PDF(Pubmed)
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：
骨关节炎代表着巨大的社会经济负担，并对日常生活和生产力产生重大影响。非甾体抗炎药（NSAIDs）广泛用于治疗骨关节炎，以抑制炎症，疼痛,和刚度，提高身体机能。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。非选择性环氧合酶（COX）抑制剂和环氧合酶-1（COX-1）抑制剂与由于前列腺素的抑制而增加的胃肠道不良反应有关。负责保护胃粘膜。环氧合酶-2（COX-2）抑制剂由于其在循环系统中的COX-2抑制活性而与心血管不良反应的发生率增加有关。因此,需要一种安全性更好的新型NSAID用于骨关节炎.波玛考昔是一个新的，口服活性，一类NSAID，是COX-2和碳酸酐酶（CA）的双重抑制剂。polmacoxib表现出的双重作用模式有望最大程度地减少不利的心血管作用，同时在发炎的骨关节炎关节中实现最大的有效性。本文旨在综述其药理特性,临床疗效,和波玛考昔在骨关节炎中的安全性数据。
