摘要
卡维地洛是第三代β-受体拮抗剂,对于高血压和冠心病具有安全有效地舒张血管的作用。另外,它还具有强大的抗氧化性,在人血浆中的某些代谢产物的抗氧化性更强。这些性质使其能够治疗左室功能障碍和慢性心功能不全。文献报道卡维地洛可以逆转由P-糖蛋白介导的多药耐药现象(MDR),其逆转效果和维拉帕米相似,有望发展成为一种可应用于临床的P-糖蛋白抑制剂。本文综述了卡维地洛对于MDR的逆转活性,以及逆转MDR的机制方面的研究进展。
Carvedilol, belonging to the ‘third generation＇ of β-adrenoceptor antagonists, was designed and developed as a drug with vasodilating activity for efficacious and safe treatment of hypertension and coronary artery disease. In addition, carvedilol is a potent antioxidant, and some carvedilol metabolites found in human plasma even exhibit greater antioxidative activity than carvedilol itself. These unique properties of carvedilol may be important in preventing progressive deterioration of left ventricular dysfunction and chron- ic heart failure. Recently, carvedilol has been demonstrated to reverse P-glycoprotein-mediated multidrug resistance （MDR）. Its reversal effects were comparable to verapamil and it was hopeful to be a clinical P-gp inhibitor. This review introduces its reversal activity and usefulness against MDR, as well as overviews of the mechanism by which carvedilol reverses MDR.
出处
《药学与临床研究》
2010年第1期64-66,共3页
Pharmaceutical and Clinical Research
