Makita Koshi, Ishikawa Seiji
Department of Anesthesiology, Graduate School of Medicine, Tokyo Medical and Dental University, Tokyo 113-8519.
Masui. 2006 Jul;55(7):817-25.
Remifentanil is a potent mu-opioid receptor agonist and has some unique pharmacokinetic characteristics compared to other anilidopiperidine opioids (e.g. fentanyl, alfentanil, and sufentanil). As remifentanil is metabolised rapidly by nonspecific esterases that are widespread throughout the plasma and tissuses, its duration of action is very short. It is cleared very rapidly, and its clearance is not affected by renal and hepatic function. The context-sensitive half-time of remifentanil remains consistently short, even after administration for a long time. Consequently, emergence is quick even after anesthesia of long duration. As other piperidine opioids, remifentnil has some adverse effects such as respiratory depression, muscle rigidity, bradycardia, and nausea as well as vomiting. Because of the rapid dissipation of analgesic effect following remifentanil discontinuation, postoperative analgesia should be provided before or soon after anesthesia using longer-acting opioid analgesics, non-opioid analgesics, or local as well as regional anesthesia.
瑞芬太尼是一种强效μ-阿片受体激动剂,与其他苯胺基哌啶类阿片类药物(如芬太尼、阿芬太尼和舒芬太尼)相比,具有一些独特的药代动力学特征。由于瑞芬太尼被广泛存在于血浆和组织中的非特异性酯酶迅速代谢,其作用持续时间非常短。它清除极快,且其清除不受肾功能和肝功能的影响。即使长时间给药后,瑞芬太尼的时量相关半衰期仍始终很短。因此,即使长时间麻醉后苏醒也很快。与其他哌啶类阿片类药物一样,瑞芬太尼有一些不良反应,如呼吸抑制、肌肉强直、心动过缓以及恶心和呕吐。由于停用瑞芬太尼后镇痛效果迅速消失,应在麻醉前或麻醉后不久使用长效阿片类镇痛药、非阿片类镇痛药或局部及区域麻醉提供术后镇痛。