Vadivelu Nalini, Huang Yili, Mirante Brian, Jacoby Michael, Braveman Ferne R, Hines Roberta L, Sinatra Raymond
Department of Anesthesiology, Yale University, New Haven, CT, USA.
Drug Healthc Patient Saf. 2013 Jul 3;5:151-9. doi: 10.2147/DHPS.S28829. Print 2013.
Poorly controlled acute and chronic pain can increase morbidity, impair quality of life and prolong disability. Over 80 percent of post surgical patients report moderate to severe uncontrolled postoperative pain. Over-reliance on potent opioid agonists can lead to several opioid related side effects such as gastrointestinal intolerability, respiratory depression and cognitive impairment. A recently approved dual acting central analgesic tapentadol may offer improved tolerability over traditional opioid agonists while having multimodal opioid and nonopioid analgesic benefits. Tapentadol, classified by the US Food and Drug Administration as a class 2 opioid, is currently marketed in the United States as immediate release (IR) NUCYNTA® for moderate to severe acute pain in tablets of 50 mg, 75 mg, and 100 mg, and as extended release (ER) NUCYNTA ER® for the treatment of chronic moderate to severe pain in tablets of 50 mg, 100 mg, 150 mg, 200 mg, and 250 mg. Tapentadol is a low affinity mu opioid receptor agonist and a norepinephrine reuptake inhibitor. Tapentadol has no active metabolites and this property makes it useful in patients with hepatic and renal failure. Clinical trials with tapentadol IR showed that there was improved gastrointestinal tolerability and similar pain relief as compared to oxycodone IR. Tapentadol ER allows for twice daily dosing. Clinical trials showed that tapentadol ER could effectively relieve moderate to severe chronic pain and was associated with significantly fewer gastrointestinal adverse effects as compared to oxycodone controlled release. Tapentadol ER is indicated and has Food and Drug Administration approval for the treatment of chronic painful diabetic neuropathy. The most common side effects of tapentadol are nausea (30%), vomiting (18%), dizziness (24%), and somnolence (15%). Tapentadol, due to its potential synergistic effects on norepinephrine levels, is contraindicated in patients who have taken monoamine oxidase inhibitors within the last 14 days. Caution has to be exercised with the use of tapentadol IR and tapentadol ER in the presence of other central nervous system depressants such as neuroleptics, opioids, illicit drugs, muscle relaxants, sedatives, and anxiolytics.
急慢性疼痛若控制不佳，会增加发病率、损害生活质量并延长残疾时间。超过80%的外科术后患者报告有中度至重度的术后疼痛未得到控制。过度依赖强效阿片类激动剂会导致多种与阿片类药物相关的副作用，如胃肠道不耐受、呼吸抑制和认知障碍。最近获批的双作用中枢镇痛药曲马多，相较于传统阿片类激动剂，耐受性可能更好，同时具有多模式的阿片类和非阿片类镇痛效果。曲马多被美国食品药品监督管理局归类为2类阿片类药物，目前在美国以速释（IR）剂型的盐酸曲马多片（NUCYNTA®）上市，有50毫克、75毫克和100毫克片剂，用于治疗中度至重度急性疼痛；还有缓释（ER）剂型的盐酸曲马多缓释片（NUCYNTA ER®），有50毫克、100毫克、150毫克、200毫克和250毫克片剂，用于治疗慢性中度至重度疼痛。曲马多是一种低亲和力的μ阿片受体激动剂和去甲肾上腺素再摄取抑制剂。曲马多没有活性代谢产物，这一特性使其适用于肝肾功能衰竭患者。曲马多速释剂型的临床试验表明，与羟考酮速释剂型相比，其胃肠道耐受性有所改善，且镇痛效果相似。曲马多缓释剂型允许每日给药两次。临床试验表明，与羟考酮控释剂型相比，曲马多缓释剂型能有效缓解中度至重度慢性疼痛，且胃肠道不良反应明显较少。曲马多缓释剂型已获美国食品药品监督管理局批准用于治疗慢性疼痛性糖尿病神经病变。曲马多最常见的副作用包括恶心（30%）、呕吐（18%）、头晕（24%）和嗜睡（15%）。由于曲马多对去甲肾上腺素水平可能有协同作用，在过去14天内服用过单胺氧化酶抑制剂的患者禁用。在同时使用其他中枢神经系统抑制剂（如抗精神病药、阿片类药物、非法药物、肌肉松弛剂、镇静剂和抗焦虑药）时，使用曲马多速释剂型和曲马多缓释剂型必须谨慎。
