Opioid Receptors.
Opioids are the oldest and most potent drugs for the treatment of severe pain. Their clinical application is undisputed in acute (e.g., postoperative) and cancer pain, but their long-term use in chronic pain has met increasing scrutiny. This article reviews mechanisms underlying opioid analgesia and other opioid actions. It discusses the structure, function, and plasticity of opioid receptors; the central and peripheral sites of analgesic actions and side effects; endogenous and exogenous opioid receptor ligands; and conventional and novel opioid compounds. Challenging clinical situations, such as the tension between chronic pain and addiction, are also illustrated.
Department of Anesthesiology and Critical Care Medicine, Freie Universität Berlin, Charité Campus Benjamin Franklin, 12200 Berlin, Germany; email: christoph.stein@charite.de.|Helmholtz Virtual Institute, Multifunctional Biomaterials for Medicine, 14513 Teltow, Germany.
Christoph
C
Stein
D000701:Analgesics, Opioid / Q000494:pharmacology / Q000627:therapeutic use*; D059350:Chronic Pain / Q000188:drug therapy; D004361:Drug Tolerance; D006801:Humans; D008024:Ligands; D009292:Narcotic Antagonists / Q000627:therapeutic use; D009473:Neuronal Plasticity; D009293:Opioid-Related Disorders / Q000209:etiology; D010146:Pain / Q000188:drug therapy* / Q000378:metabolism; D011957:Receptors, Opioid / Q000819:agonists* / Q000187:drug effects / Q000378:metabolism*; D015398:Signal Transduction; D013997:Time Factors
D000701:Analgesics, Opioid; D008024:Ligands; D009292:Narcotic Antagonists; D011957:Receptors, Opioid
addiction; inflammation; pain; peripheral; plasticity; tolerance