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Oxykodon je polosyntetický opioidní alkaloid podobný morfinu s analgetickým účinkem. Oxykodon uplatňuje svůj analgetický účinek vazbou na mu-receptory v centrálním nervovém systému (CNS), čímž napodobuje účinky endogenních opioidů. Vazba opiátového receptoru stimuluje výměnu GTP za PDB v G-proteinovém komplexu a inhibuje adenylátcyklázu, čímž zabraňuje tvorbě cAMP. Dále je inhibováno uvolňování nociceptivních neurotransmiterů, jako je substance P, kyselina gama-aminomáselná (GABA), dopamin, acetylcholin a noradrenalin. Oxykodon rovněž inhibuje uvolňování vazopresinu, somatostatinu, inzulinu a glukagonu. Kromě toho oxykodon uzavírá napěťově řízené vápníkové kanály typu N a otevírá draslíkové kanály vázané na G-protein, vnitřně opravuje draslíkové kanály, což vede k hyperpolarizaci a snížení nervové excitability.
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