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Oxycodone is a semi-synthetic morphine like opioid alkaloid with analgesic effect. Oxycodone exerts its analgesic effect by binding to mu receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opioids. Binding of the opiate receptor stimulates the exchange of GTP for PDB in the G-protein complex and inhibits adenylate cyclase, thereby preventing cAMP production. Furthermore, the release of nociceptive neurotransmitters such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine and norepinephrine is inhibited. Oxycodone also inhibits the release of vasopressin, somatostatin, insulin and glucagon. In addition, oxycodone closes voltage-gated N-type calcium channels and opens G protein-bound potassium channels, internally repairing potassium channels, resulting in hyperpolarization and decreased neural excitability.

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