Sorkin E M, Clissold S P
Drugs. 1987 Apr;33(4):296-345. doi: 10.2165/00003495-198733040-00002.
Nicardipine is an antagonist of calcium influx through the slow channel of the cell membrane and has been shown to be an effective and relatively well-tolerated treatment for stable effort angina and rest angina due to coronary artery spasm, and mild to moderate hypertension. Although its exact mechanism of action in these disease states has not been precisely defined, the potent coronary and peripheral arterial dilator properties of nicardipine, with concomitant improvements in oxygen supply/demand and reductions in systemic vascular resistance, are of major importance. Clinical studies have shown that nicardipine appears to be effective in the treatment of chronic stable exercise-induced angina pectoris and possibly in angina at rest due to coronary artery spasm. In the treatment of stable angina, nicardipine has proved to be equally as effective as nifedipine. However, haemodynamic and clinical studies indicate that nicardipine may have a further advantage of not depressing cardiac conduction or left ventricular function, even in patients with compromised cardiac pumping ability. Nicardipine also appears to be useful as initial monotherapy or in combination with other antihypertensive drugs when used in the treatment of mild to moderate hypertension, and may have some advantages over other vasodilators in this regard in that it may not be as frequently associated with fluid retention or weight gain as other similar drugs. In the treatment of hypertension nicardipine has been shown to be as effective as drugs such as hydrochlorothiazide, cyclopenthiazide, propranolol and verapamil in short term studies although confirmation of its long term usefulness in well-designed clinical trials is still required. Similarly, although the use of nicardipine in other disorders such as congestive heart failure and cerebrovascular disease has provided encouraging preliminary results, more studies are needed to clarify its place in their treatment. Side effects appear to be dose related and more frequent within the first few weeks of therapy. Most of these effects are minor and transient in nature and include headache, flushing and peripheral oedema. Thus, there is no doubt that nicardipine provides a suitable alternative to other drugs available for the treatment of angina and hypertension. However, further well-designed comparative clinical trials are needed to clarify its relative place in the long term management of these disorders.
尼卡地平是一种通过细胞膜慢通道阻止钙内流的拮抗剂，已被证明是治疗稳定型劳力性心绞痛、冠状动脉痉挛所致静息性心绞痛以及轻至中度高血压的有效且耐受性相对良好的药物。尽管其在这些疾病状态下的确切作用机制尚未完全明确，但尼卡地平强大的冠状动脉和外周动脉扩张特性，以及随之而来的氧供/氧需改善和全身血管阻力降低，至关重要。临床研究表明，尼卡地平似乎对治疗慢性稳定型运动诱发的心绞痛有效，对冠状动脉痉挛所致静息性心绞痛可能也有效。在治疗稳定型心绞痛方面，尼卡地平已被证明与硝苯地平同样有效。然而，血流动力学和临床研究表明，即使在心脏泵血能力受损的患者中，尼卡地平可能还有一个额外的优势，即不会抑制心脏传导或左心室功能。尼卡地平在用于治疗轻至中度高血压时，作为初始单一疗法或与其他抗高血压药物联合使用似乎也很有用，在这方面它可能比其他血管扩张剂有一些优势，因为它可能不像其他类似药物那样频繁地与液体潴留或体重增加相关。在高血压治疗的短期研究中，尼卡地平已被证明与氢氯噻嗪、环戊噻嗪、普萘洛尔和维拉帕米等药物同样有效，不过仍需要精心设计的临床试验来证实其长期有效性。同样，尽管尼卡地平用于充血性心力衰竭和脑血管疾病等其他疾病的治疗已取得令人鼓舞的初步结果，但仍需要更多研究来明确其在这些疾病治疗中的地位。副作用似乎与剂量相关，在治疗的最初几周内更常见。这些影响大多性质轻微且短暂，包括头痛、脸红和外周水肿。因此，毫无疑问，尼卡地平为治疗心绞痛和高血压的其他可用药物提供了合适的替代选择。然而，需要进一步精心设计的比较临床试验来明确其在这些疾病长期管理中的相对地位。
