Newnham D M, Wheeldon N M, McFarlane L C, Clark G A, McDevitt D G, Lipworth B J
Department of Clinical Pharmacology, University of Dundee, Ninewells Hospital and Medical School, UK.
Eur J Clin Pharmacol. 1994;46(6):511-5. doi: 10.1007/BF00196107.
Extrapulmonary beta 2-adrenoceptor mediated responses to salbutamol were evaluated in 9 healthy female subjects during the follicular (day 2-4, Visit 1) and luteal (day 21-23, Visit 2) phases of the menstrual cycle, and were compared with those of 9 age-matched male controls. At each visit, salbutamol was given by intravenous infusion for 30 minutes at a dose of 0.2 mg.kg-1.min-1. Plasma salbutamol concentration and responses in heart rate (HR), finger tremor (Tr), Q-T interval (Q-Tc), serum potassium (K), serum insulin (Ins) and serum glucose (Glu) were measured at baseline and at 10, 20 and 30 minutes after commencing the infusion. Comparisons were made between sexes and between visits for peak responses calculated as percentage change from baseline. Mean plasma salbutamol concentration (ng.ml-1) were not significantly different between males and females on Visit 1: 6.9 (95% CI 6.01, 7.82) vs 7.3 (95% CI 6.4, 8.3), or on Visit 2: 6.9 (95% CI 6.0, 7.8) vs 7.2 (95% CI 6.3, 8.1). On Visit 1, significantly greater responses were demonstrated in females, compared with males for K (as mean difference): 6 (95% CI 1, 11)%, Tr: 17 (95% CI 1, 33)%, Q-Tc: 8 (95% CI 2, 14)% and Ins: 276 (95% CI 71, 481)%. In addition, a significantly greater response was demonstrated in females on Visit 1 compared with males on Visit 2 for HR (as mean difference): 32 (95% CI 1, 63)%, and for Ins: 262 (95% CI 57, 467)%. Thus, despite no difference in plasma salbutamol concentrations, female subjects exhibited greater responsiveness to salbutamol compared with males during the follicular phase of the menstrual cycle. This suggests that in vivo, females have enhanced sensitivity of extrapulmonary beta 2-adrenoceptors.
在9名健康女性受试者的月经周期卵泡期（第2 - 4天，第1次访视）和黄体期（第21 - 23天，第2次访视）评估了肺外β2 - 肾上腺素能受体介导的对沙丁胺醇的反应，并与9名年龄匹配的男性对照进行了比较。每次访视时，以0.2mg·kg-1·min-1的剂量静脉输注沙丁胺醇30分钟。在基线以及开始输注后10、20和30分钟测量血浆沙丁胺醇浓度以及心率（HR）、手指震颤（Tr）、Q - T间期（Q - Tc）、血清钾（K）、血清胰岛素（Ins）和血清葡萄糖（Glu）的反应。以相对于基线的百分比变化计算的峰值反应在性别之间以及访视之间进行比较。第1次访视时，男性和女性的平均血浆沙丁胺醇浓度（ng·ml-1）无显著差异：6.9（95%CI 6.01, 7.82）对7.3（95%CI 6.4, 8.3）；第2次访视时：6.9（95%CI 6.0, 7.8）对7.2（95%CI 6.3, 8.1）。在第1次访视时，女性在K（平均差异）方面的反应显著大于男性：6（95%CI 1, 11）%，Tr：17（95%CI 1, 33）%，Q - Tc：8（95%CI 2, 14）%，Ins：276（95%CI 71, 481）%。此外，在第1次访视时女性在HR（平均差异）方面的反应显著大于第2次访视时的男性：32（95%CI 1, 63）%，Ins方面：262（95%CI 57, 467）%。因此，尽管血浆沙丁胺醇浓度无差异，但在月经周期的卵泡期，女性受试者对沙丁胺醇的反应性高于男性。这表明在体内，女性肺外β2 - 肾上腺素能受体的敏感性增强。
