Rehman Saif Ur, Maqsood Muhammad Haisum, Bajwa Hamza, Tameez Ud Din Asim, Malik Mustafa N
Internal Medicine, King Edward Medical University / Mayo Hospital, Lahore, PAK.
Internal Medicine, Rawalpindi Medical University, Rawalpindi, PAK.
Cureus. 2019 Jun 4;11(6):e4827. doi: 10.7759/cureus.4827.
Opioid use disorder (OUD) is a rapidly growing challenge worldwide and is characterized by an increase in dependence on opioids up to a point that a person loses control over the drug use. Multiple drugs are approved for its treatment, including methadone, buprenorphine, and diazepam. Although not approved, clonidine is also used for the treatment of OUD. On May 16, 2018, the United States Food and Drug Administration (FDA) approved a new drug lofexidine hydrochloride for the treatment of opioid withdrawal symptoms. Lofexidine is a centrally acting alpha two receptor agonist. It reduces the neurochemical surge by inhibiting the conversion of adenosine triphosphate (ATP) into cyclic adenosine monophosphate (cAMP) which in turn decrease the sympathetic outflow. This results in the improvement of withdrawal symptoms. When compared with methadone and buprenorphine, it is equally effective in controlling withdrawal symptoms. Its efficacy is also similar to clonidine with a better side effects profile. The adverse effects of lofexidine include bradycardia, hypotension, orthostasis, somnolence, sedation, dry mouth, and rebound elevations in blood pressure and prolongation of QT interval. Lofexidine is contraindicated in patients who are on beta-blockers and angiotensin converting enzyme inhibitors (ACE inhibitors). In our review, we have discussed the clinical efficacy and safety profile of lofexidine in treating opioid withdrawal symptoms and its comparison to other available treatment options.
阿片类药物使用障碍（OUD）在全球范围内是一个迅速增长的挑战，其特征是对阿片类药物的依赖增加，直至一个人失去对药物使用的控制。多种药物被批准用于治疗该疾病，包括美沙酮、丁丙诺啡和地西泮。尽管未被批准，但可乐定也用于治疗OUD。2018年5月16日，美国食品药品监督管理局（FDA）批准了一种新药盐酸洛非西定用于治疗阿片类药物戒断症状。洛非西定是一种中枢作用的α2受体激动剂。它通过抑制三磷酸腺苷（ATP）转化为环磷酸腺苷（cAMP）来减少神经化学激增，进而减少交感神经输出。这导致戒断症状得到改善。与美沙酮和丁丙诺啡相比，它在控制戒断症状方面同样有效。其疗效也与可乐定相似，但副作用更小。洛非西定的不良反应包括心动过缓、低血压、直立性低血压、嗜睡、镇静、口干以及血压反弹性升高和QT间期延长。正在服用β受体阻滞剂和血管紧张素转换酶抑制剂（ACE抑制剂）的患者禁用洛非西定。在我们的综述中，我们讨论了洛非西定在治疗阿片类药物戒断症状方面的临床疗效和安全性概况，以及它与其他可用治疗方案的比较。
