Controlled Drug Administration Studies of High-Dose Buprenorphine in Humans

摘要: Buprenorphine was developed in the early 1970s by Reckitt and Colman Products (Hull, UK) as part of a wide-ranging search for an effective analgesic with lower abuse potential reduced toxicity compared morphine (1). Many buprenorphine’s chemical pharmacological properties, including ready diffusion highly lipophilic drug across blood-brain barrier its high binding avidity opiate receptors, led to selection this thebaine derivative best compound further development. Despite high-affinity potency (25–40 times more potent than morphine), buprenorphine has efficacy pain relief is classified partial agonist at µ receptors. dissociates slowly from resulting long duration action and, potentially, abuse. These properties researchers United States Public Health Service’s Addiction Research Center investigate pharmacotherapy opioid addiction (2).