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新型选择性β1肾上腺素能受体部分激动剂扎莫特罗治疗体位性低血压

Xamoterol, a new selective beta-1-adrenoceptor partial agonist, in the treatment of postural hypotension.

作者信息

Mehlsen J, Trap-Jensen J

出版信息

Acta Med Scand. 1986;219(2):173-7. doi: 10.1111/j.0954-6820.1986.tb03295.x.

DOI:10.1111/j.0954-6820.1986.tb03295.x
PMID:2870611
Abstract

Three patients severely disabled from postural hypotension were treated with xamoterol, a selective beta-1-adrenoceptor antagonist with a high degree of partial agonist activity. Oral treatment (200 mg b.i.d.) was chosen on the basis of the effects of acute intravenous administration of xamoterol and pindolol, a non-selective beta-adrenoceptor antagonist with partial agonist activity. In these patients pindolol had a predominantly antagonist effect, whereas xamoterol had a predominantly agonist effect after intravenous administration. Oral treatment was carried out with placebo control in a single-blind fashion. The patients reported gradual improvement during the first days of treatment. After 1 month of oral treatment, heart rate had increased by 15 beats/min, systolic blood pressure from 131 to 170 mmHg, diastolic blood pressure from 77 to 91 mmHg and mean blood pressure by 22 mmHg (mean values, supine). During the placebo period (2 weeks) heart rate decreased to pretreatment levels and mean blood pressure was reduced by only 14 mmHg. The patients reported substantial improvement in their condition during active medication. Xamoterol seems to be a useful alternative in the treatment of postural hypotension.

摘要

三名因体位性低血压而严重致残的患者接受了沙美特罗治疗,沙美特罗是一种具有高度部分激动剂活性的选择性β1肾上腺素能受体拮抗剂。基于沙美特罗和吲哚洛尔(一种具有部分激动剂活性的非选择性β肾上腺素能受体拮抗剂)急性静脉给药的效果,选择了口服治疗(200毫克,每日两次)。在这些患者中,吲哚洛尔静脉给药后主要表现为拮抗作用,而沙美特罗静脉给药后主要表现为激动作用。口服治疗采用单盲方式并设安慰剂对照。患者报告在治疗的最初几天病情逐渐改善。口服治疗1个月后,心率增加了15次/分钟,收缩压从131毫米汞柱升至170毫米汞柱,舒张压从77毫米汞柱升至91毫米汞柱,平均血压升高了22毫米汞柱(仰卧位平均值)。在安慰剂期(2周),心率降至治疗前水平,平均血压仅降低了14毫米汞柱。患者报告在积极用药期间病情有显著改善。沙美特罗似乎是治疗体位性低血压的一种有用的替代药物。

相似文献

1
Xamoterol, a new selective beta-1-adrenoceptor partial agonist, in the treatment of postural hypotension.新型选择性β1肾上腺素能受体部分激动剂扎莫特罗治疗体位性低血压
Acta Med Scand. 1986;219(2):173-7. doi: 10.1111/j.0954-6820.1986.tb03295.x.
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Xamoterol in the treatment of orthostatic hypotension associated with multiple system atrophy (Shy-Drager syndrome).扎莫特罗治疗多系统萎缩(夏伊-德雷格综合征)相关的体位性低血压
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Selective beta-adrenoceptor partial agonist effects of pindolol and xamoterol on skeletal muscle assessed by plasma creatine kinase changes in healthy subjects.通过健康受试者血浆肌酸激酶变化评估吲哚洛尔和扎莫特罗对骨骼肌的选择性β-肾上腺素能受体部分激动作用。
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Effects of xamoterol a new beta-adrenoceptor partial agonist, in patients with angina pectoris.新型β-肾上腺素能受体部分激动剂扎莫特罗对心绞痛患者的影响。
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Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol.环丙洛尔、扎莫特罗和吲哚洛尔对β-1肾上腺素能受体激动剂及拮抗剂效能和选择性的比较分析
J Pharmacol Exp Ther. 1987 Sep;242(3):1025-34.

引用本文的文献

1
Current pharmacologic treatment for orthostatic hypotension.
Clin Auton Res. 2008 Mar;18 Suppl 1:14-8. doi: 10.1007/s10286-007-1003-1. Epub 2008 Mar 27.
2
Differential effects of beta-adrenoceptor partial agonists in patients with postural hypotension.
Eur J Clin Pharmacol. 1993;44(1):7-11. doi: 10.1007/BF00315272.
3
Treating postural hypotension.治疗体位性低血压。
Br Med J (Clin Res Ed). 1987 Feb 14;294(6569):390-1. doi: 10.1136/bmj.294.6569.390.
4
Xamoterol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use.
Xamoterol。对其药效学、药代动力学特性及治疗用途的初步综述。
Drugs. 1988 Oct;36(4):455-74. doi: 10.2165/00003495-198836040-00004.
5
Myocardial, coronary, and peripheral effects of xamoterol (ICI 118,587) in open-chest pigs.Xamoterol(ICI 118,587)对开胸猪的心肌、冠状动脉及外周的影响
Cardiovasc Drugs Ther. 1989 Mar;3(1):91-7. doi: 10.1007/BF01881533.
6
Treatment of postural hypotension. A review.
Drugs. 1990 Jan;39(1):74-85. doi: 10.2165/00003495-199039010-00007.
7
A double-blind crossover study of oral xamoterol in postural hypotension due to diabetic autonomic neuropathy.
Clin Auton Res. 1991 Jun;1(2):119-23. doi: 10.1007/BF01826207.