Le Roux A M, Kotze D, Wium C A, Van Jaarsveld P P, Joubert J R
Department of Pharmacology, University of Stellenbosch, South Africa.
Respiration. 1991;58(3-4):192-7. doi: 10.1159/000195925.
Inhaled and oral salbutamol were compared in 12 asthmatic patients for prophylaxis in antigen-induced asthma. The patients were pretreated with 0.2- and 1.0-mg doses of inhaled salbutamol and with the standard oral 4- and 8-mg slow-release (SR) salbutamol preparations. Bronchodilatation was monitored over the ensuing 3 h and protection against antigen challenge at the end of the period. On each study day the degree of baseline airway hyperreactivity was determined by histamine challenge. Precautions were taken during the antigen challenge to ensure a reproducible response. Blood levels of salbutamol were monitored at hourly intervals for the 3 h after treatment and during the asthmatic reaction subsequent to challenge. Both the 0.2- and 1.0-mg inhalations caused immediate bronchodilation as compared to a placebo (p less than 0.05), but only the 1.0-mg dose protected subjects against antigen challenge (p less than 0.05). In comparison to the placebo, no bronchodilatation was achieved with the standard 4-mg oral preparation in spite of measurable blood levels, nor were the patients protected against antigen challenge at 3 h after pretreatment. However, the 8-mg SR salbutamol caused significant bronchodilatation within 2 h and suppressed antigen challenge responses as compared to placebo (p less than 0.05). It can be concluded that doses of inhaled salbutamol higher than the conventional 0.2- or the standard 4-mg oral preparations are required to protect asthmatics against inadvertent antigen exposure. In patients who are unable to use inhalers effectively, the SR preparation can be considered as an alternative.
对12名哮喘患者吸入和口服沙丁胺醇预防抗原诱发哮喘的效果进行了比较。患者分别接受0.2毫克和1.0毫克剂量的吸入沙丁胺醇以及标准口服4毫克和8毫克缓释(SR)沙丁胺醇制剂的预处理。在随后的3小时内监测支气管扩张情况,并在该时间段结束时监测对抗原激发的保护作用。在每个研究日,通过组胺激发来确定基线气道高反应性的程度。在抗原激发过程中采取了预防措施以确保反应的可重复性。治疗后3小时以及激发后哮喘反应期间,每隔一小时监测一次沙丁胺醇的血药浓度。与安慰剂相比,0.2毫克和1.0毫克剂量的吸入均引起了即刻支气管扩张(p<0.05),但只有1.0毫克剂量能保护受试者对抗抗原激发(p<0.05)。与安慰剂相比,标准4毫克口服制剂尽管血药浓度可测,但未实现支气管扩张,且患者在预处理后3小时也未受到抗原激发的保护。然而,8毫克SR沙丁胺醇在2小时内引起了显著的支气管扩张,并与安慰剂相比抑制了抗原激发反应(p<0.05)。可以得出结论,需要高于传统0.2毫克或标准4毫克口服制剂剂量的吸入沙丁胺醇来保护哮喘患者免受意外抗原暴露的影响。对于无法有效使用吸入器的患者,可考虑使用SR制剂作为替代方案。