Human Pharmacology and Abuse Potential of the Analgesic Buprenorphine

TLDR

Buprenorphine is a morphine‑like opioid that is 25–50 times more potent and longer‑acting. The study assessed buprenorphine’s abuse potential and its usefulness for treating narcotic addiction. Buprenorphine produced minimal clinically significant physical dependence, blocked morphine effects for about 29.5 h, has lower intrinsic activity than morphine, and demonstrates low abuse potential while being effective for treating narcotic addiction because of its long action, low dependence, lower toxicity, and narcotic blockade.

Abstract

Buprenorphine was evaluated for its abuse potential and utility in treating narcotic addiction. The drug was morphine-like but was 25 to 50 times more potent than morphine and was longer-acting. Little if any physical dependence of clinical significance was produced by buprenorphine. The effects of morphine to 120-mg doses were blocked by buprenorphine, a blockade that persisted for 29 1/2 hours. In man, buprenorphine has less intrinsic activity than morphine, and as such, as a low abuse potential. Moreover, the drug has potential for treating narcotic addiction since it is acceptable to addicts, is long-acting, produces a low level of physical dependence such that patients may be easily detoxified, is less toxic than drugs used for maintenance therapy, and blocks the effects of narcotics.