Wallin J D
Department of Medicine, Tulane University School of Medicine, New Orleans, LA 70112.
Am Heart J. 1990 Feb;119(2 Pt 2):434-7. doi: 10.1016/s0002-8703(05)80064-x.
Nicardipine hydrochloride, a dihydropyridine calcium entry-blocking drug, was administered to 66 patients with severe hypertension during three protocols designed to examine the efficacy and safety of this investigation drug. It was shown that nicardipine was uniformly effective in lowering blood pressure to a therapeutic goal of 95 mm Hg. Time to achieve therapeutic effect was dose dependent, and steady-state blood levels were achieved after 8 to 12 hours. Reductions in both systolic and diastolic blood pressure but not changes in heart rate were correlated with plasma concentrations of nicardipine. In dose-ranging studies, the minimal effective dose of nicardipine appeared to be 2 mg/hr; 1 mg/hr was an ineffective dose, and little additional effect was seen above 4 mg/hr. Side effects were modest and consisted of those associated with vasodilation--headache, flushing, and feelings of warmth. In the initial group of patients studied, local thrombophlebitis occurred in a substantial number of patients. This was seen only after 14 hours of infusion. In subsequent studies, the infusion site was changed after 12 hours, and no further cases of thrombophlebitis were seen. Nicardipine appears to be therapeutic agent for parenteral use that shows promise in the treatment of severe hypertension.
盐酸尼卡地平是一种二氢吡啶类钙通道阻滞剂，在旨在检验该研究药物疗效和安全性的三个方案中，对66例重度高血压患者使用了该药。结果显示，尼卡地平能一致有效地将血压降至95毫米汞柱的治疗目标。达到治疗效果的时间呈剂量依赖性，8至12小时后达到稳态血药浓度。收缩压和舒张压的降低与尼卡地平的血浆浓度相关，但心率无变化。在剂量范围研究中，尼卡地平的最小有效剂量似乎为2毫克/小时；1毫克/小时为无效剂量，4毫克/小时以上几乎未见额外效果。副作用较轻，包括与血管扩张相关的症状——头痛、脸红和发热感。在最初研究的患者组中，相当多患者出现了局部血栓性静脉炎。这仅在输注14小时后出现。在随后的研究中，12小时后更换了输注部位，未再出现血栓性静脉炎病例。尼卡地平似乎是一种有前途的用于治疗重度高血压的胃肠外给药治疗药物。
