Friedel H A, Sorkin E M
ADIS Drug Information Services, Auckland, New Zealand.
Drugs. 1988 Dec;36(6):682-731. doi: 10.2165/00003495-198836060-00003.
Nisoldipine is an orally administered calcium entry blocking drug structurally related to nifedipine. In limited clinical trials it has been shown to be effective and relatively well tolerated in the treatment of patients with chronic stable angina pectoris and mild to moderate essential hypertension. As for all dihydropyridine-calcium antagonists, its major properties include potent peripheral and coronary vasodilation and improvement in myocardial oxygen supply relative to demand. These actions occur without depression of cardiac conduction or left ventricular function. Short term clinical trials have shown nisoldipine to produce both symptomatic and objective improvements in patients with chronic angina of effort and have suggested a benefit in vasospastic angina. A small number of comparative trials indicate that nisoldipine is equally as effective as nifedipine. In addition, in combination with beta-adrenoceptor blockade nisoldipine appears to offer additional benefit compared with beta-blockade alone and is well tolerated. In patients with mild to moderate essential hypertension nisoldipine monotherapy, in 1 or 2 daily doses, has maintained blood pressure control and has also been a useful addition to diuretics and beta-adrenoceptor blocking drugs in patients with poorly controlled disease. Side effects appear to be dose related, generally mild and transient, and are primarily those resulting from potent peripheral vasodilation - headache, flushing and pretibial or ankle oedema. Although studies to date are promising, there are no published long term studies (greater than 1 year) of nisoldipine in comparison with other calcium entry blockers and other drugs currently in clinical use for the treatment of angina pectoris or hypertension. Until such studies are completed the exact place of nisoldipine in the treatment of these diseases remains to be established.
尼索地平是一种口服的钙通道阻滞剂，在结构上与硝苯地平相关。在有限的临床试验中，已证明它在治疗慢性稳定型心绞痛和轻度至中度原发性高血压患者时有效且耐受性相对良好。对于所有二氢吡啶类钙拮抗剂而言，其主要特性包括强效的外周和冠状动脉血管舒张作用以及心肌氧供与需求比值的改善。这些作用在不抑制心脏传导或左心室功能的情况下发生。短期临床试验表明，尼索地平可使劳力性慢性心绞痛患者在症状和客观指标上均得到改善，并提示对血管痉挛性心绞痛有益。少数比较试验表明，尼索地平与硝苯地平疗效相当。此外，与β-肾上腺素受体阻滞剂联合使用时，尼索地平似乎比单独使用β-阻滞剂更具优势，且耐受性良好。在轻度至中度原发性高血压患者中，尼索地平每日1或2次单药治疗可维持血压控制，对于血压控制不佳的患者，它也是利尿剂和β-肾上腺素受体阻滞剂的有用辅助药物。副作用似乎与剂量相关，一般较轻且为短暂性，主要是由强效外周血管舒张引起的——头痛、面部潮红和胫前或踝部水肿。尽管迄今为止的研究很有前景，但尚无关于尼索地平与其他钙通道阻滞剂及目前临床上用于治疗心绞痛或高血压的其他药物相比的长期研究（超过1年）发表。在完成此类研究之前，尼索地平在这些疾病治疗中的确切地位仍有待确定。
