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乌拉地尔通过阻断突触后α-受体,扩张末梢血管降低血压,本品还具有中枢性交感神经活性抑制作用及轻度的β_1阻断作用。本品降压效果迅速且明显,但持续时间短,将其微粒化,制成长效制剂可延长作用时间。含30mg本品的长效制剂的绝对生物活性为56%,健康人的最高血浆浓度为279±46 ng/ml。本品与血浆蛋白结合率为80%。高血压合并症的定期血液透析患者6例使用本品,共8天,其中第1天和第8天每日给药1次15mg,第2~7日每日30mg。最高血浓度第1天为147.7±9.0ng/ml,第8天为183.2±42.4 ng/ml,最高血浓度达峰时间各为6.3±1.3和6.0±1.0小时。消除
Urapidil by blocking the post-synaptic α-receptor, peripheral blood vessels to lower blood pressure, the product also has a central sympathetic nerve activity and mild β 1 blocking effect. This product antihypertensive effect is rapid and obvious, but the duration is short, it will be micronized, made of long-acting agents can extend the action time. The absolute bioactivity of the long-acting formulation containing 30 mg of this product was 56%, and the highest plasma concentration of healthy persons was 279 ± 46 ng / ml. The goods and plasma protein binding rate of 80%. Hypertension complications in patients with hemodialysis in 6 patients using this product for a total of 8 days, of which 1 and 8 days daily administration of a 15mg, 2 to 7 days daily 30mg. The highest blood concentration was 147.7 ± 9.0 ng / ml on day 1, 183.2 ± 42.4 ng / ml on day 8, and the highest peak blood concentrations were 6.3 ± 1.3 and 6.0 ± 1.0 hours, respectively. eliminate