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.

丁丙诺啡正在急救护理中实施治疗阿片类药物使用障碍的诱导治疗。在这个使用高效合成阿片类药物的时代，正在出现用于丁丙诺啡诱导的新颖且不同的算法，以优化诱导体验，促进持续治疗。具体来说，对于长期接触芬太尼或其他药物的患者，一些临床医生正在使用替代的丁丙诺啡诱导策略，例如快速最大化丁丙诺啡激动剂的作用（例如，大剂量给药），或者相反，给予较小的初始剂量并减慢丁丙诺啡的给药速度以避免拮抗剂/戒断作用（例如，微剂量）。然而，缺乏基础理论和经验数据来指导临床医生评估这种新型诱导策略。我们提供了丁丙诺啡诱导临床研究的数据，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（实现积极的激动剂与戒断平衡）是初始丁丙诺啡时阿片类药物平衡的非线性结果先前阿片类药物的剂量和 μ-阿片受体亲和力、亲脂性和 μ-阿片受体内在功效（“ALE 值”）。我们讨论了在常见临床情况下使用更小或更大剂量丁丙诺啡以优化患者诱导体验的基本原理。它假定丁丙诺啡诱导的急性临床成功（实现积极的激动剂与戒断平衡）是丁丙诺啡初始剂量和 μ-阿片受体亲和力、亲脂性和 μ-阿片类药物平衡时阿片类药物平衡的非线性结果。先前阿片类药物的受体内在功效（“ALE 值”）。我们讨论了在常见临床情况下使用更小或更大剂量丁丙诺啡以优化患者诱导体验的基本原理。它假定丁丙诺啡诱导的急性临床成功（实现积极的激动剂与戒断平衡）是丁丙诺啡初始剂量和 μ-阿片受体亲和力、亲脂性和 μ-阿片类药物平衡时阿片类药物平衡的非线性结果。先前阿片类药物的受体内在功效（“ALE 值”）。我们讨论了在常见临床情况下使用更小或更大剂量丁丙诺啡以优化患者诱导体验的基本原理。