Pharmacology, Toxicology, and Therapeutics, Centre for Cardiovascular Science, University of Edinburgh, Edinburgh, UK.
Cardiovascular Research Institute, National University Health System, Singapore City, Singapore.
Clin Transl Sci. 2021 Jul;14(4):1476-1489. doi: 10.1111/cts.13009. Epub 2021 Apr 9.
N-acetylcysteine (NAC) is an antidote to prevent acetaminophen (paracetamol-APAP)-induced acute liver injury (ALI). The 3-bag licensed 20.25 h standard regimen, and a 12 h modified regimen, are used to treat APAP overdose. This study evaluated the redox thiol response and APAP metabolites, in patients with a single APAP overdose treated with either the 20.25 h standard or 12 h modified regimen. We used liquid chromatography tandem mass spectrometry to quantify clinically important oxidative stress biomarkers and APAP metabolites in plasma samples from 45 patients who participated in a randomized controlled trial (SNAP trial). We investigated the time course response of plasma metabolites at predose, 12 h, and 20.25 h post-start of NAC infusion. The results showed that the 12 h modified regimen resulted in a significant elevation of plasma NAC and cysteine concentrations at 12 h post-infusion. We found no significant alteration in the metabolism of APAP, mitochondrial, amino acids, and other thiol biomarkers with the two regimens. We examined APAP and purine metabolism in overdose patients who developed ALI. We showed the major APAP-metabolites and xanthine were significantly higher in patients with ALI. These biomarkers correlated well with alanine aminotransferase activity at admission. Receiver operating characteristic analysis showed that at admission, plasma APAP-metabolites and xanthine concentrations were predictive for ALI. In conclusion, a significantly higher redox thiol response with the modified NAC regimen at 12 h postdose suggests this regimen may produce greater antioxidant efficacy. At baseline, plasma APAP and purine metabolites may be useful biomarkers for early prediction of APAP-induced ALI.
N-乙酰半胱氨酸(NAC)是一种解毒剂,可预防对乙酰氨基酚(扑热息痛-APAP)引起的急性肝损伤(ALI)。已获得许可的 3 袋 20.25 小时标准方案和 12 小时改良方案用于治疗 APAP 过量。本研究评估了单个 APAP 过量患者接受 20.25 小时标准方案或 12 小时改良方案治疗时的氧化还原硫醇反应和 APAP 代谢物。我们使用液相色谱串联质谱法在参与随机对照试验(SNAP 试验)的 45 名患者的血浆样本中定量测定了临床上重要的氧化应激生物标志物和 APAP 代谢物。我们研究了 NAC 输注开始后 12 小时和 20.25 小时时血浆代谢物的时间过程反应。结果表明,12 小时改良方案在输注后 12 小时导致血浆 NAC 和半胱氨酸浓度显着升高。我们发现两种方案对 APAP、线粒体、氨基酸和其他硫醇生物标志物的代谢没有显着改变。我们检查了发生 ALI 的过量患者的 APAP 和嘌呤代谢。我们表明,ALI 患者的主要 APAP 代谢物和黄嘌呤显着升高。这些生物标志物与入院时的丙氨酸氨基转移酶活性相关性良好。接收者操作特征分析表明,入院时血浆 APAP 代谢物和黄嘌呤浓度可预测 ALI。总之,改良的 NAC 方案在剂量后 12 小时显示出更高的氧化还原硫醇反应,这表明该方案可能产生更大的抗氧化功效。在基线时,血浆 APAP 和嘌呤代谢物可能是预测 APAP 诱导的 ALI 的有用生物标志物。