Oxycodone is a drug in the opioid group used to treat moderate to severe pain. It is usually taken by mouth and is available in immediate-release and controlled-release (delayed-release) formulations. Pain relief usually begins within fifteen minutes and lasts up to six hours in the immediate-release formulation. Combination products with acetaminophen, ibuprofen, naloxone and aspirin are also available.



Oxycodone, a semisynthetic opioid, is a highly selective full agonist of the μ-opioid receptor. Oxycodone has a low affinity for the δ-opioid receptor and the κ-opioid receptor , where it is also an agonist. Binding to the opioid receptors results in an opening of potassium channels and a block of calcium channels, resulting in hyperpolarization of neurons in the brain. This makes nerve cells less excitable, suppressing pain transmission to the brain.


Oxycodone has an oral bioavailability of 60% to 87%, which is unaffected by food intake. Protein binding is 45%. In this regard, oxycodone is primarily bound to serum albumin. Hepatic metabolism of oxycodone is extensive and is accomplished by 4 major reactions. CYP3A4 and CYP3A5 perform N-demethylation, CYP2D6 performs O-demethylation, and 6-keto reduction and conjugation are performed by as yet unknown enzymes. Oxycodone and its metabolites are excreted in the urine. The established elimination half-life of oxycodone is 3.2 hours for immediate-release formulations and 4.5 hours for extended-release formulations.

Drug Interactions

Drug-drug interactions may occur when concomitantly taking substances that are also degraded or induced by the CYP3A4, CYP3A5, and CYP2D6 enzymes. Increased or decreased plasma levels of the drugs taken and significant side effects may occur.


Side effects

Common side effects are euphoria, constipation, nausea, vomiting, loss of appetite, drowsiness, dizziness, itching, dry mouth, and sweating.

Severe side effects may include addiction, dependence, hallucinations, respiratory depression (a decrease in breathing), bradycardia, and low blood pressure. Those who are allergic to codeine may also be allergic to oxycodone.

The use of oxycodone in early pregnancy appears to be relatively safe.

The risk of experiencing severe withdrawal symptoms is high if a patient has become physically dependent and oxycodone is abruptly discontinued. If oxycodone has been taken regularly for a long period of time, it should be discontinued gradually rather than abruptly. People who take oxycodone regularly as a recreational drug or at higher than prescribed doses are at even higher risk for severe withdrawal symptoms. Symptoms of oxycodone withdrawal, as with other opioids, may include anxiety, panic attacks, nausea, insomnia, muscle pain, muscle weakness, fever, and other flu-like symptoms.

Toxicological Data

LD50 (rat, oral): 320 mg-kg-1

Chemical & physical properties

ATC Code N02AA05
Formula C18H21NO4
Molar Mass (g·mol−1) 315,36
Physical State solid
Melting Point (°C) 219
PKS Value 8.53
CAS Number 76-42-6
PUB Number 5284603
Drugbank ID DB00497

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All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.


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