Clinical Toxicology, Guy's and St Thomas' NHS Foundation Trust and Kings Health Partners, London, UK.
Eur J Clin Pharmacol. 2012 May;68(5):853-6. doi: 10.1007/s00228-011-1199-9. Epub 2011 Dec 29.
Long-term regular use of ketamine has been reported to be associated with severe symptomatic urinary tract problems. Methoxetamine, an arylcyclohexylamine derivative of ketamine, is marketed as a "bladder safe" derivative of ketamine, and no cases of acute toxicity following analytically confirmed methoxetamine use have been reported to date. We report here a case series of three individuals with acute toxicity related to the analytically confirmed use of methoxetamine.
Three patients aged between 28 and 42 years presented to the Emergency Department (ED) on unrelated occasions having used methoxetamine. Clinical features were suggestive of a "dissociative/catatonic" state similar to that seen with ketamine; in addition, they had clinical features of acute sympathomimetic toxicity with significant tachycardia and hypertension. All were managed with low-dose benzodiazepines and discharged home once their symptoms/signs had settled. TOXICOLOGICAL SCREENING: Serum collected at the time of presentation to the ED was analysed qualitatively and quantitatively by gas chromatography-mass spectrometry. Serum concentrations ranged from 0.09 to 0.2 mg/L; in addition, detectable levels of 6-APB/5-APB were found in one of the patients.
These three analytically confirmed cases demonstrate that acute methoxetamine-related toxicity is associated with both "dissociative" and "sympathomimetic" clinical features. The information from these three cases is useful to clinical pharmacologists, not only in managing individuals with acute methoxetamine toxicity but also in advising the appropriate legislative authorities on the risk of acute harm related to methoxetamine use. Further work is needed to determine whether methoxetamine is more "bladder friendly" than ketamine, as has been suggested by those marketing methoxetamine.
有报道称，长期规律使用氯胺酮会导致严重的症状性泌尿道问题。甲氧基胺，即氯胺酮的芳基环己基胺衍生物，被作为氯胺酮的“膀胱安全”衍生物进行销售，迄今为止，没有分析证实的甲氧基胺使用导致急性毒性的案例报告。我们在此报告三例分析证实的甲氧基胺使用相关的急性毒性病例系列。
三例年龄在 28 至 42 岁之间的患者在不同时间因使用甲氧基胺而到急诊部就诊。临床特征提示类似于氯胺酮的“分离/紧张性”状态；此外，他们还表现出急性拟交感神经毒性的临床特征，伴有明显的心动过速和高血压。所有患者均接受小剂量苯二氮䓬类药物治疗，一旦症状/体征缓解即出院回家。
在急诊部就诊时采集的血清通过气相色谱-质谱法进行定性和定量分析。血清浓度范围为 0.09 至 0.2 毫克/升；此外，在其中一位患者的血清中还发现了可检测水平的 6-APB/5-APB。
这三个经分析证实的病例表明，急性甲氧基胺相关毒性与“分离”和“拟交感神经”的临床特征有关。这三个病例的信息对临床药理学家很有用，不仅可用于管理急性甲氧基胺毒性的个体，还可就与甲氧基胺使用相关的急性危害向适当的立法机构提供建议。需要进一步的工作来确定甲氧基胺是否比氯胺酮更“对膀胱友好”，因为推销甲氧基胺的人曾这样表示。
