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新型β2肾上腺素能激动剂气雾剂。

New beta 2-adrenergic agonist aerosols.

作者信息

Kelly H W

出版信息

Clin Pharm. 1985 Jul-Aug;4(4):393-403.

PMID:2864159
Abstract

The beta 2-adrenergic agonists are reviewed in terms of their dose-response characteristics, and two newer agents, fenoterol hydrobromide and bitolterol mesylate aerosols, are reviewed in relation to older agents. The fenoterol aerosol contains a more potent beta 2-adrenergic agonist dose per puff than the other aerosols but, when given in equipotent doses, offers no advantage over available agents. Bitolterol mesylate is a prodrug that is hydrolyzed to the active beta 2-adrenergic agonist colterol by lung esterases. Bitolterol demonstrates an improved bronchoselectivity in animals, but there are insufficient comparative data in humans. Tachycardia is the dose-limiting toxicity for all beta 2-adrenergic agonists. Currently available data do not suggest an important improvement in duration of action for the newer agents over terbutaline or albuterol. Aerosol administration improves bronchoselectivity of all the agents. Optimal use of beta 2-adrenergic agonist aerosols requires understanding of the variable dose-response characteristics. The type of delivery system and patient technique are important variables in determining the dose delivered. Tube-spacer devices attached to aerosol canisters can significantly improve delivery of the beta 2-adrenergic agonists to the lungs in patients unable to synchronize actuation and inspiration. They provide minimal to no improvement in patients who can perform the appropriate technique. Aerosol administration is the route of choice for beta 2-adrenergic agonists for prophylaxis of exercise-induced bronchospasm; albuterol and terbutaline provide a prolonged duration of action with excellent beta 2-adrenergic selectivity. Patients should be carefully instructed in the optimal use of metered-dose inhalers, and some patients may benefit from use of tube-spacers.

摘要

对β2-肾上腺素能激动剂的剂量反应特性进行了综述,并将两种新型药物,即氢溴酸非诺特罗和气雾剂型甲磺酸比托特罗与旧型药物进行了比较。每喷一次,非诺特罗气雾剂所含的β2-肾上腺素能激动剂剂量比其他气雾剂更有效,但在给予等效剂量时,与现有药物相比并无优势。甲磺酸比托特罗是一种前体药物,可被肺酯酶水解为活性β2-肾上腺素能激动剂可托特罗。比托特罗在动物实验中显示出更好的支气管选择性,但在人体中的比较数据不足。心动过速是所有β2-肾上腺素能激动剂的剂量限制性毒性。目前可得的数据并未表明新型药物在作用持续时间上比特布他林或沙丁胺醇有重要改善。气雾剂给药可提高所有药物的支气管选择性。β2-肾上腺素能激动剂气雾剂的最佳使用需要了解其可变的剂量反应特性。给药系统的类型和患者的使用技巧是决定给药剂量的重要变量。对于无法同步启动和吸气的患者,连接到气雾剂罐上的储雾罐装置可显著提高β2-肾上腺素能激动剂向肺部的递送。对于能够正确操作的患者,它们的改善作用很小或没有改善。气雾剂给药是β2-肾上腺素能激动剂预防运动诱发性支气管痉挛的首选途径;沙丁胺醇和特布他林作用持续时间长,具有出色的β2-肾上腺素能选择性。应仔细指导患者如何最佳使用定量吸入器,一些患者可能会受益于储雾罐的使用。

相似文献

1
New beta 2-adrenergic agonist aerosols.新型β2肾上腺素能激动剂气雾剂。
Clin Pharm. 1985 Jul-Aug;4(4):393-403.
2
Adrenergic agonists and bronchodilator aerosol therapy in asthma.肾上腺素能激动剂与支气管扩张剂雾化疗法治疗哮喘
Clin Chest Med. 1984 Dec;5(4):659-68.
3
Tolerability of a salmeterol xinafoate/fluticasone propionate hydrofluoroalkane metered-dose inhaler in adolescent and adult patients with persistent asthma: a 52-week, open-label, stratified, parallel-group, multicenter study.丙酸氟替卡松/昔萘酸沙美特罗氢氟烷计量吸入器在青少年和成年持续性哮喘患者中的耐受性:一项为期52周的开放标签、分层、平行组、多中心研究。
Clin Ther. 2007 Jul;29(7):1390-402. doi: 10.1016/j.clinthera.2007.07.021.
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How should a pressurized beta-adrenergic bronchodilator be inhaled?加压β-肾上腺素能支气管扩张剂应如何吸入?
Eur J Respir Dis. 1981 Feb;62(1):3-21.
5
Procaterol metered aerosol in patients with chronic obstructive pulmonary disease.
Int J Clin Pharmacol Res. 1987;7(5):363-8.
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[Evaluation of procaterol aerosol as an aerosolized beta 2-adrenergic bronchodilator in conscious guinea pigs].[在清醒豚鼠中对丙卡特罗气雾剂作为雾化β2肾上腺素能支气管扩张剂的评估]
Arerugi. 1985 Nov;34(11):999-1005.
7
[Metabolism of beta-adrenergic substances. Therapeutic implications].[β-肾上腺素能物质的代谢。治疗意义]
Bull Eur Physiopathol Respir. 1985 Sep-Oct;21(5):19s-34s.
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A survey of albuterol administration practices in intubated patients in the neonatal intensive care unit.新生儿重症监护病房中插管患者沙丁胺醇给药实践的调查。
Respir Care. 2002 Jan;47(1):31-8.
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Fenoterol: a beta2-adrenergic agonist for use in asthma. Pharmacology, pharmacokinetics, clinical efficacy and adverse effects.非诺特罗:一种用于治疗哮喘的β2肾上腺素能激动剂。药理学、药代动力学、临床疗效及不良反应
Pharmacotherapy. 1985 May-Jun;5(3):109-26. doi: 10.1002/j.1875-9114.1985.tb03409.x.
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Comparison of bronchodilator responses of levosalbutamol and salbutamol given via a pressurized metered dose inhaler: a randomized, double blind, single-dose, crossover study.通过压力定量吸入器给予左沙丁胺醇和沙丁胺醇的支气管扩张剂反应比较:一项随机、双盲、单剂量、交叉研究。
Respir Med. 2007 Apr;101(4):845-9. doi: 10.1016/j.rmed.2006.02.020. Epub 2007 Feb 1.

引用本文的文献

1
Pharmacologic management of the hospitalized pediatric asthma patient.住院小儿哮喘患者的药物治疗
Clin Rev Allergy Immunol. 2001 Jun;20(3):293-326. doi: 10.1385/CRIAI:20:3:293.
2
Pharmacokinetic optimisation of asthma treatment.哮喘治疗的药代动力学优化
Clin Pharmacokinet. 1994 May;26(5):396-418. doi: 10.2165/00003088-199426050-00006.
3
Long- versus short-acting beta 2-agonists. Implications for drug therapy.长效与短效β2受体激动剂。对药物治疗的影响。
Drugs. 1994 Feb;47(2):207-22. doi: 10.2165/00003495-199447020-00001.
4
Bitolterol. A preliminary review of its pharmacological properties and therapeutic efficacy in reversible obstructive airways disease.比托特罗。对其在可逆性阻塞性气道疾病中的药理特性和治疗效果的初步综述。
Drugs. 1988 Jan;35(1):22-41. doi: 10.2165/00003495-198835010-00002.
5
The effect of respiratory disorders on clinical pharmacokinetic variables.呼吸系统疾病对临床药代动力学变量的影响。
Clin Pharmacokinet. 1990 Dec;19(6):462-90. doi: 10.2165/00003088-199019060-00004.