Oxycodone is a semisynthetic opioid synthesized from thebaine, an opioid alkaloid found in the Persian poppy, and one of the many alkaloids found in the opium poppy. It is a moderately potent opioid analgesic (orally roughly 1.5 times more potent than morphine), generally indicated for relief of moderate to severe pain.Oxycodone was developed in 1917 in Germany as one of several semi-synthetic opioids in an attempt to improve on the existing opioids.
Oxycodone is available as single-ingredient medication in immediate release and controlled release. Parenteral formulations of 10 mg/mL and 50 mg/mL are available in the UK for IV/IM administration. Combination products are also available as immediate-release formulations, with non-narcotic analgesic ingredients such as paracetamol (acetaminophen) and nonsteroidal anti-inflammatory drugs (NSAIDs), including aspirin and ibuprofen.
As it has euphoric effects similar to other opioids, oxycodone is one of the drugs abused in the current opioid epidemic in the United States. An abuse-deterrent combination with naloxone is available in managed-release tablets. If injected, the naloxone precipitates opioid withdrawal symptoms and blocks the effect of the medication. However, there have been concerns raised about the effectiveness of the abuse prevention measures.
Serious side effects of oxycodone include reduced sensitivity to pain (beyond the pain the drug is taken to reduce), euphoria, anxiolysis, feelings of relaxation, and respiratory depression. Common side effects of oxycodone include constipation (23%), nausea (23%), vomiting (12%), somnolence (23%), dizziness (13%), itching (13%), dry mouth (6%), and sweating (5%). 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, oxycodone can cause shallow breathing, slowed heart rate, cold/clammy skin, pauses in breathing, low blood pressure, constricted pupils, circulatory collapse, respiratory arrest, and death.
Oxycodone overdose has also been described to cause spinal cord infarction in high doses and ischemic damage to the brain, due to prolonged hypoxia from suppressed breathing.
Oxycodone in combination with naloxone in managed-release tablets, has been formulated to both deter abuse and reduce “opioid-induced constipation”.
Dependence, addiction, and withdrawal
Main article: Opioid dependence
The risk of experiencing severe withdrawal symptoms is high if a patient has become physically dependent and discontinues oxycodone abruptly. Medically, when the drug has been taken regularly over an extended period, it is 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 oxycodone withdrawal, as with other opioids, 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.
Oxycodone, like other opioid analgesics, tends to induce feelings of euphoria, relaxation and reduced anxiety in those who are occasional users. These effects make it one of the most commonly abused pharmaceutical drugs in the United States.
In the United States, more than 12 million people use opioid drugs recreationally. In 2010, 16,652 deaths were related to opioid overdose in combination with other drugs such as benzodiazepines and alcohol. In September 2013, the FDA released new labeling guidelines for long acting and extended release opioids requiring manufacturers to remove moderate pain as indication for use, instead stating the drug is for “pain severe enough to require daily, around-the-clock, long term opioid treatment.” The updated labeling will not restrict physicians from prescribing opioids for moderate, as needed use.
Oxycodone is the most widely recreationally used opioid in America. The U.S. Department of Health and Human Services estimates that about 11 million people in the US consume oxycodone in a non-medical way annually. In 2007, about 42,800 emergency room visits occurred due to “episodes” involving oxycodone. Diverted oxycodone may be taken orally or ingested through insufflation; used intravenously, or the heated vapors inhaled. In 2008, recreational use of oxycodone and hydrocodone were involved in 14,800 deaths. Some of the cases were due to overdoses of the acetaminophen component, resulting in fatal liver damage.
Reformulated OxyContin is causing some recreational users to change to heroin, which is cheaper and easier to obtain.