Lane N E
Department of Medicine, University of California at San Francisco 94143, USA.
J Rheumatol Suppl. 1997 Jul;49:20-4.
Pain is the major symptom that leads patients to consult their physicians for the treatment of arthritis; therefore, effective pain control is an important goal in the management of this disorder. Pharmacologic therapy begins with simple analgesics and education. In many patients, simple analgesics do not adequately control moderate arthritis pain, and nonsteroidal antiinflammatory drugs (NSAID) are substituted for or added to the analgesic therapy. While NSAID are effective in controlling pain in mild to moderate osteoarthritis (OA), they are associated with significant toxicity (most frequently gastrointestinal) and may even cause complications that result in death. Patients who experience the pain associated with arthritis would therefore benefit from the antiinflammatory and analgesic actions of agents that are devoid of significant toxicities. Cyclooxygenase-2 (COX-2) inhibitors are being evaluated in clinical trials or are in development. These agents appear to inhibit only the COX-2 isoenzyme, which is produced largely during inflammation and is responsible for the biosynthesis of prostaglandins and other mediators of inflammation as well as sensitizers to pain. Because COX-2 inhibitors do not inhibit COX-1 isoenzyme activity at pharmacologic concentrations, they are devoid of many of the toxicities that are typical side effects of NSAID. Short term studies in dental pain, OA, and rheumatoid arthritis found that the COX-2 inhibitor celecoxib was an effective analgesic but did not cause gastroduodenal erosions. It has the potential to provide analgesia and antiinflammatory action in patients with arthritis without the side effects of NSAID. Further studies are required to substantiate these findings.
疼痛是导致患者因关节炎而就医治疗的主要症状;因此,有效控制疼痛是这种疾病管理中的一个重要目标。药物治疗从简单的镇痛药和教育开始。在许多患者中,简单的镇痛药不能充分控制中度关节炎疼痛,于是非甾体抗炎药(NSAID)被用于替代镇痛药治疗或添加到镇痛药治疗中。虽然NSAID在控制轻度至中度骨关节炎(OA)疼痛方面有效,但它们具有显著的毒性(最常见的是胃肠道毒性),甚至可能导致致命的并发症。因此,经历与关节炎相关疼痛的患者将从具有显著低毒性的抗炎和镇痛药物中获益。环氧化酶-2(COX-2)抑制剂正在临床试验中接受评估或正在研发中。这些药物似乎只抑制COX-2同工酶,该同工酶主要在炎症过程中产生,负责前列腺素和其他炎症介质的生物合成以及疼痛敏化。由于COX-2抑制剂在药理浓度下不抑制COX-1同工酶活性,它们没有许多NSAID典型副作用的毒性。在牙科疼痛、OA和类风湿性关节炎方面的短期研究发现,COX-2抑制剂塞来昔布是一种有效的镇痛药,但不会引起胃十二指肠糜烂。它有可能为关节炎患者提供镇痛和抗炎作用,而没有NSAID的副作用。需要进一步的研究来证实这些发现。