Sakanashi M, Noguchi K, Chibana T, Ojiri Y, Shoji M
Department of Pharmacology, School of Medicine, University of the Ryukyus, Okinawa, Japan.
Am J Chin Med. 1993;21(1):7-16. doi: 10.1142/S0192415X93000030.
The effects of "Kyushin" (KY), a Senso (toad venom)-containing drug, on the cardiovascular system were examined by intraduodenal administration of KY in anesthetized open-chest dogs. KY (3 or 10 mg/kg) dose-dependently increased the peak positive first derivative of left ventricular pressure ((+)LVdP/dt) and mean aortic pressure, and decreased the left ventricular end-diastolic pressure (LVEDP). Myocardial oxygen consumption (MVO2) and heart rate (HR) were not significantly influenced by KY. KY produced a cardiotonic effect without any increase in MVO2, because the increase in MVO2 due to the cardiotonic effect of KY may have been cancelled by a decrease in MVO2 due to reduction of preload and the lack of increase in HR. In order to clarify the relationship between the cardiovascular effects of KY and the drug concentration in plasma, the concentration of anti-bufalin IgG reactive substance (BRS) in plasma was measured by enzyme immunoassay. The maximum BRS concentrations 20 min after administration of 3 and 10 mg/kg KY were dose-dependent. From the relationship between changes in (+)LVdP/dt and changes in BRS concentration after administration of KY, it is inferred that the effective concentration of BRS in plasma at which KY produces a cardiotonic effect in dogs is approximately 2-3 ng/ml.
通过在麻醉开胸犬十二指肠内给予含蟾酥(蟾蜍毒液)的药物“救心”(KY),研究其对心血管系统的影响。KY(3或10毫克/千克)剂量依赖性地增加左心室压力的最大正向一阶导数((+)LVdP/dt)和平均主动脉压,并降低左心室舒张末期压力(LVEDP)。心肌耗氧量(MVO2)和心率(HR)未受KY显著影响。KY产生强心作用而MVO2无任何增加,因为KY强心作用导致的MVO2增加可能已被由于前负荷降低和HR未增加导致的MVO2降低所抵消。为阐明KY的心血管效应与血浆中药物浓度之间的关系,采用酶免疫分析法测定血浆中抗蟾蜍灵IgG反应性物质(BRS)的浓度。给予3和10毫克/千克KY后20分钟时的最大BRS浓度呈剂量依赖性。根据给予KY后(+)LVdP/dt变化与BRS浓度变化之间的关系,推断出KY在犬体内产生强心作用时血浆中BRS的有效浓度约为2 - 3纳克/毫升。