Nation R L, Triggs E J, Selig M
Br J Clin Pharmacol. 1977 Aug;4(4):439-48. doi: 10.1111/j.1365-2125.1977.tb00759.x.
1 The pharmacokinetics following long term intravenous infusion of lignocaine to cardiac patients have been examined. 2 Plasma levels and half-lives of lignocaine and monoethylglycinexylidide (MEGX) showed wide inter-patient variability. 3 Toxicity reactions to therapy were associated with elevated lignocaine and/or MEGX plasma levels. 4 In a separate study the effect of age on the pharmacokinetics of lignocaine was examined using bolus doses (50 mg) of the drug to young and aged subjects. 5 Elderly subjects had significantly longer half-lives for lignocaine compared to younger individuals although no change in plasma clearance occurred. 6 The drug appeared to distribute differently in the aged as reflected by significantly increased apparent volumes of distribution. 7 The 24 h urinary recovery of the major metabolite (total 4-hydroxyxylidine) showed a significant reduction in the elderly when compared to the young. 8 The clinical significance of these studies with respect to lignocaine therapy has been discussed.
已对心脏病患者长期静脉输注利多卡因后的药代动力学进行了研究。
利多卡因和单乙基甘氨酰二甲苯(MEGX)的血浆水平及半衰期在患者之间显示出很大的变异性。
治疗的毒性反应与利多卡因和/或MEGX血浆水平升高有关。
在另一项研究中,使用大剂量(50毫克)的该药物对年轻和老年受试者进行研究,以考察年龄对利多卡因药代动力学的影响。
与年轻个体相比,老年受试者利多卡因的半衰期显著更长,尽管血浆清除率没有变化。
药物在老年人中的分布似乎有所不同,表现为分布容积明显增加。
与年轻人相比,老年人主要代谢产物(总4-羟基二甲苯)的24小时尿回收率显著降低。
已讨论了这些研究对利多卡因治疗的临床意义。