Leuven Centre for Algology and Pain Management, Anaesthesiology and Algology, Department of Cardiovascular Sciences, University Hospitals Leuven, University of Leuven, Leuven, Belgium.
Independent Researcher, Berlin, Germany.
Pain Pract. 2018 Jun;18(5):647-665. doi: 10.1111/papr.12646. Epub 2017 Nov 28.
Opioids provide effective relief from moderate-to-severe pain and should be prescribed as part of a multifaceted approach to pain management when other treatments have failed. Fixed-dose oxycodone/naloxone prolonged-release tablets (OXN PR) were designed to address the opioid class effect of opioid-induced constipation (OIC) by combining the analgesic efficacy of oxycodone with the opioid receptor antagonist, naloxone, which has negligible systemic availability when administered orally. This formulation has abuse-deterrent properties, since systemic exposure to naloxone by parenteral administration would antagonize the euphoric effects of oxycodone.
A literature search was conducted to assess the evidence base for OXN PR to treat moderate-to-severe pain and its impact on bowel function, based on published clinical trials and observational studies.
Extensive data demonstrate that OXN PR provides effective analgesia and clinically relevant improvements in bowel function in patients with OIC and moderate-to-severe cancer-related pain and noncancer pain types such as low back pain, neuropathic pain, and musculoskeletal pain. OXN PR has also been found to improve bowel function in patients with OIC refractory to multiple types of laxatives, and improve Parkinson's disease-related pain. No unanticipated safety concerns have been reported in elderly patients.
Evidence from clinical trials and observational studies confirms that for selected patients OXN PR significantly improves moderate-to-severe chronic pain and provides relief from OIC. Treatment should be tailored to individual patients to establish the lowest effective dose. An absence of analgesic ceiling effect was seen across the clinically relevant dose range investigated (≤ 160/80 mg/day).
阿片类药物可有效缓解中重度疼痛，在其他治疗方法失败时，应将其作为多模式疼痛管理的一部分开具处方。固定剂量羟考酮/纳洛酮缓释片（OXN PR）旨在通过将羟考酮的镇痛疗效与阿片受体拮抗剂纳洛酮结合，解决阿片类药物引起的便秘（OIC）的类阿片效应，纳洛酮经口服给药时系统可用性可忽略不计。这种配方具有防止滥用的特性，因为通过注射给予纳洛酮会拮抗羟考酮的欣快作用。
根据已发表的临床试验和观察性研究，进行文献检索，评估 OXN PR 治疗中重度疼痛及其对肠道功能的影响的证据基础。
大量数据表明，OXN PR 可有效缓解中重度疼痛患者的疼痛，并可改善肠道功能，对于伴有 OIC 和中重度癌症相关疼痛以及非癌症疼痛类型（如腰痛、神经病理性疼痛和肌肉骨骼疼痛）的患者具有临床意义。OXN PR 还被发现可改善对多种类型泻药难治性 OIC 患者的肠道功能，并改善帕金森病相关疼痛。在老年患者中未报告未预料到的安全性问题。
临床试验和观察性研究的证据证实，对于某些患者，OXN PR 可显著改善中重度慢性疼痛，并缓解 OIC。治疗应根据个体患者的情况进行调整，以确定最低有效剂量。在研究的临床相关剂量范围内（≤ 160/80 mg/天）未观察到镇痛作用的天花板效应。
