Herbette L G, Mason P E, Gaviraghi G, Tulenko T N, Mason R P
Department of Radiology, University of Connecticut Health Center, Farmington 06030, USA.
J Cardiovasc Pharmacol. 1994;23 Suppl 5:S16-25.
Membrane-active drugs can be characterized by direct measurements of their membrane partition coefficients, washout rates from membranes, and washin rates into membranes. There appears to be a correlation between the duration of action of such membrane-active drugs and the membrane partition coefficient in conjunction with the washout rate. Lacidipine has a high membrane partition coefficient compared to other 1,4-dihydropyridine calcium-channel antagonists and a slow washout rate from membranes. Clinically, it also exhibits an extended duration of action. This control at the membrane molecular level may provide an optimal pharmacokinetic profile for lacidipine in the treatment of hypertension. In addition, these same properties may be important for lacidipine as an antiproliferative agent in the treatment of atherosclerosis.
膜活性药物可通过直接测量其膜分配系数、从膜中的洗脱速率以及进入膜中的洗脱速率来表征。这类膜活性药物的作用持续时间与膜分配系数以及洗脱速率之间似乎存在相关性。与其他1,4 -二氢吡啶类钙通道拮抗剂相比，拉西地平具有较高的膜分配系数和较慢的从膜中的洗脱速率。在临床上，它也表现出延长的作用持续时间。这种在膜分子水平上的调控可能为拉西地平治疗高血压提供最佳的药代动力学特征。此外，这些相同的特性对于拉西地平作为治疗动脉粥样硬化的抗增殖剂可能也很重要。
