Varney Shawn M, Bebarta Vikhyat S, Vargas Toni E, Boudreau Susan, Castaneda Maria
The Department of Emergency Medicine, San Antonio Military Medical Center, San Antonio, TX.
Acad Emerg Med. 2014 Nov;21(11):1212-9. doi: 10.1111/acem.12513.
Tricyclic antidepressants (TCAs) are highly lipophilic medications used to treat posttraumatic stress disorder and chronic pain. Intravenous lipid emulsion (ILE) is a recent antidote for lipophilic drug overdose with unclear effectiveness. ILE has been studied in TCA overdose in small animals, and cases are reported in humans, but controlled studies in a larger animal model are lacking. Given the high lipophilicity of amitriptyline, a TCA, the hypothesis was that ILE would be more effective than the standard antidote sodium bicarbonate in improving amitriptyline-induced hypotension. The objective was to determine if ILE improved hypotension (defined by a mean arterial pressure [MAP] < 60% baseline) compared to sodium bicarbonate for amitriptyline overdose in a critically ill porcine model.
In this prospective, randomized, controlled trial, 24 female Sus scrofa swine weighing 45 to 55 kg were infused with amitriptyline at 0.5 mg/kg/min until the MAP reached 60% of baseline values. Animals were randomized to the experimental treatment group (ILE 7 mL/kg bolus, then 0.25 mL/kg/min) or the standard treatment group (sodium bicarbonate 2 mEq/kg plus an equal volume of saline). The primary outcome was a 50% improvement in MAP after ILE administration. We continuously monitored heart rate (HR), systolic blood pressure (sBP), MAP, and cardiac output. Electrocardiograms were recorded every 15 minutes. Serum pH, pCO2 , bicarbonate, lactate, and electrolytes were measured. Amitriptyline levels were measured by liquid chromatography/tandem mass spectrometry. Statistical methods used to detect a difference in MAP between the two treatment groups included repeated-measures analysis of variance, adjusted for treatment, time, and the interaction of treatment by time. A sample size of 12 animals per group provided a power of 0.8 and an alpha of 0.05 to detect a 50% difference in MAP.
There was no difference at baseline between ILE and sodium bicarbonate groups in mean HR, sBP, MAP, or cardiac output. Mean amounts of amitriptyline to reach hypotension and time to hypotension were similar between groups. After hypotension there was no difference between groups for mean HR, sBP, MAP, or cardiac output. The median time from hypotension to death was greater for the sodium bicarbonate group (10 minutes [IQR = 6 to 61 minutes] vs. 5 minutes [IQR = 4.5 to 6 minutes] for the ILE group; p = 0.003), but overall survival was not different. One ILE and four sodium bicarbonate pigs survived. Additionally, no difference was detected in QRS intervals between the two groups. The mean (±SD) amitriptyline level in the lipid layer was 3.34 (±2.12) μg/mL, and in the aqueous layer, 4.69 (±2.44) μg/mL. The ILE fatty layer contained 38.2% of total measurable amitriptyline, while the aqueous layer contained 53.6%.
Intravenous lipid emulsion treatment failed to improve amitriptyline-induced hypotension when compared to the standard treatment of sodium bicarbonate in a large animal model of severe TCA overdose. Larger groups with better survival may yield different results from the high mortality observed in this pilot study. Similar amounts of amitriptyline were found in the aqueous and lipid layers. These conclusions are limited to a single ILE regimen.
三环类抗抑郁药(TCAs)是用于治疗创伤后应激障碍和慢性疼痛的高度亲脂性药物。静脉脂质乳剂(ILE)是一种用于亲脂性药物过量的新型解毒剂,但其有效性尚不清楚。ILE已在小动物三环类抗抑郁药过量的研究中进行了研究,也有人类病例报告,但缺乏在大型动物模型中的对照研究。鉴于三环类抗抑郁药阿米替林具有高亲脂性,因此假设ILE在改善阿米替林引起的低血压方面比标准解毒剂碳酸氢钠更有效。目的是确定在重症猪模型中,与碳酸氢钠相比,ILE是否能改善阿米替林过量引起的低血压(定义为平均动脉压[MAP]<基线的60%)。
在这项前瞻性、随机、对照试验中,对24头体重45至55千克的雌性家猪以0.5毫克/千克/分钟的速度输注阿米替林,直至MAP达到基线值的60%。动物被随机分为实验治疗组(ILE 7毫升/千克推注,然后0.25毫升/千克/分钟)或标准治疗组(碳酸氢钠2毫当量/千克加等量生理盐水)。主要结局是ILE给药后MAP改善50%。我们持续监测心率(HR)、收缩压(sBP)、MAP和心输出量。每15分钟记录一次心电图。测量血清pH值、pCO2、碳酸氢盐、乳酸和电解质。通过液相色谱/串联质谱法测量阿米替林水平。用于检测两个治疗组之间MAP差异的统计方法包括重复测量方差分析,并根据治疗、时间以及治疗与时间的相互作用进行调整。每组12只动物的样本量提供了0.8的检验效能和0.05的α水平,以检测MAP的50%差异。
ILE组和碳酸氢钠组在基线时的平均HR、sBP、MAP或心输出量无差异。两组达到低血压的阿米替林平均用量和达到低血压的时间相似。低血压发生后,两组之间的平均HR、sBP、MAP或心输出量无差异。碳酸氢钠组从低血压到死亡的中位时间更长(10分钟[四分位间距=6至61分钟],而ILE组为5分钟[四分位间距=4.5至6分钟];p=0.003),但总体生存率无差异。1只接受ILE治疗的猪和4只接受碳酸氢钠治疗的猪存活。此外,两组之间的QRS间期未检测到差异。脂质层中阿米替林的平均(±标准差)水平为3.34(±2.12)微克/毫升,水层中为4.69(±2.44)微克/毫升。ILE脂肪层含有可测量的总阿米替林的38.2%,而水层含有53.6%。
在严重三环类抗抑郁药过量的大型动物模型中,与碳酸氢钠的标准治疗相比,静脉脂质乳剂治疗未能改善阿米替林引起的低血压。生存率更高的更大样本组可能会得出与本初步研究中观察到的高死亡率不同的结果。在水层和脂质层中发现了相似量的阿米替林。这些结论仅限于单一的ILE方案。