Lesne M
Department of Pharmacology, Catholic University of Louvain, Brussels, Belgium.
Arzneimittelforschung. 1988 Jan;38(1A):160-3.
The pharmacodynamic effects and the pharmacokinetic parameters of torasemide (1-isopropyl-3- ([4-(3-methyl-phenylamino)pyridine]-3-sulfonyl)urea) 20 mg and furosemide 40 mg were compared after oral and intravenous administration in 6 healthy volunteers. The plasma elimination half-life for i.v. and oral torasemide was 2.2 h and 2.8 h, its bioavailability after oral administration was 91%, about 25% of the total body clearance was due to renal excretion both after iv. or oral application. For furosemide, a plasma elimination half-life of 0.6 h for i.v. and 0.8 h for oral application was found. The bioavailability was 40%, and about 62% of the drug was excreted via the kidney. Both drugs produced a similar diuretic and natriuretic effect. However, torasemide showed an increased duration of action compared to furosemide and a higher relation between urinary Na and K excretion, both after i.v. and oral administration, suggesting less loss of potassium after To. Both agents were well tolerated.
在6名健康志愿者中，比较了口服和静脉注射20毫克托拉塞米（1-异丙基-3-([4-(3-甲基苯氨基)吡啶]-3-磺酰基)脲）和40毫克呋塞米后的药效学效应和药代动力学参数。静脉注射和口服托拉塞米的血浆消除半衰期分别为2.2小时和2.8小时，口服给药后的生物利用度为91%，静脉注射或口服后约25%的全身清除率是由于肾排泄。对于呋塞米，静脉注射的血浆消除半衰期为0.6小时，口服为0.8小时。生物利用度为40%，约62%的药物经肾脏排泄。两种药物都产生了相似的利尿和排钠作用。然而，与呋塞米相比，托拉塞米的作用持续时间延长，静脉注射和口服后尿钠与钾排泄之间的关系更高，这表明托拉塞米后钾的丢失较少。两种药物耐受性良好。
