Simonsson B G, Svedenblad H, Ström B
Scand J Respir Dis. 1976;57(5):252-8.
A beta2-receptor agonist, terbutaline (Bricanyl), in doses of 2.5 and 5 mg was inhaled by IPPB with a Bird Mark 8 in a double-blind cross-over randomized study on consecutive days in 12 patients with at least 15% reversibility of PEFR or FEV 1.0. One minute after the inhalation of 2.5 mg, PEFR had increased significantly; the greatest effect (+ 34%) was recorded after 120 min. After 5 mg the increase was more marked, with the greatest recorded effect (+ 43%) after 120 min; FEV1 and VC showed similar changes with a tendency towards greater and longer effects after the larger dose. Heart rate did not change. Systolic and diastolic blood pressures decreased at the most with 9 and 5 mmHg respectively, 30 min after 5 mg terbutaline. One patient reported tremor and palpitations 5 min after inhaling 5 mg. Our patients who were treated with beta-adrenergic drugs showed less systemic effects after the same dose of terbutaline than previously non-treated normal subjects in an earlier study. This may support recent findings of drug-induced tolerance to beta-stimulating agents in the heart and skeletal muscles with preservation of good effect on the airway smooth muscles, here shown as having a good residual bronchodilatory effect with clinically non-important effects on heart rate and tremor.
在一项针对12名具有至少15%的呼气峰流速(PEFR)或第1秒用力呼气容积(FEV1.0)可逆性的患者的双盲交叉随机研究中,连续数天使用Bird Mark 8型间歇正压通气(IPPB)装置吸入剂量为2.5毫克和5毫克的β2受体激动剂特布他林(博利康尼)。吸入2.5毫克后1分钟,PEFR显著增加;120分钟后记录到最大效应(+34%)。吸入5毫克后增加更为明显,120分钟后记录到最大效应(+43%);FEV1和肺活量(VC)显示出类似变化,较大剂量后效应更大且持续时间更长。心率未改变。吸入5毫克特布他林30分钟后,收缩压和舒张压分别最多下降9毫米汞柱和5毫米汞柱。一名患者在吸入5毫克后5分钟报告有震颤和心悸。在我们的研究中,接受β肾上腺素能药物治疗的患者在相同剂量的特布他林治疗后,全身效应比早期一项研究中未接受过治疗的正常受试者更少。这可能支持了最近关于心脏和骨骼肌对β刺激剂产生药物诱导耐受性的研究结果,同时对气道平滑肌仍保持良好效果,在此表现为具有良好的残余支气管扩张作用,而对心率和震颤的影响在临床上并不重要。