Opioids

Opioids

Zollner C; Stein C

Handbook Of Experimental Pharmacology

2007

Humans; Analgesics; Animals; Molecular Sequence Data; Chronic disease; Biomarkers of Pain; Drug Tolerance; Receptors; Amino Acid Sequence; Ligands; Opioid/adverse effects/pharmacology/therapeutic use; Opioid/drug effects

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.

2007

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