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长效丁丙诺啡制剂:临床实践的视角。

Prolonged-release buprenorphine formulations: Perspectives for clinical practice.

机构信息

Service universitaire d'addictologie de Lyon (SUAL), centre hospitalier Le Vinatier, 69500 Bron, France; Service d'addictologie, groupement hospitalier centre, Hospices Civils de Lyon, 69003 Lyon, France; Centre de soins, d'accompagnement et de prévention en addictologie, groupement hospitalier nord, Hospices Civils de Lyon, 69004 Lyon, France.

Service hospitalo-universitaire d'addictologie, CHU de Dijon, 21079 Dijon, France; INSERM U1093 cognition, action et plasticité sensorimotrice, UFR staps, université de Bourgogne Franche-Comté, 21078 Dijon, France.

出版信息

Therapie. 2020 Sep-Oct;75(5):397-406. doi: 10.1016/j.therap.2020.05.007. Epub 2020 May 18.

DOI:10.1016/j.therap.2020.05.007
PMID:32499082
Abstract

Buprenorphine and methadone are the two main opioid agonist treatments approved for opioid use disorder. Buprenorphine is a partial agonist of the mu opioid receptors, which has been merely available through sublingual form until now. In practice, the use of buprenorphine is smoother than that of methadone, and it induces reduced risks of overdose. However, sublingual buprenorphine also exposes to risks (e.g., withdrawal, misuse) and constraints (e.g., daily intake). Three new galenic formulations of prolonged-release buprenorphine (PRB) are being commercialized and should allow some improvements in patients' comfort and safety. This narrative review aims to describe the main technical features and efficacy and safety data of these PRBs, as well as patients' and professionals' expectancies and concerns, using data of the scientific literature and the regulatory texts. PRBs consist of one subcutaneous implant and two subcutaneous injection depots. Sixmo®/Probuphine® is a six-month-long implant which needs to be surgically placed and removed and is approved for subjects previously treated with a maximum daily dose of 8mg of sublingual buprenorphine, and can be used only for two successive periods of six months before the subject needs to be switched back to sublingual form. Sublocade® is a one-month-long depot formulation that is indicated in switch from sublingual buprenorphine, and which proposes only two dose schemes, i.e., 100 and 300mg monthly. Buvidal®/Brixadi® is a one-week- or one-month-long depot formulation with multiple dosages, which can be used in initiation or in switched from sublingual formulations. While opioid users report some concerns with a risk of coercive use of long-acting forms of buprenorphine, both users and professionals deem that these new specialties could be particularly appreciated in stabilized patients bothered with the daily intake of the treatments, or specific situations at risk of treatment dropout (e.g., following hospital discharge or prison release).

摘要

丁丙诺啡和美沙酮是两种被批准用于阿片类药物使用障碍的主要阿片类激动剂治疗药物。丁丙诺啡是μ阿片受体的部分激动剂,迄今为止仅以舌下形式使用。实际上,丁丙诺啡的使用比美沙酮更顺畅,并且它降低了过量的风险。然而,舌下丁丙诺啡也存在风险(例如戒断、滥用)和限制(例如每日摄入)。三种新的丁丙诺啡延长释放制剂(PRB)正在商业化,应该可以提高患者的舒适度和安全性。本叙述性综述旨在描述这些 PRB 的主要技术特点、疗效和安全性数据,以及患者和专业人员的期望和关注点,使用科学文献和监管文本中的数据。PRB 由一个皮下植入物和两个皮下注射储库组成。Sixmo®/Probuphine®是一种长达六个月的植入物,需要通过手术植入和取出,适用于先前接受过最大每日剂量为 8mg 舌下丁丙诺啡治疗的患者,并且只能连续使用两个六个月的时间段,然后患者需要转回舌下制剂。Sublocade®是一种为期一个月的储库制剂,适用于从舌下丁丙诺啡转换,仅提供两种剂量方案,即每月 100 和 300mg。Buvidal®/Brixadi®是一种为期一周或一个月的储库制剂,有多种剂量,可用于起始或从舌下制剂转换。虽然阿片类药物使用者对长效丁丙诺啡形式的强制使用存在一些担忧,但使用者和专业人员认为,这些新专业知识在稳定患者中可能特别受到赞赏,这些患者因每天摄入治疗药物而感到困扰,或在存在治疗中断风险的特定情况下(例如,出院后或出狱后)。

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