毒理性
肝脏测试异常在接受三环类抗抑郁药的患者中报告发生率为10%至12%，但升高很少超过正常上限的3倍。氨基转移酶异常通常是轻微的、无症状的且短暂的，即使在继续用药的情况下也会逆转。血清酶升高率特别是在普罗替林治疗期间尚未得到很好的定义。在接受三环类抗抑郁药的患者中，有报告罕见的临床明显的急性肝损伤病例，但尚未有与普罗替林相关的具体报告。典型的三环类抗抑郁药急性肝损伤的发病潜伏期范围为1至14个月。血清酶升高的模式通常是胆汁淤积性的，但也有报道肝细胞病例，包括急性肝炎样综合征伴急性肝衰竭。急性胆汁淤积性肝炎和长期黄疸的病例与其它三环类抗抑郁药有关，主要是这一类药物中最常用的阿米替林和丙咪嗪。报告的病例中常有过敏反应的迹象或症状（皮疹、发热和嗜酸性粒细胞增多），但这些症状通常是轻微且短暂的。自身抗体的形成是罕见的。普罗替林是一种很少使用三环类抗抑郁药，但怀疑其具有与阿米替林和丙咪嗪相似的不良反应特征。
Liver test abnormalities have been reported to occur in 10% to 12% of patients on tricyclic antidepressants, but elevations are uncommonly above 3 times the upper limit of normal. The aminotransferase abnormalities are usually mild, asymptomatic and transient, reversing even with continuation of medication. The rate of serum enzyme elevations specifically during protriptyline therapy has not been well defined. Rare instances of clinically apparent acute liver injury have been reported in patients on tricyclic antidepressants, but there have been no specific reports related to protriptyline. In typical tricyclic antidepressant acute liver injury, the latency to onset has ranged from 1 to 14 months. The pattern of serum enzyme elevations was typically cholestatic, but hepatocellular cases have also been reported including an acute hepatitis-like syndrome with acute liver failure. Instances of acute cholestatic hepatitis and prolonged jaundice compatible with vanishing bile duct syndrome have been linked to other tricyclic antidepressants, mostly amitriptyline and imipramine, the two most commonly used agents in this class. Signs or symptoms of hypersensitivity (rash, fever and eosinophilia) are frequent in reported cases, but these symptoms are usually mild and transient. Autoantibody formation is rare. Protriptyline is a rarely used tricyclic antidepressant but is suspected of having a profile of adverse effects similar to that of imipramine and amitriptyline.
来源:LiverTox
