Schachter M
Department of Clinical Pharmacology, St Mary's Hospital, London, U.K.
J Clin Pharm Ther. 1991 Apr;16(2):79-91. doi: 10.1111/j.1365-2710.1991.tb00288.x.
Isradipine is a potent dihydropyridine calcium channel blocker. It is highly selective for vascular smooth muscle, with very few negative inotropic or chronotropic effects. It may have minor depressant effects on the sinoatrial node, hence reducing the incidence of reflex tachycardia. The drug is extensively metabolized in the liver, with several pharmacologically inactive metabolites. As the elimination half-life is about 9 h the drug is usually given twice daily, but a once-daily modified release form is under investigation. Isradipine is effective monotherapy in essential hypertension, and has been successfully combined with pindolol and captopril. On the basis of more limited evidence it also appears to be beneficial in stable angina and in congestive cardiac failure. A trial is also under way to assess its antiatherogenic properties. Adverse effects are those predicted for a vasodilator calcium antagonist, and may be less frequent than for equivalent doses of nifedipine. This needs to be confirmed by more extensive clinical experience. Overall, isradipine can be considered favourably in essential hypertensives where a calcium channel blocker is indicated, particularly if it is desirable to avoid myocardial depression or to minimize reflex tachycardia. Its role in other cardiovascular disease awaits further evaluation.
伊拉地平是一种强效二氢吡啶类钙通道阻滞剂。它对血管平滑肌具有高度选择性,几乎没有负性肌力或负性变时作用。它可能对窦房结有轻微抑制作用,从而降低反射性心动过速的发生率。该药物在肝脏中广泛代谢,产生几种无药理活性的代谢产物。由于消除半衰期约为9小时,该药物通常每日给药两次,但每日一次的缓释剂型正在研究中。伊拉地平是原发性高血压的有效单一疗法,并且已成功与吲哚洛尔和卡托普利联合使用。基于更有限的证据,它在稳定型心绞痛和充血性心力衰竭中似乎也有益处。一项评估其抗动脉粥样硬化特性的试验也正在进行中。不良反应是血管扩张性钙拮抗剂所预期的,并且可能比同等剂量的硝苯地平更不常见。这需要更广泛的临床经验来证实。总体而言,在需要使用钙通道阻滞剂的原发性高血压患者中,可以考虑使用伊拉地平,特别是如果希望避免心肌抑制或尽量减少反射性心动过速。它在其他心血管疾病中的作用有待进一步评估。