Zannad F, Royer-Morrot M J, Zakari I, Sadoul N, Royer R J
Laboratoire de Pharmacologie Clinique, Nancy, France.
Fundam Clin Pharmacol. 1987;1(3):219-24. doi: 10.1111/j.1472-8206.1987.tb00560.x.
Twelve patients with acute myocardial infarction were given 1.5 mg/kg/5 min bolus +0.4 mg/kg/hr 6 hr IV infusion of disopyramide followed by 250 mg twice daily of a slow-release oral formulation of this drug. Plasma concentrations of total disopyramide rapidly reached steady-state within the therapeutic margins. The plasma steady-state concentrations of the major metabolite mono-N-dealkyl-disopyramide (MND) showed large intra-individual variations. There was no correlation between plasma levels of either disopyramide or MND and the occurrence of anticholinergic side effects. The drug had no significant effect on mean blood pressure, heart rate, or ECG intervals. This therapeutic regimen, including conversion from the IV form to oral slow-release tablets, could be recommended in myocardial infarction.
12例急性心肌梗死患者接受了丙吡胺治疗,静脉推注剂量为1.5mg/kg,5分钟内推注完毕,随后6小时以0.4mg/kg/小时的速度静脉输注,之后给予该药物的缓释口服制剂,每日两次,每次250mg。总丙吡胺的血浆浓度在治疗范围内迅速达到稳态。主要代谢产物单-N-去烷基丙吡胺(MND)的血浆稳态浓度在个体间存在较大差异。丙吡胺或MND的血浆水平与抗胆碱能副作用的发生之间没有相关性。该药物对平均血压、心率或心电图间期没有显著影响。这种治疗方案,包括从静脉剂型转换为口服缓释片,可推荐用于心肌梗死患者。