药代动力学/药效学特征beta-2-agonists特布他林、舒喘灵和非诺特罗。
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Hochhaus G,莫尔曼H
药代动力学/药效学特征beta-2-agonists特布他林、舒喘灵和非诺特罗。
Int中国新药杂志Toxicol。1992年9月30日(9):342 - 62。
- PubMed ID
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1358833 (在PubMed]
- 文摘
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临床药物动力学和药代动力学/动态属性的该项药物非诺特罗、沙丁胺醇、特布他林进行了综述。硫酸轭合物的主要代谢产物是人。这些衍生品相当弱的蛋白质绑定绑定最为明显观察到如非诺特罗(40%)。处理后注射用显示了所有物质的线性multi-exponential行为也stereo-selective药物动力学。注射用后,药物口服后主要通过肾脏消除过程而明显的代谢间隙(高第一遍效果)负责生物利用度很低,特别是对于非诺特罗(2%)。非诺特罗总间隙约两倍舒喘宁和特布他林。beplayapp七到15%的气溶胶交付通常到达体循环。然而在呼吸系统疾病患者,肺吸收是高度依赖疾病状态。药物动力学在儿童不明显不同于成人表示每公斤体重。肾功能衰竭患者而不是哮喘病患者显示改变药代动力学资料。 Only insignificant interactions with other drugs have been found. Pharmacokinetic/dynamic modeling approaches indicated that fenoterol is 25 times more active at the site of action than salbutamol and terbutaline, but all three drugs show similar bronchopulmonary selectivities. When the overall clinical activity, determined by pharmacokinetic and dynamic properties is compared, the activity gap is reduced: fenoterol (8) greater than salbutamol (2) greater than terbutaline (1). Differences in the first pass effect even inverse the pattern after oral administration. PK/PD modeling quantified the pulmonary effect after inhalation and suggested that the higher incidence of side effects for fenoterol might be linked to an overdosing problem. The application of PK/PD principles may improve the clinical usage and therapy of beta-2-adrenergic drugs.