Gillman P K
Pioneer Valley Private Hospital, Mackay, Queensland, Australia.
Br J Anaesth. 2005 Oct;95(4):434-41. doi: 10.1093/bja/aei210. Epub 2005 Jul 28.
Toxicity resulting from excessive intra-synaptic serotonin, historically referred to as serotonin syndrome, is now understood to be an intra-synaptic serotonin concentration-related phenomenon. Recent research more clearly delineates serotonin toxicity as a discreet toxidrome characterized by clonus, hyper-reflexia, hyperthermia and agitation. Serotonergic side-effects occur with serotonergic drugs, and overdoses of serotonin re-uptake inhibitors (SRIs) frequently produce marked serotonergic side-effects, and in 15% of cases, moderate serotonergic toxicity, but not to a severe degree, which produces hyperthermia and risk of death. It is only combinations of serotonergic drugs acting by different mechanisms that are capable of raising intra-synaptic serotonin to a level that is life threatening. The combination that most commonly does this is a monoamine oxidase inhibitor (MAOI) drug combined with any SRI. There are a number of lesser-known drugs that are MAOIs, such as linezolid and moclobemide; and some opioid analgesics have serotonergic activity. These properties when combined can precipitate life threatening serotonin toxicity. Possibly preventable deaths are still occurring. Knowledge of the properties of these drugs will therefore help to ensure that problems can be avoided in most clinical situations, and treated appropriately (with 5-HT(2A) antagonists for severe cases) if they occur. The phenylpiperidine series opioids, pethidine (meperidine), tramadol, methadone and dextromethorphan and propoxyphene, appear to be weak serotonin re-uptake inhibitors and have all been involved in serotonin toxicity reactions with MAOIs (including some fatalities). Morphine, codeine, oxycodone and buprenorphine are known not to be SRIs, and do not precipitate serotonin toxicity with MAOIs.
历史上被称为血清素综合征的由突触内血清素过量导致的毒性,现在被理解为一种与突触内血清素浓度相关的现象。最近的研究更清楚地将血清素毒性描述为一种以阵挛、反射亢进、体温过高和激动为特征的独特中毒综合征。血清素能药物会产生血清素能副作用,血清素再摄取抑制剂(SRIs)过量经常会产生明显的血清素能副作用,在15%的病例中会产生中度血清素能毒性,但程度不严重,不会导致体温过高和死亡风险。只有通过不同机制起作用的血清素能药物组合才能够将突触内血清素提高到危及生命的水平。最常见的能做到这一点的组合是单胺氧化酶抑制剂(MAOI)药物与任何一种SRIs联合使用。有一些不太知名的药物是MAOIs,如利奈唑胺和吗氯贝胺;一些阿片类镇痛药具有血清素能活性。这些特性联合起来可能会引发危及生命的血清素毒性。仍有一些可能可预防的死亡发生。因此,了解这些药物的特性将有助于确保在大多数临床情况下能够避免问题,如果问题发生,也能得到适当治疗(严重病例使用5-HT(2A)拮抗剂)。苯基哌啶系列阿片类药物、哌替啶(度冷丁)、曲马多、美沙酮、右美沙芬和丙氧芬似乎是弱血清素再摄取抑制剂,并且都曾与MAOIs发生血清素毒性反应(包括一些死亡病例)。吗啡、可待因、羟考酮和丁丙诺啡已知不是SRIs,与MAOIs联合使用时不会引发血清素毒性。