Jain D, Dasgupta P, Hughes L O, Lahiri A, Raftery E B
Department of Cardiology, Northwick Park Hospital and Clinical Research Centre, Harrow, Middlesex, England.
Eur J Clin Pharmacol. 1990;38(2):111-4. doi: 10.1007/BF00265967.
Ranolazine (RS-43285) has been shown to possess significant anti-ischaemic properties in a canine model of reversible myocardial ischaemia. The clinical efficacy of this new agent was assessed by a single blind, placebo controlled study of 14 patients with chronic stable angina. A 2 week placebo phase was followed by therapy with 30 mg and 60 mg of ranolazine tid for 2 weeks each. Graded, symptom limited treadmill exercise tests were performed at the end of each phase, 1.5 h (AM) and 7 h (PM) after the morning dose. An additional exercise test 1.5 h after the first dose of 30 mg was included to assess the acute dose response. In the AM study, the mean exercise time increased from 6.9 min (placebo) to 7.8 min after the first dose of 30 mg and to 8.2 min and 8.5 min respectively at the end of 30 mg and 60 mg phases. In the PM study, exercise time improved from 6.5 min (placebo) to 8.2 min and 7.8 min respectively at the end of 30 mg and 60 mg phases. The time to onset of angina showed a similar improvement. No significant changes were observed in the resting and peak exercise heart rates and blood pressure. This preliminary study suggests that ranolazine may significantly prolong exercise time in patients with stable coronary artery disease without altering heart rates and blood pressure.
雷诺嗪（RS - 43285）已被证明在犬可逆性心肌缺血模型中具有显著的抗缺血特性。通过一项对14例慢性稳定型心绞痛患者进行的单盲、安慰剂对照研究，评估了这种新药的临床疗效。先进行为期2周的安慰剂阶段，随后分别用30毫克和60毫克雷诺嗪每日三次治疗，各治疗2周。在每个阶段结束时、晨服后1.5小时（上午）和7小时（下午）进行分级、症状受限的平板运动试验。在首次服用30毫克后1.5小时额外进行一次运动试验，以评估急性剂量反应。在上午的研究中，平均运动时间从6.9分钟（安慰剂）在首次服用30毫克后增加到7.8分钟，在30毫克和60毫克阶段结束时分别增加到8.2分钟和8.5分钟。在下午的研究中，运动时间在30毫克和60毫克阶段结束时分别从6.5分钟（安慰剂）改善到8.2分钟和7.8分钟。心绞痛发作时间也有类似改善。静息和运动高峰时的心率及血压未观察到显著变化。这项初步研究表明，雷诺嗪可能显著延长稳定型冠状动脉疾病患者的运动时间，而不改变心率和血压。
