Jones Mark R, Carney Martin J, Kaye Rachel J, Prabhakar Amit, Kaye Alan D
Tulane University School of Medicine, New Orleans, LA, USA.
Department of Biochemistry, Bowdoin College, Brunswick, ME, USA.
Curr Pain Headache Rep. 2016 Jun;20(6):36. doi: 10.1007/s11916-016-0565-9.
Prescription opioid abusers frequently tamper with opioid tablets in order to either accelerate the delivery of the euphoria-inducing agent or to alter the route of delivery, such that it may be delivered intranasally or intravenously. As one strategy to combat the opioid epidemic in the USA, drug manufacturers have begun to explore formulations which resist such tampering by abusers. Techniques to prevent tampering consist of physical barriers to crushing, chewing, and drug extraction, or aversive or antagonistic agents, incorporated within the formulation itself. Recent years have seen the development of numerous extended-release opioid agents, which are described in this review. This article provides a comprehensive summary of the pharmacology, benefits, risks, and processes behind the development of currently available extended-release opioid drugs, as well as a glimpse into promising future formulations.
处方阿片类药物滥用者经常篡改阿片类药片，以加速产生欣快感的药物释放或改变给药途径，使其可以通过鼻内或静脉给药。作为美国应对阿片类药物流行的一项策略，药品制造商已开始探索能抵抗滥用者此类篡改行为的制剂。防止篡改的技术包括对碾碎、咀嚼和药物提取的物理屏障，或制剂本身所含的厌恶剂或拮抗剂。近年来已研发出多种缓释阿片类药物，本文对此进行综述。本文全面总结了目前可用的缓释阿片类药物的药理学、益处、风险及研发过程，还展望了未来有前景的制剂。
