Plosker G L, Faulds D
Adis International Limited.
Drugs. 1996 Aug;52(2):232-53. doi: 10.2165/00003495-199652020-00009.
Nisoldipine coat-core is a long-acting formulation of the dihydropyridine calcium antagonist (calcium channel blocker) nisoldipine, suitable for once daily administration in the treatment of patients with hypertension. In clinical trials in patients with mild to moderate hypertension, nisoldipine coat-core has efficacy and tolerability similar to those of other calcium antagonists, and antihypertensive efficacy equivalent to that of agents from various other drug classes including beta-blockers, thiazide diuretics and ACE inhibitors. Unlike beta-blockers and thiazide diuretics, calcium antagonists (including nisoldipine coat-core) are not associated with clinically significant adverse metabolic effects on the serum lipid profile or glycaemic control. Nevertheless, published guidelines or consensus papers on the pharmacological management of patients with hypertension recommend calcium antagonists (and other drugs) as "alternative first-line' agents, while beta-blockers and diuretics are generally considered to be first-line therapy because of demonstrated benefits in terms of cardiovascular morbidity and mortality in this clinical setting. Nisoldipine coat-core maintains consistent plasma drug concentrations and antihypertensive effects throughout the 24-hour dosage interval, thereby attenuating intermittent reflex increases in sympathetic activity. This pharmacological profile may have important clinical implications; recent retrospective data suggest an association between moderate to high dosages of short-acting dihydropyridine calcium antagonists and adverse cardiovascular events, although this has yet to be confirmed in large prospective trials. In addition, the high degree of vasoselectivity of nisoldipine minimises negative inotropic effects which may be observed with less selective agents such as nifedipine. Nisoldipine coat-core is, therefore, a useful alternative to other antihypertensive agents in the management of patients with hypertension, providing consistent antihypertensive efficacy and good tolerability with once daily administration.
尼索地平包芯片是二氢吡啶类钙拮抗剂（钙通道阻滞剂）尼索地平的长效制剂，适用于高血压患者每日一次给药治疗。在轻度至中度高血压患者的临床试验中，尼索地平包芯片的疗效和耐受性与其他钙拮抗剂相似，降压疗效与包括β受体阻滞剂、噻嗪类利尿剂和血管紧张素转换酶抑制剂在内的其他各类药物相当。与β受体阻滞剂和噻嗪类利尿剂不同，钙拮抗剂（包括尼索地平包芯片）对血清脂质谱或血糖控制无临床显著不良代谢影响。然而，已发表的关于高血压患者药物治疗的指南或共识文件推荐钙拮抗剂（及其他药物）作为“替代一线”药物，而β受体阻滞剂和利尿剂通常被视为一线治疗药物，因为在这种临床情况下它们在心血管发病率和死亡率方面已显示出益处。尼索地平包芯片在整个24小时给药间隔内维持稳定的血浆药物浓度和降压效果，从而减弱交感神经活动的间歇性反射性增加。这种药理学特性可能具有重要的临床意义；最近的回顾性数据表明，中高剂量的短效二氢吡啶类钙拮抗剂与不良心血管事件之间存在关联，尽管这一点尚未在大型前瞻性试验中得到证实。此外，尼索地平的高血管选择性可将负性肌力作用降至最低，而硝苯地平等选择性较低的药物可能会出现这种作用。因此，在高血压患者的治疗中，尼索地平包芯片是其他抗高血压药物的有用替代品，每日一次给药可提供持续的降压疗效和良好的耐受性。
