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非诺特罗干粉对哮喘患者的支气管扩张、致震颤、心血管及低钾血症作用的研究。

Studies on the bronchodilator, tremorogenic, cardiovascular and hypokalaemic effects of fenoterol dry powder in asthma.

作者信息

Bauer K G, Kaik B, Sertl K, Kaik G A

机构信息

University of Vienna Medical School, Department of Internal Medicine I, Division of Clinical Pharmacology, Vienna, Austria.

出版信息

Br J Clin Pharmacol. 1993 Oct;36(4):285-92. doi: 10.1111/j.1365-2125.1993.tb00366.x.

DOI:10.1111/j.1365-2125.1993.tb00366.x
PMID:12959305
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1364680/
Abstract
  1. The airway and tremor response and cardiovascular and hypokalaemic effects of single and cumulative doses of fenoterol given by dry powder capsules (DPC) and by metered dose inhaler (MDI) were studied in asthmatics in two randomized, crossover trials. 2. Single doses of fenoterol DPC and MDI (0.2 mg, 0.4 mg), investigated in 24 subjects, produced similar, dose-dependent increases in FEV1. Fenoterol DPC caused less tremor response and less hypokalaemic effects than fenoterol MDI. 3. Cumulative doses of fenoterol DPC and MDI (0.2, 0.6, 1.4, 3.0, 6.2 mg), investigated in 12 subjects, produced a comparable bronchodilatation (mean maximum increase in FEV1 was 0.53 +/- 0.06/0.52 +/- 0.081 for DPC/MDI) and a similar, dose-dependent rise in heart rate (35 +/- 3.81/41 +/- 2.25 beats min(-1)). The rise in tremor and the fall in plasma potassium were smaller after DPC than after MDI. The mean maximum changes were 51.58 +/- 6.41/95.83 +/- 6.75 cm s(-2) for tremor and -0.68 +/- 0.09/-0.96 +/- 0.10 mmol l(-1) for potassium. 4. Our findings may result from a difference in the pharmacokinetics of the dry powder and the aerosol formulation, particularly differences in distribution and absorption. 5. In conclusion, fenoterol DPC used in low therapeutic doses (0.2,0.4 mg), is preferable to the MDI. Fenoterol DPC used as rescue medication in high cumulative doses, do not suggest a greater safety margin than the MDI and the same restrictions should be considered for the fenoterol dry powder formulation as suggested for the MDI.
摘要
  1. 在两项随机交叉试验中,对哮喘患者研究了通过干粉胶囊(DPC)和定量吸入器(MDI)给予单次和累积剂量非诺特罗的气道和震颤反应以及心血管和低钾血症效应。2. 在24名受试者中研究的单次剂量非诺特罗DPC和MDI(0.2毫克、0.4毫克),使第一秒用力呼气容积(FEV1)产生了相似的剂量依赖性增加。非诺特罗DPC引起的震颤反应和低钾血症效应比非诺特罗MDI少。3. 在12名受试者中研究的非诺特罗DPC和MDI的累积剂量(0.2、0.6、1.4、3.0、6.2毫克),产生了相当的支气管扩张作用(DPC/MDI的FEV1平均最大增加量为0.53±0.06/0.52±0.081)以及相似的剂量依赖性心率升高(35±3.81/41±2.25次/分钟)。DPC给药后震颤增加和血浆钾下降比MDI后更小。震颤的平均最大变化为51.58±6.41/95.83±6.75厘米/秒²,钾的平均最大变化为-0.68±0.09/-0.96±0.10毫摩尔/升。4. 我们的发现可能源于干粉和气雾剂制剂药代动力学的差异特别是分布和吸收方面的差异。5. 总之,低治疗剂量(0.2、0.4毫克)使用的非诺特罗DPC比MDI更可取。高累积剂量用作急救药物的非诺特罗DPC,并未显示出比MDI有更大的安全边际,并且对于非诺特罗干粉制剂应考虑与MDI相同的限制。

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本文引用的文献

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Serum potassium and the electrocardiogram in hypokalemia.低钾血症时的血清钾与心电图
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Pharmacodynamic effects of inhaled dry powder formulations of fenoterol and colforsin in asthma.非诺特罗和双嘧达莫吸入干粉制剂在哮喘中的药效学作用。
Clin Pharmacol Ther. 1993 Jan;53(1):76-83. doi: 10.1038/clpt.1993.11.
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Assessment of beta-adrenergic receptor blockade after isamoltane, a 5-HT1-receptor active compound, in healthy volunteers.在健康志愿者中评估5-羟色胺1(5-HT1)受体活性化合物异戊胺后β-肾上腺素能受体阻滞情况。
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Airway response to salbutamol: effect of regular salbutamol inhalations in normal, atopic, and asthmatic subjects.气道对沙丁胺醇的反应:正常、特应性和哮喘患者中规律吸入沙丁胺醇的效果。
Thorax. 1982 Apr;37(4):280-7. doi: 10.1136/thx.37.4.280.
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Pretreatment of exercise-induced asthma by fenoterol delivered as inhalation powder and pressurized aerosol.用吸入粉雾剂和定量气雾剂递送的非诺特罗对运动诱发性哮喘进行预处理。
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A comparison between aerosol and inhaled powder administration of fenoterol in adult asthmatics.
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Inhaled powder compared with aerosol administration of fenoterol in asthmatic children.吸入性粉末与沙丁胺醇气雾剂在哮喘儿童中的应用比较。 (注:原文中“fenoterol”有误,正确的药物名应该是“salbutamol”,译文按照正确药物名翻译)
Arch Dis Child. 1980 Jan;55(1):73-4. doi: 10.1136/adc.55.1.73.
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A comparison of fenoterol powder capsules and fenoterol metered dose spray in bronchial asthma.非诺特罗粉胶囊与非诺特罗定量喷雾剂治疗支气管哮喘的比较。
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10
Fenoterol inhalation powder as an alternative to treatment with the metered dose inhaler.非诺特罗吸入粉作为定量吸入器治疗的替代方案。
Eur J Respir Dis Suppl. 1983;130:48-53.