Bailey R R
Br J Clin Pharmacol. 1979;8(Suppl 2):135S-140S.
Labetalol has been used to treat patients with renal hypertension or hypertension in the presence of renal functional impairment. In some patients changes in the glomerular filtration rate (GFR) were followed during the treatment. Sixty patients were treated with labetalol for up to 24 months. Forty-nine of the patients were taking a diuretic and 23 were receiving additional antihypertensive therapy. The antihypertensive effect of labetalol has so far been assessed in 51 patients. Forty-six of these 51 patients have responded with a fall in the mean supine BP from 184/115 to 148/93 mmHg and the mean erect BP from 176/112 to 138/89 mmHg. The mean daily maintenance dose of labetalol for the responders was 418 mg (range 100-1200 mg). The majority of patients were controlled by less than 600 mg daily. Side-effects occurred in 38% of patients, the most serious of which was left ventricular failure in four patients with severe cardiac and renal disease. Other side-effects included transient postural hypotension, scalp tingling and problems with micturition. Fluid retention was frequent but was easily controlled with diuretics. In only three of 31 patients was there a fall in the GFR which could possibly be attributable to the treatment. These changes were small and not clinically significant. An improvement or stabilization of the GFR was noted frequently. Labetalol by intravenous infusion proved disappointing and quite unpredictable in its action. A large single oral dose was effective in hypertensive emergencies. Labetalol, preferably in combination with a diuretic, was a safe and effective drug for patients with hypertension and renal functional impairment.
拉贝洛尔已被用于治疗肾性高血压患者或存在肾功能损害时的高血压患者。在一些患者的治疗过程中,对肾小球滤过率(GFR)的变化进行了跟踪。60例患者接受拉贝洛尔治疗长达24个月。其中49例患者正在服用利尿剂,23例患者正在接受额外的抗高血压治疗。到目前为止,已对51例患者评估了拉贝洛尔的抗高血压作用。这51例患者中有46例有反应,平均仰卧位血压从184/115 mmHg降至148/93 mmHg,平均直立位血压从176/112 mmHg降至138/89 mmHg。有反应患者的拉贝洛尔平均每日维持剂量为418 mg(范围为100 - 1200 mg)。大多数患者通过每日剂量低于600 mg得到控制。38%的患者出现副作用,其中最严重的是4例患有严重心脏和肾脏疾病的患者发生左心室衰竭。其他副作用包括短暂性体位性低血压、头皮刺痛和排尿问题。液体潴留很常见,但用利尿剂很容易控制。在31例患者中,只有3例的GFR下降可能归因于治疗。这些变化很小,无临床意义。经常注意到GFR有所改善或稳定。静脉输注拉贝洛尔的效果令人失望,其作用相当不可预测。大剂量单次口服对高血压急症有效。拉贝洛尔,最好与利尿剂联合使用,对高血压和肾功能损害患者是一种安全有效的药物。