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依美昔布:药理学与治疗学的新进展。

Imrecoxib: Advances in Pharmacology and Therapeutics.

机构信息

Department of Pharmacy, the Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, Zhejiang Province, People's Republic of China.

VIP Geriatric Ward, Division of Nursing, the Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, Zhejiang Province, People's Republic of China.

出版信息

Drug Des Devel Ther. 2024 May 22;18:1711-1725. doi: 10.2147/DDDT.S464485. eCollection 2024.

Abstract

Imrecoxib, a cyclooxygenase-2 (COX-2) selective non-steroidal anti-inflammatory drug (NSAID), was discovered via the balanced inhibition strategy of COX-1/COX-2. It is indicated for the relief of painful symptoms of osteoarthritis. There have been some pharmacological and therapeutic advances since the approval of imrecoxib in 2011. However, an update review in this aspect is not yet available. Relevant literature until January 2024 was identified by search of PubMed, Web of science, Embase and CNKI. From the perspective of efficacy, imrecoxib provides relief of osteoarthritis symptoms, and potential off-label use for treatment of idiopathic pulmonary fibrosis, perioperative pain, hand-foot syndrome, axial spondyloarthritis, COVID-19, cartilage injury, and malignancies such as lung and colon cancer. From a safety point of view, imrecoxib showed adverse effects common to NSAIDs; however, it has lower incidence of new-onset hypertension than other types of selective COX-2 inhibitors, less gastrointestinal toxicities than non-selective NSAIDs, weaker risk of drug interaction than celecoxib, and more suitable for elderly patients due to balanced inhibition of COX-1/COX-2. From a pharmacoeconomic perspective, imrecoxib is more cost-effective than celecoxib and diclofenac for osteoarthritis patients. With the deepening of the disease pathophysiology study of osteoarthritis, new therapeutic schemes and pharmacological mechanisms are constantly discovered. In the field of osteoarthritis treatment, mechanisms other than the analgesic and anti-inflammatory effects of COX-2 inhibitors are also being explored. Taken together, imrecoxib is a moderate selective COX-2 inhibitor with some advantages, and there would be more clinical applications and research opportunities in the future.

摘要

依托昔布是一种环氧化酶-2(COX-2)选择性非甾体抗炎药(NSAID),通过 COX-1/COX-2 的平衡抑制策略发现。它用于缓解骨关节炎的疼痛症状。自 2011 年依托昔布获得批准以来,已经有了一些药理学和治疗学方面的进展。然而,在这方面还没有更新的综述。通过在 PubMed、Web of Science、Embase 和中国知网(CNKI)上搜索,确定了截至 2024 年 1 月的相关文献。从疗效的角度来看,依托昔布能缓解骨关节炎症状,还有治疗特发性肺纤维化、围手术期疼痛、手足综合征、中轴型脊柱关节炎、COVID-19、软骨损伤和肺癌、结肠癌等恶性肿瘤的潜在适应证。从安全性的角度来看,依托昔布表现出与 NSAIDs 常见的不良反应;然而,与其他类型的选择性 COX-2 抑制剂相比,它的新发高血压发生率较低,与非选择性 NSAIDs 相比,胃肠道毒性较小,与塞来昔布相比,药物相互作用的风险较弱,并且由于 COX-1/COX-2 的平衡抑制,更适合老年患者。从药物经济学的角度来看,依托昔布治疗骨关节炎患者比塞来昔布和双氯芬酸更具成本效益。随着骨关节炎疾病病理生理学研究的深入,新的治疗方案和药理学机制不断被发现。在骨关节炎治疗领域,也在探索 COX-2 抑制剂除了镇痛和抗炎作用之外的机制。总的来说,依托昔布是一种中等选择性 COX-2 抑制剂,具有一些优势,在未来会有更多的临床应用和研究机会。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbc5/11128231/d10a21e4afbb/DDDT-18-1711-g0001.jpg

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