Oltmanns D, Pottage A, Endell W
Eur J Clin Pharmacol. 1983;25(6):787-90. doi: 10.1007/BF00542521.
The disposition of tocainide following an i.v. infusion of tocainide HCl 100 mg was studied in 6 patients with decompensated cirrhosis (ascites) and renal dysfunction. In one patient with active hepatic necrosis the terminal plasma half-life was 57.4, and in the others the half life ranged from 16.0 to 29.0 h. The increase in half-life was correlated with biochemical evidence of renal dysfunction, but not with individual tests of hepatic function. Non-renal clearance of tocainide was similar to values reported previously in healthy subjects and patients with acute myocardial infarction. The apparent volume of distribution of tocainide was increased and the pattern of distribution was abnormal in some patients, as plasma concentrations increased after an initial fall and the elevated concentrations then persisted for several hours. This abnormality appeared to be most marked in patients with the greatest degree of liver dysfunction.
对6例失代偿期肝硬化(腹水)伴肾功能不全患者静脉输注100mg盐酸妥卡尼后的妥卡尼处置情况进行了研究。1例有活动性肝坏死的患者,其血浆终末半衰期为57.4小时,其他患者的半衰期在16.0至29.0小时之间。半衰期的延长与肾功能不全的生化证据相关,但与肝功能的单项检测无关。妥卡尼的非肾清除率与先前报道的健康受试者和急性心肌梗死患者的值相似。妥卡尼的表观分布容积增加,且在一些患者中分布模式异常,因为血浆浓度在初始下降后升高,然后升高的浓度持续数小时。这种异常在肝功能障碍程度最大的患者中似乎最为明显。