Department of Psychiatry and Behavioral Neurosciences, School of Medicine, and Department of Pharmacy Practice, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI.
Department of Emergency Medicine, Highland Hospital-Alameda Health System, University of California, San Francisco, CA.
Ann Emerg Med. 2022 Dec;80(6):509-524. doi: 10.1016/j.annemergmed.2022.05.032. Epub 2022 Aug 6.
Buprenorphine induction for treating opioid use disorder is being implemented in emergency care. During this era of high-potency synthetic opioid use, novel and divergent algorithms for buprenorphine induction are emerging to optimize induction experience, facilitating continued treatment. Specifically, in patients with chronic fentanyl or other drug exposures, some clinicians are using alternative buprenorphine induction strategies, such as quickly maximizing buprenorphine agonist effects (eg, macrodosing) or, conversely, giving smaller initial doses and slowing the rate of buprenorphine dosing to avoid antagonist/withdrawal effects (eg, microdosing). However, there is a lack of foundational theory and empirical data to guide clinicians in evaluating such novel induction strategies. We present data from clinical studies of buprenorphine induction and propose a neuropharmacologic working model, which posits that acute clinical success of buprenorphine induction (achieving a positive agonist-to-withdrawal balance) is a nonlinear outcome of the opioid balance at the time of initial buprenorphine dose and mu-opioid-receptor affinity, lipophilicity, and mu-opioid-receptor intrinsic efficacy (the "ALE value") of the prior opioid. We discuss the rationale for administering smaller or larger doses of buprenorphine to optimize the patient induction experience during common clinical situations.
在急救护理中，正在实施丁丙诺啡诱导治疗阿片类药物使用障碍。在目前高浓度合成阿片类药物使用的时代，新的和不同的丁丙诺啡诱导算法正在出现，以优化诱导体验，促进持续治疗。具体来说，对于慢性芬太尼或其他药物暴露的患者，一些临床医生正在使用替代丁丙诺啡诱导策略，例如快速最大化丁丙诺啡激动剂的作用（例如，大剂量），或者相反，给予较小的初始剂量并减慢丁丙诺啡给药速度，以避免拮抗剂/戒断作用（例如，小剂量）。然而，缺乏基础性理论和经验数据来指导临床医生评估这些新的诱导策略。我们提出了丁丙诺啡诱导的临床研究数据，并提出了一个神经药理学工作模型，该模型假设丁丙诺啡诱导的急性临床成功（实现积极的激动剂-戒断平衡）是初始丁丙诺啡剂量时阿片类药物平衡、μ-阿片受体亲和力、脂溶性和μ-阿片受体内在效能（“ALE 值”）的非线性结果先前的阿片类药物。我们讨论了在常见临床情况下给予较小或较大剂量丁丙诺啡以优化患者诱导体验的原理。
