临床药理学的doxazosin原发性高血压患者。

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Cubeddu LX, Fuenmayor N, Caplan N,渡轮D

临床药理学的doxazosin原发性高血压患者。

中国新药杂志。1987年4月,41 (4):439 - 49。doi: 10.1038 / clpt.1987.54。

PubMed ID

2951051 (在PubMed

]

文摘

Doxazosin是一个新的喹唑啉衍生物,如哌唑嗪、选择性α1-receptors。三方交叉、随机、开放研究原发性高血压患者在18进行调查的临床药物动力学2,4,8毫克doxazosin在稳定状态。最初的2毫克剂量的药物代谢动力学情况也进行了研究。Doxazosin显示线性药物动力学。从2到8毫克剂量的增加(稳态)生产比例增加doxazosin血清水平(最大血浆药物浓度(Cmax)最低血浆药物浓度(C min),和O-24-hour曲线下面积(AUC (p-24)),而半衰期(t1/2)(分别为19.4、18.7和19.7小时),体积的分布(3.4,3.4,和3.6 L /公斤,分别),从血清间隙(2.2,2.2,和2.1毫升/分钟/公斤,分别),和程度的蛋白质绑定(分别为1.2%、1.0%和1.0%的)剂量无关。类似t1/2和时间达到峰值浓度(达峰时间)获得了2毫克初始剂量和2毫克稳定状态。α1-Acid doxazosin治疗期间糖蛋白水平持平。Doxazosin降低仰卧位和站的收缩压和舒张压。降低血压与心率的增加有关。峰值降血压药和tachycardic效果发生5.7 + / - 0.1小时后政府,而Cmax实现2.4 + / - 0.7小时(达峰时间)。 Greater decreases in systolic blood pressure and increases in heart rate were seen in standing than in supine position. The reduction in standing systolic and diastolic blood pressure with 8 mg was greater than with 2 mg (P less than 0.05); however, the increases in heart rate were not different. Dizziness, headaches, and dry mouth were the most frequent side effects. This study indicates that doxazosin shows linear pharmacokinetics between 2 and 8 mg and that because of its long t1/2, once-a-day administration should be adequate for the treatment of hypertension.

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药物

Doxazosin