Jordan Colleen G, Kennalley Amy L, Roberts Alivia L, Nemes Kaitlyn M, Dolma Tenzing, Piper Brian J
Department of Medical Education, Geisinger Commonwealth School of Medicine, Scranton, PA 18509, USA.
Center for Pharmacy Innovation and Outcomes, Forty Fort, PA 18704, USA.
Pharmacy (Basel). 2022 Apr 19;10(3):48. doi: 10.3390/pharmacy10030048.
The opioid epidemic is an ongoing public health crisis, and the United States health system is overwhelmed with increasing numbers of opioid-related overdoses. Methocinnamox (MCAM) is a novel mu opioid receptor antagonist with an extended duration of action. MCAM has potential to reduce the burden of the opioid epidemic by being used as an overdose rescue treatment and a long-term treatment for opioid use disorder (OUD). The currently available treatments for OUD include naloxone, naltrexone, and methadone. These treatments have certain limitations, which include short duration of action, patient non-compliance, and diversion. A narrative review was conducted using PubMed and Google Scholar databases covering the history of the opioid epidemic, pain receptors, current OUD treatments and the novel drug MCAM. MCAM could potentially be used as both a rescue and long-term treatment for opioid misuse. This is due to its pseudo-irreversible antagonism of the mu opioid receptor, abnormally long duration of action of nearly two weeks, and the possibility of using kappa or delta opioid receptor agonists for pain management during OUD treatment. MCAM's novel pharmacokinetic and pharmacodynamic properties open a new avenue for treating opioid misuse.
阿片类药物流行是一场持续的公共卫生危机，美国卫生系统因与阿片类药物相关的过量用药人数不断增加而不堪重负。甲氧基肉桂肟（MCAM）是一种新型的μ阿片受体拮抗剂，作用持续时间延长。MCAM有潜力通过用作过量用药抢救治疗和阿片类药物使用障碍（OUD）的长期治疗来减轻阿片类药物流行的负担。目前可用的OUD治疗方法包括纳洛酮、纳曲酮和美沙酮。这些治疗方法有一定的局限性，包括作用持续时间短、患者不依从以及药物转移。使用PubMed和谷歌学术数据库进行了一项叙述性综述，内容涵盖阿片类药物流行的历史、疼痛受体、当前的OUD治疗方法以及新药MCAM。MCAM有可能用作阿片类药物滥用的抢救和长期治疗药物。这是由于其对μ阿片受体的拟不可逆拮抗作用、近两周的异常长作用持续时间，以及在OUD治疗期间使用κ或δ阿片受体激动剂进行疼痛管理的可能性。MCAM新的药代动力学和药效学特性为治疗阿片类药物滥用开辟了一条新途径。
