Stieber Juliane
Institute for Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander-University, Erlangen-Nuremberg, Germany.
Methods Find Exp Clin Pharmacol. 2008 Oct;30(8):633-41. doi: 10.1358/mf.2008.30.8.1268816.
Ivabradine has been approved as a heart rate-lowering agent for use in the treatment of chronic stable angina pectoris in case of contraindication or intolerance to beta-blockers. This drug effectively lowers the heart rate by inhibiting the pacemaker current I(f) in the sinoatrial node. It appears to induce fewer adverse reactions than other drugs used for reducing the heart rate, such as calcium channel blockers or beta-blockers. Because of this favorable profile, ivabradine could become the first-choice drug when pure heart rate-lowering is the therapeutic goal. This review evaluates experimental and preclinical data to investigate the possibilities, as well as the limitations, of the clinical use of ivabradine. In experimental studies, it has been shown that ivabradine does have some unfavorable pharmacodynamic properties, such as the block of all four hyperpolarization-activated cyclic nucleotide-gated channels and block of other ion channels at high concentrations. Clinical studies, however, indicate that those properties do not result in clinical consequences as long as ivabradine is given at the recommended dose and contraindications are strictly observed.
伊伐布雷定已被批准作为一种降低心率的药物，用于在禁忌使用β受体阻滞剂或对其不耐受的情况下治疗慢性稳定性心绞痛。该药物通过抑制窦房结中的起搏电流I(f)有效降低心率。与其他用于降低心率的药物（如钙通道阻滞剂或β受体阻滞剂）相比，它似乎引起的不良反应更少。由于这种良好的特性，当单纯降低心率是治疗目标时，伊伐布雷定可能成为首选药物。本综述评估了实验和临床前数据，以研究伊伐布雷定临床应用的可能性及局限性。在实验研究中，已表明伊伐布雷定确实具有一些不良的药效学特性，例如阻断所有四种超极化激活的环核苷酸门控通道以及在高浓度下阻断其他离子通道。然而，临床研究表明，只要按照推荐剂量给药并严格遵守禁忌证，这些特性不会导致临床后果。
