Department of Palliative Care, University Medical Center Freiburg, Robert-Koch-Str. 3, D-79106 Freiburg, Germany.
Expert Rev Gastroenterol Hepatol. 2013 Jan;7(1):13-26. doi: 10.1586/egh.12.63.
Opioids are the drugs of choice for treating moderate-to-severe pain, especially for patients in the end stage of cancer or other advanced illnesses, and also in critical care or for the treatment of chronic pain. Side effects such as nausea, pruritus, dizziness and constipation have to be controlled in order to use these drugs to their full potential. Opioid-induced bowel syndrome and constipation caused by activation of μ-receptors in the gut can have such distressing effects that some patients prefer to forego adequate pain control. Methylnaltrexone is a μ-opioid receptor antagonist that, unlike naltrexone or naloxone, does not pass the blood-brain barrier, and therefore does not impair the centrally mediated analgesic effect of opioids. It is licensed for the treatment of opioid-induced constipation in palliative care in more than 50 countries. This article presents practically relevant pharmacological data, basic research results and evidence from clinical research about methylnaltrexone, and outlines potential future therapeutic options for this promising drug.
阿片类药物是治疗中重度疼痛的首选药物，尤其适用于癌症晚期或其他晚期疾病患者、重症监护患者或慢性疼痛患者。为了充分发挥这些药物的作用，必须控制恶心、瘙痒、头晕和便秘等副作用。肠道 μ 受体激活引起的阿片类药物诱导的肠道综合征和便秘可能会产生如此令人痛苦的影响，以至于一些患者宁愿放弃充分的疼痛控制。美沙纳曲酮是一种 μ 阿片受体拮抗剂，与纳曲酮或纳洛酮不同，它不能通过血脑屏障，因此不会损害阿片类药物的中枢介导的镇痛作用。它在 50 多个国家被批准用于姑息治疗中阿片类药物引起的便秘。本文介绍了美沙纳曲酮的实用相关药理学数据、基础研究结果和临床研究证据，并概述了这种有前途的药物的潜在未来治疗选择。
