Martini Dyllon Ivy, Nacca Nicholas, Haswell David, Cobb Timothy, Hodgman Michael
Department of Emergency Medicine, Upstate New York Poison Center, SUNY Upstate Medical University , Syracuse, NY , USA.
Clin Toxicol (Phila). 2015 Mar;53(3):185-7. doi: 10.3109/15563650.2015.1009993. Epub 2015 Feb 11.
Metaxalone has only recently been associated with serotonin syndrome. The mechanism of action of this centrally acting muscle relaxant is unknown; however, the observation of serotonin syndrome in patients with metaxalone overdose suggests a role in the serotonergic pathway.
(Case 1) A 29-year-old woman with overdose of metaxalone presented to the emergency department with altered mental status, seizure-like activity, hyperthermia, rigidity in the lower extremities, myoclonus, and hyperreflexia. Vital signs on arrival include blood pressure of 168/80 mmHg, heart rate of 208 beats per minute (bpm), respirations of 20/min, a temperature of 41.6° C rectally, and room air oxygen saturation of 97%. She was intubated and sedated with benzodiazepines, and actively cooled. Serum paroxetine concentration was 23 (therapeutic range: 20-200) ng/mL, and serum metaxalone concentration was 31 mcg/mL (peak plasma concentrations average 0.9 mcg/mL at 3.3 h following a single oral dose of 400 mg). (Case 2) A 27-year-old man presented to the emergency department with altered mental status, rigidity in his lower extremities, myoclonus, and hyperreflexia. Vital signs on arrival include blood pressure of 158/131 mmHg, heart rate of 126 bpm, respiratory rate of 20 breaths per minute, and temperature of 37.2°C, with oxygen saturation of 98% on room air. His medication list included metaxalone and escitalopram. He was managed aggressively with IV boluses of diazepam, in total 80 mg, in the emergency department. Serum escitalopram concentration was 24 ng/mL with a therapeutic range of 21-64 ng/mL, and serum metaxalone concentration was 58 mcg/mL.
These two cases suggest that at supratherapeutic concentrations metaxalone has serotonergic effects. Severe serotonin toxicity may result from metaxalone abuse in individuals using a selective serotonin reuptake inhibitor therapeutically.
美他沙酮直到最近才与血清素综合征相关联。这种中枢性肌肉松弛剂的作用机制尚不清楚;然而,在美他沙酮过量患者中观察到血清素综合征表明其在血清素能途径中发挥作用。
(病例1)一名29岁女性因过量服用美他沙酮就诊于急诊科,出现精神状态改变、癫痫样活动、高热、下肢僵硬、肌阵挛和反射亢进。入院时生命体征包括血压168/80 mmHg、心率208次/分钟、呼吸频率20次/分钟、直肠温度41.6°C以及室内空气氧饱和度97%。她接受了气管插管并用苯二氮䓬类药物镇静,并积极降温。血清帕罗西汀浓度为23(治疗范围:20 - 200)ng/mL,血清美他沙酮浓度为31 mcg/mL(单次口服400 mg后3.3小时血浆峰值浓度平均为0.9 mcg/mL)。(病例2)一名27岁男性因精神状态改变、下肢僵硬、肌阵挛和反射亢进就诊于急诊科。入院时生命体征包括血压158/131 mmHg、心率126次/分钟、呼吸频率20次/分钟、体温37.2°C,室内空气氧饱和度98%。他的用药清单包括美他沙酮和艾司西酞普兰。在急诊科,他接受了总量80 mg的静脉注射地西泮积极治疗。血清艾司西酞普兰浓度为24 ng/mL,治疗范围为21 - 64 ng/mL,血清美他沙酮浓度为58 mcg/mL。
这两个病例表明,在超治疗浓度下美他沙酮具有血清素能效应。在治疗性使用选择性血清素再摄取抑制剂的个体中,美他沙酮滥用可能导致严重的血清素毒性。