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选择性环氧化酶2(COX-2)抑制剂是治疗类风湿关节炎和骨关节炎的一类新型非甾体抗炎药(NSAIDs)。选择性COX-2抑制剂分为倾向性COX-2抑制剂(美洛昔康、尼美舒利和双氯芬酸等)和特异性COX-2抑制剂(塞来昔布、罗非昔布、伐地考昔、依托考昔等),前者对COX-2的抑制作用明显大于对COX-1的抑制作用,但在抑制COX-2的同时也会部分抑制COX-1,后者仅对COX-2有强烈抑制作用。选择性COX-2抑制剂的主要不良反应为消化道溃疡、穿孔或出血,肾功能损伤,凝血功能障碍,以及血栓形成等。其机制与选择性COX-2抑制剂能同时抑制COX-1和COX-2,减弱其对消化道黏膜的保护作用、使肾小球滤过率下降而加重钠钾潴留、抑制细胞色素P4502C9酶活性而降低华法林代谢率以及影响血栓素A2和前列腺素I2的平衡等有关。同时服用选择性COX-2抑制剂与质子泵抑制剂可降低消化道不良反应的发生率;高血压病患者或有水钠潴留倾向者服用选择性COX-2抑制剂时,应定期监测血药浓度及肾功能,调整降压药剂量,避免多种NSAIDs同时应用;选择性COX-2抑制剂与小剂量阿司匹林联合应用可防治心血管不良反应。一旦出现不良反应,应立即停药并对症治疗。
Selective cyclooxygenase 2 (COX-2) inhibitors are a new class of non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of rheumatoid arthritis and osteoarthritis. Selective COX-2 inhibitors are classified into pro-active COX-2 inhibitors (meloxicam, nimesulide and diclofenac, etc.) and specific COX-2 inhibitors (celecoxib, rofecoxib, Etoposide, etc.), the former of the inhibition of COX-2 was significantly greater than the inhibition of COX-1, but in the inhibition of COX-2 also partially inhibited COX-1, the latter only strongly inhibited COX-2 effect. The main adverse effects of selective COX-2 inhibitors are peptic ulcer, perforation or bleeding, renal dysfunction, coagulopathy, and thrombosis. The mechanism and selective COX-2 inhibitors can inhibit both COX-1 and COX-2 at the same time, weaken their protective effect on gastrointestinal mucosa, decrease glomerular filtration rate, increase sodium-potassium retention and inhibit cytochrome P4502C9 enzyme Activity and reduce the metabolic rate of warfarin and affect the balance of thromboxane A2 and prostaglandin I2 and so on. At the same time taking selective COX-2 inhibitors and proton pump inhibitors can reduce the incidence of gastrointestinal adverse reactions; hypertension or patients with Shuinazhuliu preferred selective COX-2 inhibitors should be regularly monitored blood Concentration and renal function, adjust the dose of antihypertensive drugs, to avoid the simultaneous application of multiple NSAIDs; selective COX-2 inhibitors and low-dose aspirin combination can prevent cardiovascular adverse reactions. In the event of adverse reactions, should be immediately discontinued and symptomatic treatment.