及时给予尼索地平对预防心肌ATP分解至关重要。

Timely administration of nisoldipine essential for prevention of myocardial ATP catabolism.

作者信息

De Jong J W

出版信息

Eur J Pharmacol. 1985 Nov 26;118(1-2):53-9. doi: 10.1016/0014-2999(85)90662-4.

Abstract

Calcium entry blockers can effectively preserve high-energy phosphates in ischemic heart. However, little is known about the optimal timing of drug therapy. The moment of nisoldipine administration in relation to its protective efficacy during ischemia and reperfusion was studied in rat hearts. Nisoldipine (50 nM), given some time before a reduction of about 90% in coronary flow diminished ATP-catabolite efflux during both ischemia and reperfusion by up to 85%. In contrast, drug administration at the onset of ischemia, or during ischemia or during reperfusion was completely without protective effect. Similarly, early nisoldipine application gave rise to ischemic ATP, adenylate charge and creatine phosphate values higher than those in untreated or late-treated hearts. Nisoldipine decreased the tension developed before ischemia by up to 66%, without affecting (post)ischemic function. Nisoldipine spares energy effectively only if administered to the heart prior to ischemia. This presumably has to do with its negative inotropy before flow reduction.

摘要

钙通道阻滞剂可有效保护缺血心脏中的高能磷酸化合物。然而，关于药物治疗的最佳时机却知之甚少。我们在大鼠心脏中研究了尼索地平给药时间与其在缺血和再灌注期间保护效果的关系。在冠状动脉血流量减少约90%之前的一段时间给予尼索地平（50 nM），可使缺血和再灌注期间的ATP分解代谢产物外流量减少多达85%。相比之下，在缺血开始时、缺血期间或再灌注期间给药则完全没有保护作用。同样，早期应用尼索地平可使缺血时的ATP、腺苷酸能荷和磷酸肌酸值高于未治疗或晚期治疗的心脏。尼索地平可使缺血前产生的张力降低多达66%，而不影响（缺血后）心脏功能。尼索地平只有在缺血前给药才能有效节省能量。这可能与其在血流量减少前的负性肌力作用有关。