Bonadei Ivano, Vizzardi Enrico, Quinzani Filippo, Piovanelli Barbara, Rovetta Riccardo, D'Aloia Antonio, Cas Livio D
Section of Cardiovascular diseases, Department of Experimental and Applied Medicine, University of Study of Brescia.
Recent Pat Cardiovasc Drug Discov. 2011 Sep;6(3):215-21. doi: 10.2174/157489011797377103.
Chronic stable angina affects 6-7 million Americans and contributes to a significant reduction in quality of life and life expectancy. Current pharmacotherapy for reducing episodes of exertional angina includes β-blockers, calcium channel blockers and long-acting nitrates. Patients may have contraindications to the use of one or more of these agents or be unable to tolerate initial or larger therapeutic doses. As a result of the inability of current management strategies to optimally control episodes of chronic angina, new therapies have been investigated that do not have some of the limitations of current therapies. New therapies for chronic stable angina are based on a mechanism involving membrane current such as the funny current and the late Na current. Ranolazine (Ran) is an antianginal drug acting on I(Na). After its current indication in the chronic stable angina, the role of this molecule is still being studied for prophylaxis of certain arrhythmias and treatment of heart failure. Moreover, have been recently developed new interesting patents of novel pharmaceutical effects and derivates of Ran.
慢性稳定型心绞痛影响着600万至700万美国人,显著降低了生活质量和预期寿命。目前用于减少劳力性心绞痛发作的药物治疗包括β受体阻滞剂、钙通道阻滞剂和长效硝酸盐类药物。患者可能对使用这些药物中的一种或多种存在禁忌,或者无法耐受初始或更大的治疗剂量。由于目前的管理策略无法最佳地控制慢性心绞痛发作,因此人们研究了一些没有当前疗法某些局限性的新疗法。慢性稳定型心绞痛的新疗法基于一种涉及膜电流的机制,如起搏电流和晚钠电流。雷诺嗪(Ran)是一种作用于I(Na)的抗心绞痛药物。在其目前用于慢性稳定型心绞痛的适应症之后,该分子在预防某些心律失常和治疗心力衰竭方面的作用仍在研究中。此外,还开发了关于雷诺嗪新的有趣的药物效应和衍生物的新专利。