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利美尼定对中枢神经系统和肾脏的作用

[Effects of rilmenidine on the central nervous system and kidney].

作者信息

Fillastre J P

机构信息

Service de néphrologie, CHU Rouen, Bois-Guillaume, France.

出版信息

Arch Mal Coeur Vaiss. 1989 Dec;82 Spec No 5:19-23.

PMID:2517005
Abstract

Rilmenidine is an oxazoline with antihypertensive properties characterised by a dissociation of its antihypertensive and central side effects and the absence of tolerance. After a single dose, the antihypertensive activity is directly related to the dose of rilmenidine. Secondary sedative effects and dryness of the mouth are no different to those observed with placebo at doses of 0.5 and 1.0 mg. In two randomised trials versus placebo (N = 126) and versus clonidine (N = 333) in hypertensive patients after a 1 month washout period under placebo, the antihypertensive effect of rilmenidine was superior to placebo and comparable to that of clonidine (0.150 mg once or twice daily). After 4 and 6 weeks' treatment with rilmenidine (1 mg once or twice daily) the average decrease in supine systolic-diastolic BP was 21-15 mmHg and the average percentage of normalised values (diastolic BP less than or equal to 90 mmHg) was 60 per cent. The incidence of somnolence was comparable to that observed with placebo and 2 to 3 times less than that with equihypotensive doses of clonidine. No patients withdrew from the trial because of side effects. The sustained antihypertensive effect in an open trial of 269 patients treated for one year and 134 patients for two years, showed that there was no tolerance with rilmenidine. This result is probably related to the absence of salt and water retention and the conservation of renal function observed in single dose regime in healthy subjects and in chronic administration in hypertensives. No significant changes were observed in renal blood flow, glomerular filtration, filtration fraction, serum or urinary electrolyte concentrations.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

利美尼定是一种具有抗高血压特性的恶唑啉,其特点是抗高血压作用与中枢副作用分离且无耐受性。单次给药后,抗高血压活性与利美尼定剂量直接相关。在0.5毫克和1.0毫克剂量时,继发性镇静作用和口干与安慰剂组观察到的情况无差异。在两项针对高血压患者的随机试验中,经过1个月安慰剂洗脱期后,与安慰剂(N = 126)及可乐定(N = 333)对比,利美尼定的抗高血压效果优于安慰剂,与可乐定(每日0.150毫克,一次或两次)相当。用利美尼定(每日1毫克,一次或两次)治疗4周和6周后,仰卧位收缩压 - 舒张压平均下降21 - 15毫米汞柱,血压正常化值(舒张压小于或等于90毫米汞柱)的平均百分比为60%。嗜睡发生率与安慰剂组相当,比等降压剂量可乐定低2至3倍。没有患者因副作用退出试验。在一项对269例患者进行一年治疗和134例患者进行两年治疗的开放试验中,利美尼定持续的抗高血压作用表明其无耐受性。该结果可能与健康受试者单剂量给药及高血压患者长期给药时未观察到盐和水潴留以及肾功能保存有关。肾血流量、肾小球滤过、滤过分数、血清或尿电解质浓度均未观察到显著变化。(摘要截短于250字)

相似文献

1
[Effects of rilmenidine on the central nervous system and kidney].利美尼定对中枢神经系统和肾脏的作用
Arch Mal Coeur Vaiss. 1989 Dec;82 Spec No 5:19-23.
2
[Efficacy and acceptability of rilmenidine in mild to moderate arterial hypertension. A multicenter, randomized, double-blind trial, in comparison with methyldopa in 157 patients].利美尼定治疗轻至中度动脉高血压的疗效和可接受性。一项多中心、随机、双盲试验,与甲基多巴对比,共157例患者
Arch Mal Coeur Vaiss. 1989 Dec;82 Spec No 5:31-8.
3
Acceptability of rilmenidine and long-term surveillance of plasma concentrations in hypertensive patients with renal insufficiency.肾素抑制剂利美尼定在肾功能不全高血压患者中的可接受性及血药浓度长期监测
Am J Med. 1989 Sep 18;87(3C):41S-45S. doi: 10.1016/0002-9343(89)90505-6.
4
[Multicenter, double-blind study comparing rilmenidine 1 mg and hydrochlorothiazide 25 mg in 244 patients].[多中心、双盲研究:244例患者中瑞米吉仑1毫克与氢氯噻嗪25毫克的比较]
Arch Mal Coeur Vaiss. 1989 Dec;82 Spec No 5:39-46.
5
[Effects of rilmenidine (hyperium) on lipid balance in hyperlipidemic hypertensive patients. Randomized, controlled, double-blind 8-week study vs. captopril in parallel groups].[利美尼定(Hyperium)对高脂血症高血压患者脂质平衡的影响。与卡托普利平行组进行的随机、对照、双盲8周研究]
Ann Cardiol Angeiol (Paris). 1996 Dec;45(10):595-601.
6
[Rilmenidine, a new antihypertensive agent in the first line treatment of essential arterial hypertension. Multicenter double-blind study versus atenolol].[利美尼定,一种用于原发性高血压一线治疗的新型抗高血压药物。与阿替洛尔的多中心双盲研究]
Presse Med. 1991;20(27):1265-71.
7
A multicenter double-blind comparative study of rilmenidine and clonidine in 333 hypertensive patients.一项针对333名高血压患者进行的瑞米吉仑与可乐定的多中心双盲对照研究。
Am J Cardiol. 1988 Feb 24;61(7):81D-85D. doi: 10.1016/0002-9149(88)90471-7.
8
Rilmenidine and vigilance. Review of clinical studies.利美尼定与警觉性。临床研究综述。
Am J Med. 1989 Sep 18;87(3C):67S-72S. doi: 10.1016/0002-9343(89)90509-3.
9
[Pharmaco-epidemiologic evaluation of rilmenidine in 18,235 hypertensive patients].[对18235例高血压患者进行的利美尼定药物流行病学评估]
Presse Med. 1995 Dec 9;24(38):1857-64.
10
Dose-effect relationship of rilmenidine after chronic administration.瑞米吉仑长期给药后的剂量-效应关系。
Eur J Clin Pharmacol. 1993;45(2):157-60. doi: 10.1007/BF00315498.