Phase I Study of Injectable, Depot Naltrexone for the Relapse Prevention Treatment of Opioid Dependence

作者：Wang Xuyi; Wang Juelu; Xiang Xiaojun; Li Haiyan; Liu Zheyuan; Gong Zhehui; Dong Guoming; Liu Gang; Li Jin; Hao Wei^*

来源：American Journal on Addictions, 2014, 23(2): 162-169.

DOI：10.1111/j.1521-0391.2013.12085.x

Background and ObjectivesWe tested long-acting injectable depot naltrexone for its tolerability, pharmacokinetics, and safety in Phase I.
MethodsThe Phase I trial enrolled 36 healthy participants in two panels (A, B). In Panel A, 24 subjects were randomly assigned to the high-dosage group (400mg naltrexone, n=6; placebo, n=6) or low-dosage group (200mg naltrexone, n=6; placebo, n=6). In Panel B, 12 subjects were randomized to take six doses of monthly injectable naltrexone (400mg) or placebo.
ResultsAfter a single injection of naltrexone 200 and 400mg, means (SD) of naltrexone plasma concentrations were .57 (.28)ng/ml and 1.5 (.8)ng/ml 30 days post-injection. There was no effect of accumulation after multiple dosing. Eleven of 30 subjects (36.67%) who were administered injectable depot naltrexone reported a total of 12 adverse events (AEs). Seven of these 11 AEs were coded as possibly related with study medication. All treatment-related AEs were mild in severity. No serious treatment-related AEs occurred.
Discussion and ConclusionsThis long-acting formulation of injectable depot naltrexone is well tolerated, results in constant plasma concentration of naltrexone for at least 1 month.
Scientific SignificanceThe tolerability and safety of long-acting injectable depot naltrexone are good. (Am J Addict 2014;23:162-169)

• 出版日期2014-3
• 单位中南大学