Anderson J L, Anastasiou-Nana M, Dayton V D, Creagar R N, Jensen R L, Wright G J
J Cardiovasc Pharmacol. 1985 May-Jun;7(3):609-12. doi: 10.1097/00005344-198505000-00030.
Myocardial and plasma bethanidine kinetics were determined in five dogs after an intravenous dose of 6 mg/kg/10 min. Serial myocardial drug concentrations were determined from endomyocardial samples obtained by transvenous biopsies between 15 min and 72 h. Tissue and plasma samples were assayed by gas-liquid chromatography. Bethanidine was rapidly concentrated in myocardium within 15 min. Tissue/plasma drug ratios averaged 131 +/- 35 between 15 min and 2 h and 53 +/- 10 between 6 and 48 h. Parallel biexponential decay then occurred for both tissue and plasma compartments; the terminal half-life approximated 16 h. Based on differences in rates of myocardial drug kinetics, the cardiac antifibrillatory effects of bethanidine may occur more rapidly than those of bretylium.
在五只犬静脉注射6毫克/千克/10分钟剂量后，测定了心肌和血浆中苄乙胍的动力学。通过经静脉活检在15分钟至72小时之间从心内膜样本中测定系列心肌药物浓度。组织和血浆样本通过气液色谱法进行分析。苄乙胍在15分钟内迅速在心肌中浓缩。在15分钟至2小时之间组织/血浆药物比率平均为131±35，在6至48小时之间为53±10。然后组织和血浆区室均出现平行的双指数衰减；终末半衰期约为16小时。基于心肌药物动力学速率的差异，苄乙胍的心脏抗纤颤作用可能比溴苄铵的作用出现得更快。
