responsible for protecting the gastric mucosa. Cyclooxygenase-2 (COX-2) inhibitors are associated with an increased incidence of adverse cardiovascular effects due to their COX-2 inhibitory activity in the circulatory system. Therefore, there is a need for a newer NSAID that has a better safety profile to be used in osteoarthritis. Polmacoxib is a new, orally active, first-in-class NSAID that is a dual inhibitor of COX-2 and carbonic anhydrase (CA). The dual mode of action exhibited by polmacoxib is expected to minimize adverse cardiovascular effects while achieving maximum effectiveness in inflamed osteoarthritic joints. This article aims to review the pharmacological properties, clinical efficacy, and safety data of polmacoxib in osteoarthritis.

摘要

骨关节炎带来了巨大的社会经济负担,对日常生活和生产力产生了重大影响。非甾体抗炎药(NSAIDs)被广泛用于骨关节炎的治疗,以抑制炎症、疼痛和僵硬,并改善身体功能。然而,由于各种副作用,大多数医疗保健专业人员避免长期使用NSAIDs。非选择性环氧化酶(COX)抑制剂和环氧化酶-1(COX-1)抑制剂由于抑制了负责保护胃黏膜的前列腺素,会增加胃肠道不良反应。环氧化酶-2(COX-2)抑制剂由于其在循环系统中的COX-2抑制活性,会增加不良心血管事件的发生率。因此,需要一种安全性更好的新型NSAIDs用于骨关节炎的治疗。泊马昔布是一种新型的、口服活性的、同类首创的NSAIDs,它是COX-2和碳酸酐酶(CA)的双重抑制剂。预计泊马昔布表现出的双重作用模式将在最大程度减少不良心血管影响的同时,在发炎的骨关节炎关节中实现最大疗效。本文旨在综述泊马昔布在骨关节炎中的药理特性、临床疗效和安全性数据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3971/11099947/132851589f7d/cureus-0016-00000058446-i01.jpg

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