Poliwoda Salomon, Noor Nazir, Jenkins Jack S, Stark Cain W, Steib Mattie, Hasoon Jamal, Varrassi Giustino, Urits Ivan, Viswanath Omar, Kaye Adam M, Kaye Alan D
Department of Anesthesiology, Mount Sinai Medical Center.
Ochsner-LSU Health Shreveport Medical School.
Health Psychol Res. 2022 Aug 20;10(3):37517. doi: 10.52965/001c.37517. eCollection 2022.
Buprenorphine, a novel long-acting analgesic, was developed with the intention of two purposes: analgesia and opioid use disorder. Regarding its pharmacodynamics, it is a partial agonist at mu receptors, an inverse agonist at kappa receptors, and an antagonist at delta receptors. For the purpose of analgesia, three formulations of buprenorphine were developed: IV/IM injectable formulation (Buprenex®), transdermal patch formulation (Butrans®), and buccal film formulation (Belbuca®). Related to opioid dependence, the formulations developed were subcutaneous extended release (Sublocade®), subdermal implant (Probuphine®), and sublingual tablets (Subutex®). Lastly, in order to avoid misuse of buprenorphine for opioid dependence, two combination formulations paired with naloxone were developed: film formulation (Suboxone®) and tablet formulation (Zubsolv®). In this review, we present details of each formulation along with their similarities and differences between each other and clinical considerations.
丁丙诺啡是一种新型长效镇痛药，其研发目的有两个：镇痛和治疗阿片类药物使用障碍。就其药效学而言，它是μ受体的部分激动剂、κ受体的反向激动剂和δ受体的拮抗剂。为了实现镇痛目的，开发了三种丁丙诺啡制剂：静脉注射/肌肉注射剂型（Buprenex®）、透皮贴剂剂型（Butrans®）和口腔贴膜剂型（Belbuca®）。与阿片类药物依赖相关的制剂有皮下缓释剂型（Sublocade®）、皮下植入剂型（Probuphine®）和舌下片剂（Subutex®）。最后，为了避免丁丙诺啡被滥用用于阿片类药物依赖，开发了两种与纳洛酮联用的复方制剂：贴膜剂型（Suboxone®）和片剂剂型（Zubsolv®）。在本综述中，我们将介绍每种制剂的详细信息，以及它们之间的异同点和临床注意事项。
