临床内科病例500份-251.pptVIP

谢谢大家！ * * 这是一张关于美托洛尔平片的血浆药物浓度和时间关系的示意图.口服美托洛尔平片1-2小时后,药物浓度达到峰值,随后药物浓度衰减,其衰减速度由药物的半衰期所决定. 倍他受体阻滞剂在峰值浓度时可以导致过度的β1阻滞，同时即使是对心脏选择性的β受体阻滞剂也会干扰β2受体.况且,在给药后期由于血药浓度低于有效治疗浓度,会失去β1阻滞作用.因此阿斯利康公司决定开发倍他乐克缓释制剂,以达到一天一次,24小时保持平稳的有效血药浓度 This slides illustrates plasma concentration over time for an immediate release tablet. The plasma concentration reaches a peak 1-2 hours after tablet intake and thereafter follows a decline depending on the half-life of the drug. For a beta-blocker the plasma peak can lead to too much beta1-blockade, and for a cardioselective beta-blocker also interference with beta2-receptors