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静脉注射双醋洛尔。拉贝洛尔的R-R光学异构体对重度高血压患者的影响。

Intravenous dilevalol. Effects of the R-R optical isomer of labetalol in patients with severe hypertension.

作者信息

Wallin J D, Cook M E, Clifton G G, Blasucci D J, Poland M

机构信息

Department of Medicine, Tulane University School of Medicine, New Orleans, LA 70112.

出版信息

Arch Intern Med. 1988 Mar;148(3):534-8. doi: 10.1001/archinte.148.3.534.

DOI:10.1001/archinte.148.3.534
PMID:3277568
Abstract

Dilevalol hydrochloride, the R-R optical isomer of labetalol hydrochloride, was administered intravenously to subjects with severe hypertension. Twelve subjects with supine diastolic blood pressure of more than 115 mm Hg (mean, 124 +/- 2 mm Hg) were studied. Initial doses of 25 mg of dilevalol administered as a slowly given bolus reduced blood pressure by 14/16 mm Hg. With subsequent additional boluses to a total dose of up to 600 mg, supine diastolic blood pressure was reduced to less than 95 mm Hg in ten of 12 subjects studied (mean reduction, 28 mm Hg). Side effects were minimal and upright blood pressure at the time of reduction of blood pressure to goal was not significantly different from supine blood pressure. Plasma renin activity decreased in 11 of 11 subjects studied. Plasma epinephrine concentrations did not change significantly, whereas plasma norepinephrine concentrations increased 2 1/2-fold, probably reflecting the effect of beta 2-agonism on norepinephrine release. Dilevalol appears to be a safe and effective way of lowering blood pressure short term when intravenous antihypertensive therapy is indicated.

摘要

盐酸地来洛尔是盐酸拉贝洛尔的R-R光学异构体,将其静脉注射给重度高血压患者。研究了12名仰卧位舒张压超过115 mmHg(平均为124±2 mmHg)的受试者。初始剂量为25 mg盐酸地来洛尔,以缓慢推注方式给药,可使血压降低14/16 mmHg。随后追加推注,总剂量达600 mg时,在研究的12名受试者中,有10名仰卧位舒张压降至95 mmHg以下(平均降低28 mmHg)。副作用极小,血压降至目标值时的直立位血压与仰卧位血压无显著差异。在研究的11名受试者中,有11名血浆肾素活性降低。血浆肾上腺素浓度无显著变化,而血浆去甲肾上腺素浓度增加了2.5倍,这可能反映了β2激动剂对去甲肾上腺素释放的影响。当需要静脉降压治疗时,盐酸地来洛尔似乎是一种短期安全有效的降压方法。

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引用本文的文献

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Comparison of the effects of dilevalol and propranolol on systemic and regional haemodynamics in healthy volunteers at rest and during exercise.双醋洛尔与普萘洛尔对健康志愿者静息及运动时全身和局部血流动力学影响的比较。
Eur J Clin Pharmacol. 1994;47(1):39-47. doi: 10.1007/BF00193476.
2
The effects of a single dose of dilevalol on [3H]-noradrenaline plasma kinetics and plasma lipoprotein cholesterol concentrations.单次剂量双醋洛尔对[3H]-去甲肾上腺素血浆动力学及血浆脂蛋白胆固醇浓度的影响。
Br J Clin Pharmacol. 1990 Mar;29(3):281-7. doi: 10.1111/j.1365-2125.1990.tb03637.x.
3
Comparative effects of dilevalol and atenolol on lung function and airway response to methacholine in hypertensive subjects.
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Br J Clin Pharmacol. 1990 Jun;29(6):725-31. doi: 10.1111/j.1365-2125.1990.tb03694.x.
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