Standiford Helm, Andrea M Trescot, James Colson, Nalini Sehgal, Sanford Silverman
BACKGROUND: The opioid receptor antagonists naloxone and naltrexone are competitive antagonists at the mu, kappa, and sigma receptors with a higher affinity for the mu receptor and lacking any mu receptor efficacy. Buprenorphine is classified as a partial agonist. It has a high affinity, but low efficacy at the mu receptor where it yields a partial effect upon binding. It also, however, possesses kappa receptor antagonist activity making it useful not only as an analgesic, but also in opioid abuse deterrence, detoxification, and maintenance therapies...
March 2008: Pain Physician