[14C] -布美他尼在人体中的代谢情况。
Fate of [14C]-bumetanide in man.
作者信息
Pentikäinen P J, Penttilä A, Neuvonen P J, Gothoni G
出版信息
Br J Clin Pharmacol. 1977 Feb;4(1):39-44. doi: 10.1111/j.1365-2125.1977.tb00664.x.
Abstract
- The fate of bumetanide was studied in four healthy volunteers both after intravenous oral administration of [14C]-bumetanide (0.5 mg). 2. The absorption of oral [14C]-bumetanide was rapid (absorption half-life 0.61 h) and complete with a urinary recovery of about 80% of the intravenous or oral dose during 48 h. 3. The elimination of [14C]-bumetanide was rapid with a half-life of elimination (T 1/2 beta) of 1.5 h. 4. Protein bound fraction of [14C]-bumetanide in plasma was 95%. No bumetanide was found in red blood cells. 5. Four metabolites of [14C]-bumetanide were found in urine. Together they accounted for about one third of the radio-activity excreted into urine during the first 6 h after the administration of the drug. 6. Bumetanide is rapidly and completely absorbed from the gastrointestinal tract, bound extensively to plasma proteins, metabolized to some extent and excreted rapidly, principally into urine.
摘要
- 在4名健康志愿者静脉注射和口服[14C] -布美他尼（0.5毫克）后，对布美他尼的转归进行了研究。2. 口服[14C] -布美他尼吸收迅速（吸收半衰期0.61小时），且在48小时内尿中回收率约为静脉注射或口服剂量的80%，吸收完全。3. [14C] -布美他尼消除迅速，消除半衰期（T 1/2β）为1.5小时。4. 血浆中[14C] -布美他尼的蛋白结合率为95%。在红细胞中未发现布美他尼。5. 尿中发现了[14C] -布美他尼的4种代谢产物。给药后最初6小时内，它们合起来约占排泄到尿中的放射性的三分之一。6. 布美他尼从胃肠道迅速且完全吸收，与血浆蛋白广泛结合，在一定程度上被代谢，并迅速排泄，主要排泄到尿中。
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