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托拉塞米耳毒性的定量评估。

Quantitative assessment of torasemide ototoxicity.

作者信息

Klinke R, Mertens M

机构信息

Zentrum der Physiologie, Klinikum der Johann Wolfgang Goethe-Universität, Frankfurt/Main, Fed. Rep. of Germany.

出版信息

Arzneimittelforschung. 1988 Jan;38(1A):153-5.

PMID:3370060
Abstract

Torasemide (1-isopropyl-3- ([4-(3-methyl-phenylamino)pyridine]-3-sulfonyl)urea), a new loop diuretic, was quantitatively tested for ototoxicity in cats. The toxic dose that causes a defined hearing loss in 50% of the animals (TD50) was determined. TD50 was calculated as 20.8 mg/kg. This is slightly but not significantly above the value for furosemide (18.37 mg/kg). Hearing function tended to recover after the acute effect. The main metabolite in man (1-isopropyl-3-([(3-carboxy-anilino)-3-pyridyl]sulfonyl)urea, M5) showed no ototoxic action even in excessive doses. To ensure complete recovery, hearing function was tested in animals pretreated with torasemide in doses higher than TD50. There was no indication for permanent hearing impairment in these pretreated animals.

摘要

托拉塞米(1-异丙基-3-([4-(3-甲基苯氨基)吡啶]-3-磺酰基)脲)是一种新型袢利尿剂,对猫进行了耳毒性定量测试。测定了导致50%的动物出现明确听力损失的毒性剂量(TD50)。TD50计算为20.8mg/kg。这略高于呋塞米的值(18.37mg/kg),但无显著差异。急性作用后听力功能有恢复趋势。人体中的主要代谢产物(1-异丙基-3-([(3-羧基苯胺基)-3-吡啶基]磺酰基)脲,M5)即使大剂量使用也无耳毒性作用。为确保完全恢复,对用高于TD50剂量的托拉塞米预处理的动物进行了听力功能测试。这些预处理动物未出现永久性听力损害迹象。

相似文献

1
Quantitative assessment of torasemide ototoxicity.托拉塞米耳毒性的定量评估。
Arzneimittelforschung. 1988 Jan;38(1A):153-5.
2
Quantitative evaluation of ototoxic side effects of furosemide, piretanide, bumetanide, azosemide and ozolinone in the cat--a new approach to the problem of ototoxicity.
Naunyn Schmiedebergs Arch Pharmacol. 1985 Nov;331(2-3):275-82. doi: 10.1007/BF00634249.
3
Comparative pharmacodynamics of torasemide and furosemide in patients with oedema.托拉塞米与呋塞米对水肿患者的药效学比较
Arzneimittelforschung. 1988 Jan;38(1A):180-3.
4
Pharmacokinetics and metabolism of torasemide in man.托拉塞米在人体中的药代动力学与代谢
Arzneimittelforschung. 1988 Jan;38(1A):164-6.
5
Chemistry and pharmacological properties of the pyridine-3-sulfonylurea derivative torasemide.吡啶-3-磺酰脲衍生物托拉塞米的化学与药理特性
Arzneimittelforschung. 1988 Jan;38(1A):144-50.
6
Comparison of efficacy and tolerance of different oral doses of torasemide and furosemide in patients with advanced chronic renal failure.不同口服剂量托拉塞米和呋塞米对晚期慢性肾衰竭患者疗效及耐受性的比较
Arzneimittelforschung. 1988 Jan;38(1A):212-4.
7
Comparison of diuretic effects and pharmacokinetics of torasemide and furosemide after a single oral dose in patients with hydropically decompensated cirrhosis of the liver.托拉塞米与呋塞米单次口服给药后对肝性腹水失代偿期患者利尿效果及药代动力学的比较
Arzneimittelforschung. 1988 Jan;38(1A):176-9.
8
Single dose comparison of torasemide and furosemide in patients with advanced renal failure.
Arzneimittelforschung. 1988 Jan;38(1A):200-4.
9
Ototoxicity of loop diuretics.袢利尿剂的耳毒性。
Otolaryngol Clin North Am. 1993 Oct;26(5):829-44.
10
Testing strategy for ototoxic side effects.耳毒性副作用的测试策略。
Scand Audiol Suppl. 1981;14 Suppl:95-109.

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Drugs. 1995 Jan;49(1):121-42. doi: 10.2165/00003495-199549010-00009.
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Torasemide. A review of its pharmacological properties and therapeutic potential.托拉塞米:其药理特性与治疗潜力综述
Drugs. 1991 Jan;41(1):81-103. doi: 10.2165/00003495-199141010-00008.