通过计量剂量吸入和肌内注射输送的上腺素之间系统暴露的比较
Jack Yongfeng Zhang1, Mary Ziping Luo1, Tony Marrs1
1Amphastar Pharmaceuticals, Inc., Rancho Cucamonga, California, USA.
Journal of aerosol medicine and pulmonary drug delivery
|August 29, 2024
概括
普里马丁MIST (上腺素计量剂量吸入器) 与上腺素注射器和阿尔布特罗尔吸入器相比,显著降低了全身药物暴露. 这种较低的暴露与喘患者吸入上腺素的更安全的心血管特征相关.
科学领域:
- 药理学和毒理学 药理学和毒理学
- 呼吸系统医学 呼吸系统医学
- 心血管安全心血管安全
背景情况:
- 对于用于治疗喘的上腺素计量剂量吸入器 (MDIs) 的心血管安全存在担忧.
- 以前的担忧往往源于上腺素的注射途径,而不是吸入.
- 阿尔布醇吸入器是一种常见的喘治疗比较器.
研究的目的:
- 评估和比较通过MDI输送的上腺素系统性药物暴露与肌肉内 (IM) 注射.
- 为了比较上腺素MDI与阿尔布特罗尔MDI的全身暴露.
- 了解上腺素/阿尔布罗尔给药途径与心血管效应之间的关系.
主要方法:
- 一个随机的,评估者盲目的,三臂交叉研究在28名健康成年人.
- 在MDI和IM给药后,比较上腺素和阿尔布醇的血水平.
- 通过生命体征,心电图,不良事件和实验室测试来评估安全性.
主要成果:
- 上腺素MDI的全身药物暴露率比IM上腺素低约9倍,比albuterolMDI低约122倍.
- 上腺素MDI显示了快速的血药物清除,与IM上腺素或阿尔布特罗尔MDI不同.
- 上腺素MDI和阿尔布特罗尔MDI对心血管的影响很小;IM上腺素导致血压和心率的暂时增加.
结论:
- 上腺素MDI (Primatene MIST) 与IM上腺素和阿尔布特罗尔MDI相比,显示系统性药物暴露明显较低.
- 减少吸入上腺素的全身暴露与有利的安全性相关,缺乏显著的心血管不良影响.
- 研究结果支持上腺素MDI在喘治疗中的安全性,特别是与其他给药途径相比,心血管影响.
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