top of page
< Back

Oxycodone


Mechanism of action:

Oxycodone is an opioid and a semi-synthetic morphinan derivative. Oxycodone activates mu-opioid receptors in the central nervous system. Through Gi/o protein coupling, it inhibits adenylyl cyclase, lowers cAMP levels, and suppresses presynaptic voltage-gated Ca2+ channels, thereby blocking calcium influx and reducing the release of pain-related neurotransmitters such as glutamate and substance P. At the same time, it activates postsynaptic K+ channels, promotes potassium efflux, and causes neuronal hyperpolarization.

Reference(s):

1. DePriest AZ et al. (2015). Metabolism and Disposition of Prescription Opioids: A Review. Forensic Sci Rev. 


2. Leow KP et al. (1993). Determination of the serum protein binding of oxycodone and morphine using ultrafiltration. Ther Drug Monit. 


3. Ruan X et al. (2017). Revisiting Oxycodone Analgesia: A Review and Hypothesis. Anesthesiol Clin.

bottom of page