Fowler S F, Murray K M
Department of Pharmacy Practice and Administration, College of Pharmacy, University of South Carolina, Columbia 29208, USA.
Am J Health Syst Pharm. 1995 Aug 15;52(16):1771-80; quiz 1814-5. doi: 10.1093/ajhp/52.16.1771.
The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of torsemide are reviewed. Torsemide belongs to the pyridine-sulfonylurea class of loop diuretics. Its primary site of activity is the thick ascending limb of the loop of Henle, where it blocks active reabsorption of sodium and chloride, resulting in diuresis, natriuresis, and other effects. Torsemide has high bioavailability, a relatively long half-life, and a prolonged duration of activity. It is highly protein bound. Clinical trials indicate that torsemide is effective in the treatment of hypertension and of edema and other symptoms in patients with chronic renal failure (CRF), hepatic dysfunction, or congestive heart failure (CHF). Torsemide has infrequent, mild, and transient adverse effects; among the most common are orthostatic hypotension, fatigue, dizziness, and nervousness. The recommended initial oral dosages of torsemide are 10-20 mg/day for CHF, 20 mg/day for CRF, 5 mg/day for hypertension, and 5-10 mg/day (in combination with a potassium-sparing diuretic or aldosterone antagonist) for hepatic cirrhosis. In most patients, the pharmacokinetic advantages of torsemide over other loop diuretics are unlikely to translate into a substantial edge in clinical outcomes, and in practice there may be no cost advantages. Although torsemide does not offer major advantages over other loop diuretics, it may be of benefit in patients who do not respond to or cannot tolerate other agents.
本文综述了托拉塞米的药理学、药代动力学、临床疗效、不良反应以及用法用量。托拉塞米属于吡啶磺酰脲类髓袢利尿剂。其主要作用部位是髓袢升支粗段,在该部位它可阻断钠和氯的主动重吸收,从而产生利尿、排钠及其他效应。托拉塞米具有高生物利用度、相对较长的半衰期和较长的作用持续时间。它与蛋白质高度结合。临床试验表明,托拉塞米在治疗高血压以及慢性肾衰竭(CRF)、肝功能不全或充血性心力衰竭(CHF)患者的水肿及其他症状方面有效。托拉塞米的不良反应较少、程度较轻且为一过性;最常见的不良反应包括体位性低血压、疲劳、头晕和紧张。托拉塞米推荐的初始口服剂量为:用于CHF时为10 - 20mg/天,用于CRF时为20mg/天,用于高血压时为5mg/天,用于肝硬化时为5 - 10mg/天(与保钾利尿剂或醛固酮拮抗剂联合使用)。在大多数患者中,托拉塞米相较于其他髓袢利尿剂的药代动力学优势不太可能转化为临床结局上的显著优势,并且在实际应用中可能不存在成本优势。尽管托拉塞米相对于其他髓袢利尿剂没有明显优势,但对于对其他药物无反应或不能耐受的患者可能有益。