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具有扩张血管作用的新一代β受体阻滞剂兼有α受体和β受体阻滞作用,其血液动力学模型与常规β受体阻滞剂不同。降低总外周血管阻力的作用在理论上为治疗原发性高血压提供了更为合理的方法。然而,不甚理想的是长期应用时α1受体阻滞作用尚不肯定(如拉贝洛尔)。拉贝洛尔和卡维地洛是具有不同药效学和药劝学性质的消旋混合物,有必要研究各种立体异构体的性质。目前获得的卡维地洛和拉贝洛尔的临床效果令人鼓舞,因此值得进一步开发江有α受体和β受体阻滞作用的药物,研究其药效学和药动学性质以及立体异构体之间的重要药效学和药动学差异。
A new generation of beta-blockers with vasodilator effects combines both alpha-receptor and beta-blocker effects with different hemodynamic models than conventional beta-blockers. The effect of reducing total peripheral vascular resistance has theoretically provided a more rational approach to the treatment of essential hypertension. However, it is less than ideal (for example, labetalol) for the role of α1 receptor blockade in long-term use. Labetalol and carvedilol are racemic mixtures with different pharmacodynamic and pharmacological properties and it is necessary to study the properties of various stereoisomers. The current clinical effects of carvedilol and labetalol are encouraging, and therefore it is worth furthering the development of a drug that has the effects of α-receptor and β-blocker and its pharmacodynamic and pharmacokinetic properties as well as three-dimensional Important pharmacodynamic and pharmacokinetic differences between isomers.