临床药理学的普鲁氯嗪健康的年轻男性。

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Isah AO,罗林斯博士贝特曼DN

临床药理学的普鲁氯嗪健康的年轻男性。

Br中国新药杂志。1991;12月32 (6):677 - 84。

PubMed ID
1768559 (在PubMed
]
文摘

1。普鲁氯嗪的药代学和药效学(PCZ)研究了单12.5毫克输液后健康的年轻男性和50毫克口服剂量,在重复剂量为14天(25毫克每天两次)。2。口服生物利用度很低,一个N-desmethyl代谢物检测。等离子体间隙高(0.98 - 1公斤h)和分布的体积大(12.9 - 1公斤)在静脉输液给药。3所示。PCZ的终端消除半衰期是9 + / - 1 h和8 + / - 2 h后静脉输液和单一口服给药,分别。药物和代谢物的尿复苏是低。4所示。积累PCZ及其代谢物发生后重复给药。 The half-life at the end of 14 days therapy was 18 +/- 4 h. 5. Postural tachycardia, decreased salivary flow, impaired psychomotor function and a diminished level of arousal were observed after intravenous PCZ. Similar effects, but of lower magnitude were observed after single oral doses. During chronic dosing postural tachycardia and antihistaminic effects were observed, the latter not being observed after single doses. 6. After single intravenous dosing the maximal drug effects occurred 2-4 h after peak plasma drug concentrations for all measures except for plasma prolactin and self-scored restlessness 7. An antagonist action at dopamine (D2), muscarinic-cholinergic and alpha-adrenoceptors is postulated after single doses, with antihistaminic effects during chronic dosing, possibly indicating the presence of an active metabolite.

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药物
药物靶点
药物 目标 生物 药理作用 行动
普鲁氯嗪 alpha -肾上腺素能受体(蛋白质组) 蛋白质组 人类
未知的
拮抗剂
细节
普鲁氯嗪 α2肾上腺素能受体(蛋白质组) 蛋白质组 人类
没有
拮抗剂
细节
普鲁氯嗪 组胺H1受体 蛋白质 人类
未知的
拮抗剂
细节
药物反应
反应
细节