van den Berg W, Leferink J G, Maes R A, Fokkens J K, Kreukniet J, Bruynzeel P L
Eur J Respir Dis Suppl. 1984;134:181-93.
In 8 asthmatic subjects, serum concentrations of terbutaline were correlated with changes in volume of air expelled in the first second of forced expiration (FEV1), other parameters of lung function, c-AMP plasma concentrations and finger tremor values after administration of either 5 mg terbutaline sulphate orally, 0.5 mg terbutaline sulphate subcutaneously or an oral placebo. Prior to the investigation, the patients had not used bronchodilators for 10-14 days. All lung function parameters and tremor values showed a significant correlation with the terbutaline (serum) concentrations in the central compartment and with the c-AMP plasma concentrations. FEV1 was the least variable lung function test. The maximal effect on FEV1 occurred 30-60 min after the subcutaneous dose and 2-4 h after the oral dose, corresponding with the maximal terbutaline serum concentrations and c-AMP plasma levels. In this study, the FEV1 improvement showed a linear relationship with the terbutaline serum concentrations between 1.6 and 6 ng/mL. Three out of 8 asthmatics showed an increase in tremor of more than 6 dB after subcutaneous administration, which corresponded with the awareness of this side-effect. In contrast to theophylline and anticholinergic agents, terbutaline serum concentrations showed a very low interindividual variance. As a consequence, the serum terbutaline concentration was almost predictable. However, the lung function improvement was not predictable since there seems to exist an individual sensitivity for this agonist.
在8名哮喘患者中,口服5毫克硫酸特布他林、皮下注射0.5毫克硫酸特布他林或口服安慰剂后,特布他林的血清浓度与用力呼气第一秒呼出的气量(FEV1)变化、其他肺功能参数、血浆环磷腺苷(c-AMP)浓度以及手指震颤值相关。在调查前,患者已停用支气管扩张剂10 - 14天。所有肺功能参数和震颤值均与中央室中的特布他林(血清)浓度以及血浆c-AMP浓度显著相关。FEV1是变异性最小的肺功能测试。皮下给药后30 - 60分钟以及口服给药后2 - 4小时,对FEV1产生最大效应,这与特布他林血清浓度和血浆c-AMP水平的最大值相对应。在本研究中,FEV1的改善与特布他林血清浓度在1.6至6纳克/毫升之间呈线性关系。8名哮喘患者中有3名在皮下给药后震颤增加超过6分贝,这与对这种副作用的感知相对应。与茶碱和抗胆碱能药物不同,特布他林血清浓度个体间差异非常小。因此,血清特布他林浓度几乎是可预测的。然而,肺功能的改善是不可预测的,因为似乎存在对这种激动剂的个体敏感性。