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托拉塞米:一种吡啶磺酰脲类袢利尿剂。

Torsemide: a pyridine-sulfonylurea loop diuretic.

作者信息

Blose J S, Adams K F, Patterson J H

机构信息

University of North Carolina at Chapel Hill 27599, USA.

出版信息

Ann Pharmacother. 1995 Apr;29(4):396-402. doi: 10.1177/106002809502900411.

Abstract

OBJECTIVE

To review the clinical pharmacology of torsemide and to compare it with currently available loop diuretics, particularly furosemide.

DATA SOURCES

An English-language MEDLINE search, 1985 to October 1994, was used to identify pertinent literature, including review articles.

DATA EXTRACTION

Data from scientific literature were extracted, evaluated, and summarized for presentation. Pivotal and representative studies are discussed relating to the pharmacology, pharmacokinetics, and use of torsemide in patients with congestive heart failure, renal disease, hepatic disease, and hypertension.

DATA SYNTHESIS

Torsemide is a loop diuretic of the pyridine-sulfonylurea class. The bioavailability of torsemide is approximately 80%, with little first-pass metabolism, and torsemide can be given without regard to meals. The serum concentration reaches its peak within 1 hour after oral administration and diuresis lasts approximately 6-8 hours. Torsemide is eliminated both hepatically (80%) and renally (20%) as unchanged drug with an elimination half-life of about 3.5 hours. Because of the high bioavailability, oral and intravenous doses are therapeutically equivalent. Torsemide, and other loop diuretics such as furosemide, are indicated for the treatment of edema associated with congestive heart failure, renal disease, and hepatic disease. They also are indicated for the treatment of hypertension alone or in combination with other antihypertensive agents. Depending on the indication, the recommended initial adult dosage of torsemide is between 5 and 20 mg once daily orally or intravenously. Special dosage adjustments in the elderly are not necessary.

CONCLUSIONS

Torsemide is a loop diuretic similar to furosemide, with similar indications. Torsemide is characterized by good bioavailability and once-daily dosing and, compared with furosemide, provides generally equivalent therapeutic efficacy.

摘要

目的

回顾托拉塞米的临床药理学,并将其与现有的袢利尿剂,特别是呋塞米进行比较。

资料来源

利用1985年至1994年10月的英文医学文献数据库检索相关文献,包括综述文章。

资料提取

提取、评估并总结科学文献中的数据以进行呈现。讨论了有关托拉塞米在充血性心力衰竭、肾脏疾病、肝脏疾病和高血压患者中的药理学、药代动力学及应用的关键和代表性研究。

资料综合

托拉塞米是一种吡啶磺酰脲类袢利尿剂。托拉塞米的生物利用度约为80%,首过代谢少,给药时无需考虑进食时间。口服给药后1小时内血清浓度达到峰值,利尿作用持续约6 - 8小时。托拉塞米以原形药物经肝脏(80%)和肾脏(20%)消除,消除半衰期约为3.5小时。由于生物利用度高,口服和静脉给药的治疗效果相当。托拉塞米以及其他袢利尿剂如呋塞米,适用于治疗与充血性心力衰竭、肾脏疾病和肝脏疾病相关的水肿。它们也适用于单独或与其他抗高血压药物联合治疗高血压。根据适应证,推荐的托拉塞米初始成人剂量为每日口服或静脉注射5至20毫克。老年人无需特殊剂量调整。

结论

托拉塞米是一种与呋塞米类似的袢利尿剂,适应证相似。托拉塞米的特点是生物利用度好且每日给药一次,与呋塞米相比,具有大致相当的治疗效果。

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