Fillastre J P
Service de néphrologie, CHU Rouen, Bois-Guillaume, France.
Arch Mal Coeur Vaiss. 1989 Dec;82 Spec No 5:19-23.
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)
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)