Trade names Roxicodone, OxyContin, Oxecta, OxyIR, Endone, Oxynorm, OxyNEO
Routes of administration: oral, intramuscular, intravenous, intranasal, subcutaneous, transdermal, rectal, epidural.
Bioavailability 60–87%.
Protein binding 45%,
Hepatic metabolism primarily CYP3A and to a lesser extent, CYP2D6 to
It is broken down by CYP3A4 to inactive metabolite noroxycodone, and by CYP2D6 active metabolite oxymorphone, which is more potent than the parent drug.
Biological half-life 2–4 hours.
Excretion Urine 83%.
A semisynthetic opioid synthesized from thebaine, an opioid alkaloid found in the opium poppy.
A moderately potent opioid analgesic generally indicated for relief of moderate to severe pain.
Available as single-ingredient medication in immediate release and controlled release.
Combination products are also available as immediate release formulations, with non-narcotic ingredients such as nonsteroidal anti-inflammatory drugs (NSAID) and acetaminophen.
Available as controlled-release tablet, intended to be taken every 12 hours.
Controlled-release oxycodone is comparable to instant-release oxycodone, morphine, and hydromorphone in management of moderate to severe cancer pain, with fewer side effects than morphine.
Only approved for oral use, available as tablets and oral solutions.
Has a significant antidepressant effect.[14]
Common side effects include:euphoria, constipation, fatigue, dizziness, nausea, vomiting, dry mouth, anxiety, itching, and sweating.
Less common side effects, experienced by less than 5% of patients, include loss of appetite, nervousness, abdominal pain, diarrhea, urine retention, dyspnea, and hiccups.
In high doses, overdoses, or in some persons not tolerant to opioids, can cause shallow breathing, bradycardia, cold-clammy skin, apnea, hypotension, miosis, circulatory collapse, respiratory arrest, and death.
Oxycodone in combination with naloxone in managed-release tablets, has been formulated to reduce side effects.
The risk of severe withdrawal symptoms is high if a patient has become physically dependent and discontinues oxycodone abruptly.
It should be withdrawn gradually rather than abruptly.
People who regularly use oxycodone recreationally or at higher than prescribed doses are at even higher risk of severe withdrawal symptoms.
The symptoms of withdrawal may include: anxiety, panic attack, nausea, insomnia, muscle pain, muscle weakness, fevers, and other flu-like symptoms.
Withdrawal symptoms have also been reported in newborns whose mothers had been either injecting or orally taking oxycodone during pregnancy.
Chronic use often causes concurrent hypogonadism or hormone imbalance.
Oxycodone and/or its major metabolites may be measured in blood or urine to monitor for clearance, abuse, or assist in a medicolegal death investigation.
Peak plasma levels of the drug are attained in about one hour, while in contrast, after a dose of OxyContin ,an oral controlled-release formulation, peak plasma levels of oxycodone occur in about three hours.
Is distributed to skeletal muscle, liver, intestinal tract, lungs, spleen, and brain.
With conventional oral doses starts to reduce pain within 10–15 minutes on an empty stomach.
OxyContin starts to reduce pain within one hour.
Metabolized by the cytochrome P450 enzyme system in the liver, making it vulnerable to drug interactions.
Some people are fast metabolizers, resulting in reduced analgesic effect, but increased adverse effects.
Some people are slow metabolisers, resulting in increased toxicity without improved analgesia.
The dose of OxyContin must be reduced in patients with reduced hepatic function.
Oxycodone and its metabolites are mainly excreted in the urine and sweat.
It accumulates in patients with renal impairment.
Taken orally, 20 mg of immediate release oxycodone is equivalent to 30 mg of morphine.
Extended release oxycodone is considered to be twice as potent as oral morphine.
One of the most commonly abused pharmaceutical drugs in the United States.
Estimates that about 11 million people in the US consume oxycodone in a non-medical way annually.
Diverted oxycodone may be taken orally or ingested through insufflation, used intravenously, or the heated vapors inhaled.
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