Opioids.
Opioids are the most effective and widely used drugs in the treatment of severe pain. They act through G protein-coupled receptors. Four families of endogenous ligands (opioid peptides) are known. The standard exogenous opioid analgesic is morphine. Opioid agonists can activate central and peripheral opioid receptors. Three classes of opioid receptors (mu, delta, kappa) have been identified. Multiple pathways ofopioid receptor signaling (e.g., G(i/o) coupling, cAMP inhibition, Ca++ channel inhibition) have been described. The differential regulation of effectors, preclinical pharmacology, clinical applications, and side effects will be reviewed in this chapter.
Zöllner
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Klinik für Anaesthesiologie und operative Intensivmedizin, Charité-Universitätsmedizin Berlin, Campus Benjamin Franklin, Hindenburgdamm 30, 12200 Berlin, Germany.
Stein
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D000595:Amino Acid Sequence; D000701:Analgesics, Opioid / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D002908:Chronic Disease; D004361:Drug Tolerance; D006801:Humans; D008024:Ligands; D008969:Molecular Sequence Data; D011957:Receptors, Opioid / Q000187:drug effects
D000701:Analgesics, Opioid; D008024:Ligands; D011957:Receptors, Opioid