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托拉塞米。其药理特性与治疗效果的最新进展。

Torasemide. An update of its pharmacological properties and therapeutic efficacy.

作者信息

Dunn C J, Fitton A, Brogden R N

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1995 Jan;49(1):121-42. doi: 10.2165/00003495-199549010-00009.

Abstract

The pharmacological properties and therapeutic use of the high-ceiling loop diuretic torasemide (torsemide) were previously reviewed in Drugs in 1991, the following being a re-examination of the role of the drug in the light of data that have subsequently become available (particularly in the management of oedematous disorders). Torasemide produces a more prolonged water and electrolyte excretion than equipotent diuretic doses of furosemide (frusemide), but does not increase kaliuresis to the same extent. Dosages of torasemide of 2.5 to 5 mg/day do not affect plasma renin activity or aldosterone release to a clinically significant extent, although torasemide 20mg increases plasma renin levels, angiotensin II activity and urinary dopamine and prostaglandin E excretion. Studies published since the previous review have confirmed the efficacy of low dosages of torasemide (2.5 to 5 mg/day) in the treatment of hypertension, and have shown it to be effective when administered orally at a dosage of 5 to 20 mg/day in the management of congestive heart failure. Dosages of up to 400 mg/day increased urinary volume excretion and natriuresis in patients with chronic renal failure. Bodyweight and peripheral oedema were reduced by torasemide 10 to 200 mg/day as monotherapy, and 5 to 20 mg/day when coadministered with spironolactone, in patients with nephrotic syndrome. Dosages of 10 to 40 mg/day, either as monotherapy or in conjunction with an aldosterone antagonist, reduced ascites, oedema and bodyweight in patients with hydropically decompensated liver failure. Adverse effects due to torasemide are usually mild and transient in nature. No evidence of ototoxicity has been demonstrated in humans, and torasemide does not appear to affect blood glucose levels, serum uric acid concentrations, or serum potassium levels at dosages below 5 mg/day. Thus, additional evidence has accumulated for the clinical efficacy of torasemide in the management of mild to moderate essential hypertension and oedematous conditions which require diuretic therapy. Further studies are now required to confirm the long term efficacy and tolerability of torasemide, and to investigate the place of the drug in therapy relative to cardiovascular agents other than furosemide and the thiazide diuretics.

摘要

高效能袢利尿剂托拉塞米的药理特性及治疗用途曾在1991年的《药物》杂志上进行过综述,以下是根据后续可得数据(特别是在水肿性疾病的管理方面)对该药物作用的重新审视。与等效剂量的呋塞米相比,托拉塞米产生的水和电解质排泄作用持续时间更长,但在同等程度上不会增加尿钾排泄。托拉塞米2.5至5毫克/天的剂量在临床上对血浆肾素活性或醛固酮释放无显著影响,尽管20毫克托拉塞米会增加血浆肾素水平、血管紧张素II活性以及尿多巴胺和前列腺素E的排泄。自上次综述以来发表的研究证实了低剂量托拉塞米(2.5至5毫克/天)治疗高血压的疗效,并表明其以5至20毫克/天的口服剂量用于治疗充血性心力衰竭时有效。高达400毫克/天的剂量可增加慢性肾衰竭患者的尿量排泄和尿钠排泄。在肾病综合征患者中,托拉塞米10至200毫克/天作为单一疗法,与螺内酯合用时5至20毫克/天,可减轻体重和外周水肿。10至40毫克/天的剂量,无论是单一疗法还是与醛固酮拮抗剂联合使用,均可减轻肝性腹水失代偿患者的腹水、水肿和体重。托拉塞米引起的不良反应通常性质轻微且短暂。在人类中未证实有耳毒性证据,且在剂量低于5毫克/天时,托拉塞米似乎不影响血糖水平、血清尿酸浓度或血清钾水平。因此,已有更多证据表明托拉塞米在治疗轻度至中度原发性高血压及需要利尿剂治疗的水肿性疾病方面具有临床疗效。现在需要进一步研究以证实托拉塞米的长期疗效和耐受性,并研究该药物相对于呋塞米和噻嗪类利尿剂以外的心血管药物在治疗中的地位。

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