临床torasemide的药代学和药效学。

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可耐福H, Mutschler E

临床torasemide的药代学和药效学。

Pharmacokinet。1998年1月,34 (1):24。doi: 10.2165 / 00003088-199834010-00001。

PubMed ID
9474471 (在PubMed
]
文摘

新循环利尿剂torasemide属于吡啶磺酰脲类类。它是吸收和产量在健康个体bioavailablity约80%,甚至更高的患者的水肿。beplayapp这是大约两倍的“古典”循环利尿剂呋喃苯胺酸(速尿灵)[26 - 65%]。Torasemide高度绑定到蛋白质是呋喃苯胺酸(99%)。的体积分布torasemide被确定为0.2 L /公斤与0.11 - 0.18 L /公斤呋喃苯胺酸。Torasemide经历广泛的肝代谢;只有20%的家长尿液中药物恢复不变。相比之下只有10到20%的呋喃苯胺酸进行二期metabolisation(葡糖苷酸)。torasemide在慢性肾功能衰竭肾清除率下降比例的降低患者的肾小球滤过率,而总等离子体间隙的肾清除率(3倍)似乎是独立于肾功能。正如所料,torasemide的肾排泄代谢产物在肾脏疾病明显迟钝。 The pharmacokinetics of torasemide are significantly influenced by liver disease. Total plasma clearance of torasemide was reduced to about half of that found in the control group, yielding an increase in elimination half-life. A greater than normal fraction of torasemide was recovered in the urine of patients with cirrhosis. In contrast, the kinetics of furosemide appeared to depend more on kidney function than on liver disease. The pharmacodynamics of torasemide are principally the same as those reported from conventional loop diuretics due to their interference with one binding site in the thick ascending limb of Henle's loop, the Na+:K+:2Cl- carrier. The maximum natriuretic effect of all loop diuretics amounts to about 3 mmol Na+/min. Members of this class differ, however, with respect to their intravenous potency or affinity for the receptor, respectively: bumetanide > piretanide > torasemide > furosemide. So far, the only loop diuretic which has been shown to effectively lower high blood pressure is torasemide. This effect occurs at the low dose of 2.5 mg/day.

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药物
药物载体
药物 航空公司 类 生物 药理作用 行动
Torasemide 血清白蛋白 蛋白质 人类
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