Absorption of naloxone in patients prescribed buprenorphine-naloxone

IF 2.5 4区 医学 Q2 SUBSTANCE ABUSE
Ian Michel BA, Domenic Ochal BSc, Aniket Paharia, Paul Jannetto PhD, Scott Breitinger MD, Tyler Oesterle MD, MPH
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Abstract

Background and Objectives

When administered as prescribed, the naloxone component of buprenorphine-naloxone combination medications is putatively considered inert due to reduced naloxone bioavailability via transmucosal. However, there is a growing body of evidence to the contrary. The aim of our study is to determine the extent of naloxone absorption in a large cohort of patients receiving sublingual buprenorphine-naloxone.

Methods

Using the Mayo Clinic Unified Data Platform, 425 patients prescribed sublingual buprenorphine/naloxone who received a controlled substance monitoring panel (CSMP) between January 1, 2022, and January 1, 2023 were identified and included. The CSMP is an immunoassay panel that confirms positive results quantitatively with gas chromatography mass spectrometry or liquid chromatography tandem mass spectrometry. This panel provides urinary detection for buprenorphine (cutoff: 5 ng/mL), naloxone (25 ng/mL), as well as their respective metabolites norbuprenorphine (5 ng/mL), norbuprenorphine-glucuronide (20 ng/mL), and naloxone-glucuronide (100 ng/mL).

Results

Of our 425 patients, 76% had norbuprenorphine (n = 323), and 77% had norbuprenorphine-glucuronide (n = 327) in their toxicology tests, respectively. Naloxone-glucuronide was detected in 91% (n = 294) of the specimens with norbuprenorphine and 88.7% (n = 290) of the specimens with norbuprenorphine-glucuronide.

Conclusion and Scientific Significance

To our knowledge, this is the largest study to date demonstrating the presence of naloxone metabolites in patients taking combined buprenorphine-naloxone medications. The results of this study refute the notion that naloxone absorption is negligible when administered in sublingual preparations. Further research on how this absorption impacts medication usage, dosing, adherence, and side effects is necessary.

服用丁丙诺啡-纳洛酮的患者纳洛酮的吸收。
背景和目的:当按规定给药时,丁丙诺啡-纳洛酮联合药物中的纳洛酮成分被认为是惰性的,因为纳洛酮通过粘膜的生物利用度降低。然而,越来越多的证据表明事实并非如此。本研究的目的是确定接受舌下丁丙诺啡-纳洛酮治疗的大量患者对纳洛酮的吸收程度。方法:利用梅奥诊所统一数据平台,对2022年1月1日至2023年1月1日期间接受受控物质监测面板(CSMP)的425例服用丁丙诺啡/纳洛酮的患者进行识别和纳入。CSMP是一种免疫分析面板,可通过气相色谱质谱法或液相色谱串联质谱法定量确认阳性结果。该面板提供丁丙诺啡(截止值:5 ng/mL)、纳洛酮(25 ng/mL)及其各自的代谢物去甲丁丙诺啡(5 ng/mL)、去甲丁丙诺啡-葡萄糖醛酸盐(20 ng/mL)和纳洛酮-葡萄糖醛酸盐(100 ng/mL)的尿液检测。结果:在425例患者中,76%的患者在毒理学试验中使用去甲丁丙诺啡(n = 323), 77%的患者在毒理学试验中使用去甲丁丙诺啡-葡糖苷(n = 327)。去甲丁丙诺啡组和去甲丁丙诺啡-葡糖苷组分别有91% (n = 294)和88.7% (n = 290)检出纳洛酮-葡糖苷。结论和科学意义:据我们所知,这是迄今为止证明服用丁丙诺啡-纳洛酮联合药物的患者中存在纳洛酮代谢物的最大研究。本研究的结果驳斥了纳洛酮在舌下制剂中吸收可以忽略不计的观点。有必要进一步研究这种吸收如何影响药物的使用、剂量、依从性和副作用。
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来源期刊
CiteScore
5.00
自引率
0.00%
发文量
118
期刊介绍: The American Journal on Addictions is the official journal of the American Academy of Addiction Psychiatry. The Academy encourages research on the etiology, prevention, identification, and treatment of substance abuse; thus, the journal provides a forum for the dissemination of information in the extensive field of addiction. Each issue of this publication covers a wide variety of topics ranging from codependence to genetics, epidemiology to dual diagnostics, etiology to neuroscience, and much more. Features of the journal, all written by experts in the field, include special overview articles, clinical or basic research papers, clinical updates, and book reviews within the area of addictions.
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