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降压药吡那地尔(Pinacidil)是通过开放平滑肌细胞膜钾通道使之超极化,而直接松弛血管壁。可称为钾通道开放剂(Potassiun channel openers)。药动学:鼠和狗口服本品后,迅速完全吸收,0.5～1小时达血浆峰浓度。生物利用度分别为80％(鼠)和100％(狗),说明鼠有首过效应。血浆半衰期分别为1和2小时。肝、肾分布容积较大。本品在肝内通过生物转化变成本品的N-氧化物后,由肾排泄;该代谢产物有部分可逆性。药效学:鼠口服本品单剂的降压效果,
Pinacidil, a hypotensive drug, directly relaxes the vascular wall by opening the potassium channel of the smooth muscle cell to hyperpolarization. Can be called Potassiun channel openers. Pharmacokinetics: rats and dogs oral administration of this product, quickly and completely absorbed, 0.5 ~ 1 hour plasma peak concentration. Bioavailability was 80% (mouse) and 100% (dog), indicating that the first-pass effect of the mouse. Plasma half-lives were 1 and 2 hours, respectively. Liver, kidney distribution volume larger. This product in the liver through biological transformation into the product of N-oxide, excreted by the kidneys; the metabolites are partially reversible. Pharmacodynamics: rat oral administration of this product single-agent antihypertensive effect,