临床药物动力学的一些更新的利尿剂。

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Beermann B,磨米

临床药物动力学的一些更新的利尿剂。

Pharmacokinet。1987年10月,13 (4):254 - 66。doi: 10.2165 / 00003088-198713040-00003。

PubMed ID
3311532 (在PubMed
]
文摘

目前已经开发出了一些新的利尿剂。本文总结了发表其中一些知识。Azosemide循环利尿剂。生物利用度约为15%,它的半衰期为2到3小时。肾和non-renal间隙是1.32和5.4 L / h,分别。Etozolin也是一个循环利尿剂。它正迅速代谢活性代谢物,ozolinone。的胃肠吸收etozolin几乎是完整的。血浆半衰期etozolin和ozolinone 2和10小时,分别。化合物主要是消除代谢物。 Renal and liver impairment do not seem to change the pharmacokinetics. Fenquizone has properties similar to the thiazides. The plasma half-life is approximately 17 hours. Apparent volume of distribution averaged 686 L and renal clearance is 7.2 L/h. Indapamide acts predominantly on the proximal segment of the distal tubule and also has direct vasodilatory effects. Gastrointestinal uptake is at least 80%. The drug binds highly to carbonic anhydrases of red blood cells. Protein binding is about 80%, while terminal plasma half-life is 15 hours and the apparent volume of distribution 25 L. Renal clearance is 0.3 L/h and non-renal clearance 0.9 L/h. Several metabolites have been described, of which one major metabolite is pharmacologically active. Muzolimine is a loop diuretic. Its uptake is almost complete, but decreased substantially by food. The protein binding is about 65%, the apparent volume of distribution is about 1 L/kg and average terminal half-life 10 to 20 hours. Elimination is mainly non-renal, and non-renal clearance ranges between 0.5 and 1.32 L/h. The pharmacokinetics of the drug do not seem to be changed in cardiac failure. Terminal plasma half-life is essentially unchanged in patients with renal failure, except in those with very severe reduction of glomerular filtration rate. Piretanide is a loop diuretic which is about 6 times as potent as frusemide (furosemide). Its bioavailability is most likely complete in healthy subjects and in renal patients. Protein binding in healthy subjects is about 95%. The plasma half-life of the drug is about 1 hour and apparent volume of distribution averages about 17 L. Renal and non-renal clearance are about 6 L/h, although renal clearance is decreased in renal failure: this decrease is correlated with glomerular filtration rate. Non-renal clearance is unchanged in renal failure, as is the apparent volume of distribution.(ABSTRACT TRUNCATED AT 400 WORDS)

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