成瘾研究与治疗杂志

抽象的

The Effects of 6β-Naltrexol, a Putative Neutral Opioid Antagonist, in Opioid-Dependent Subjects: A Proof-of-Concept Trial

John Mendelson, Linghui Li, Keith Flower, Will Harris, Jeremy R Coyle, C Y Angie Chen, Wolfgang Sadee and Gantt P Galloway

Potential complications of prescription opioid use include abuse and constipation. 6β-Naltrexol (6βNTX), a neutral opioid antagonist, may alleviate these complications when co-formulated with μ-opioid analgesics. In a double-blind ascending dose study, four subjects on methadone maintenance received 6βNTX (0.05, 0.15, 0.50 and 1.0 mg). 6βNTX was generally well tolerated; three of four subjects reported willingness to take higher doses. Increased gastrointestinal activity was evidenced by decreased oral-cecal transit time and prompt laxation at higher doses.