McAllister R G
J Clin Pharmacol. 1975 Nov-Dec;15(11-12):771-8. doi: 10.1002/j.1552-4604.1975.tb02341.x.
Guanethidine sulfate, a potent antihypertensive agent with a prolonged duration of action, was given in large oral doses to eight hypertensive patients in a loading technique. Blood pressure control resulted within one to three days without side effects, with total loading doses varying from 125 to 650 mg. Based on the drug's pharmacokinetic properties, a maintenance dose required to sustain the desired antihypertensive effects was calculated from the loading dose for each individual. Blood pressure was satisfactorily controlled in the seven patients followed for at least 12 months, and no modification of the calculated guanethidine dose was required. Side effects were minimal and well tolerated. The ease of initial blood pressure regulation with this regimen and the precision with which a maintenance dose can be determined suggest that guanethidine deserves a more prominent role in the therapy of established hypertension.
硫酸胍乙啶是一种作用持久的强效抗高血压药物,采用负荷给药技术对8例高血压患者给予大剂量口服。1至3天内血压得到控制,且无副作用,总负荷剂量为125至650毫克。根据该药物的药代动力学特性,从每个个体的负荷剂量计算出维持所需降压效果所需的维持剂量。对7例随访至少12个月的患者,血压得到了满意控制,无需调整计算出的胍乙啶剂量。副作用极小且耐受性良好。该方案初始血压调节的简便性以及确定维持剂量的精确性表明,胍乙啶在已确诊高血压的治疗中应发挥更突出的作用。