Sir Mortimer B. Davis Jewish General Hospital, Montréal, Canada;
J Pain Res. 2010 Feb 8;3:1-9. doi: 10.2147/jpr.s4989.
The undertreatment of acute pain is common in many health care settings. Insufficient management of acute pain may lead to poor patient outcomes and potentially life-threatening complications. Opioids provide relief of moderate to severe acute pain; however, therapy with pure μ-opioid agonists is often limited by the prevalence of side effects, particularly opioid-induced nausea and vomiting. Tapentadol is a novel, centrally acting analgesic with 2 mechanisms of action, μ-opioid receptor agonism and norepinephrine reuptake inhibition. The analgesic effects of tapentadol are independent of metabolic activation and tapentadol has no active metabolites; therefore, in theory, tapentadol may be associated with a low potential for interindividual efficacy variations and drug-drug interactions. Previous phase 3 trials in patients with various types of moderate to severe acute pain have shown that tapentadol immediate release (IR; 50 to 100 mg every 4 to 6 hours) provides analgesia comparable to that provided by the pure μ-opioid agonist comparator, oxycodone HCl IR (10 or 15 mg every 4 to 6 hours), with a lower incidence of nausea, vomiting, and constipation. Findings suggest tapentadol may represent an improved treatment option for acute pain.
在许多医疗保健环境中,急性疼痛的治疗不足很常见。急性疼痛管理不足可能导致患者预后不良,并可能导致危及生命的并发症。阿片类药物可缓解中度至重度急性疼痛;然而,纯μ-阿片受体激动剂治疗常受到副作用的影响,特别是阿片类药物引起的恶心和呕吐。他喷他多是一种新型中枢作用镇痛药,具有 2 种作用机制,μ-阿片受体激动作用和去甲肾上腺素再摄取抑制作用。他喷他多的镇痛作用不依赖于代谢激活,且他喷他多没有活性代谢物;因此,理论上,他喷他多可能与个体间疗效变化和药物相互作用的潜在风险低有关。在各种类型的中度至重度急性疼痛患者中进行的先前的 3 期试验表明,他喷他多速释制剂(50 至 100mg,每 4 至 6 小时一次)提供的镇痛作用与纯μ-阿片受体激动剂对照药盐酸羟考酮速释制剂(10 或 15mg,每 4 至 6 小时一次)相当,但恶心、呕吐和便秘的发生率较低。研究结果表明,他喷他多可能是急性疼痛的一种更好的治疗选择。