Pallasch T J, Gill C J
Oral Surg Oral Med Oral Pathol. 1985 Jan;59(1):15-20. doi: 10.1016/0030-4220(85)90108-2.
The agonist/antagonist analgesics, butorphanol (Stadol) and nalbuphine (Nubain), are being increasingly employed as intravenous sedation agents; nalbuphine will be available in the future as an oral analgesic. The drugs possess numerous pharmacologic similarities and some dissimilarities. Both are equianalgesic (and nalbuphine is equipotent) with morphine parenterally and codeine orally. Their pharmacokinetics are similar; nalbuphine has a longer duration of action. Both may precipitate an abstinence syndrome in narcotic-dependent persons and will probably be associated with low-level drug abuse potential. They are both agonists of the kappa opioid receptor and partial agonists of the mu receptor. Butorphanol is a partial agonist of the sigma receptor responsible for psychotomimetic effects. The incidence of adverse effects is low, sedation being the most common. In cardiac-risk patients, nalbuphine does not increase cardiac work or oxygen requirements; nor do increasing doses of nalbuphine increase the duration of respiratory depression. Both drugs possess plateau respiratory depressant actions.
激动剂/拮抗剂类镇痛药，如布托啡诺（ Stadol）和纳布啡（Nubain），越来越多地被用作静脉镇静剂；纳布啡未来将作为口服镇痛药上市。这两种药物在药理学上有许多相似之处，也有一些不同之处。它们在肠道外与吗啡、口服与可待因的镇痛效果相当（纳布啡效力相当）。它们的药代动力学相似；纳布啡的作用持续时间更长。两者都可能在依赖麻醉品的人身上引发戒断综合征，并且可能与低水平的药物滥用可能性有关。它们都是κ阿片受体激动剂和μ受体部分激动剂。布托啡诺是负责拟精神病作用的σ受体的部分激动剂。不良反应的发生率较低，最常见的是镇静作用。在有心脏风险的患者中，纳布啡不会增加心脏负担或氧气需求；增加纳布啡剂量也不会增加呼吸抑制的持续时间。两种药物都具有平稳的呼吸抑制作用。
