Franssen E J F, Kunst P W A, Bet P M, Strack van Schijndel R J M, van Loenen A C, Wilhelm A J
Department of Pharmacy, University Hospital, Vrije Universiteit, Amsterdam, The Netherlands.
Ther Drug Monit. 2003 Apr;25(2):248-51. doi: 10.1097/00007691-200304000-00018.
Two cases are presented of intentional intoxications with the tricyclic antidepressants (TCAs) nortriptyline (NT) and amitriptyline (AT). The peak plasma concentrations were 2290 microg/L and 2900 microg/L, respectively. The active metabolites E-10-hydroxynortriptyline (EHNT) and Z-10-hydroxynortriptyline (ZHNT) profiles were quite different as monitored for 5 to 10 days after presumed drug intake. In conclusion, these cases illustrate that (1) metabolite formation and elimination after intake of an overdose dose of NT and AT are stereoselective, and (2) NT and EHNT toxicokinetics and toxicodynamics are quite different. It also shows that a patient with a severe TCA overdose can still survive if he or she receives appropriate and quick supportive care, even if the prognostic markers QRS time, coma grade, and serum TCA levels predict poor outcome.
本文报告了两例故意过量服用三环类抗抑郁药去甲替林（NT）和阿米替林（AT）的案例。血浆峰值浓度分别为2290微克/升和2900微克/升。在假定服药后5至10天的监测中，活性代谢物E-10-羟基去甲替林（EHNT）和Z-10-羟基去甲替林（ZHNT）的情况有很大不同。总之，这些案例表明：（1）过量服用NT和AT后代谢物的形成和消除具有立体选择性；（2）NT和EHNT的毒代动力学和毒效动力学有很大差异。这也表明，即使QRS时间、昏迷分级和血清三环类抗抑郁药水平等预后指标预示预后不良，但严重三环类抗抑郁药过量的患者如果得到适当和及时的支持治疗仍可存活。
