Description

Oxycodone, sold under brand name OxyContin among others, is an opioid medication used for the treatment of moderate to severe pain. It is usually taken by mouth, and is available in immediate-release and controlled-release formulations. The onset of pain relief typically begins within 15 minutes and lasts for up to six hours with the immediate-release formulation. In the United Kingdom, it is available by injection. Combination products are also available with paracetamol (acetaminophen) or aspirin.

Common side effects include constipation, nausea, sleepiness, dizziness, itching, dry mouth, and sweating. Severe side effects may include addiction, respiratory depression (a reduction in breathing), and low blood pressure. Those allergic to codeine may also be allergic to oxycodone. The use of oxycodone in early pregnancy appears relatively safe. Opioid withdrawal may occur if rapidly stopped. Oxycodone acts by activating the μ-opioid receptor. When taken by mouth, it has roughly 1.5 times the effect of the equivalent amount of morphine.

Oxycodone was first made in Germany in 1916 from thebaine. It is available as a generic medication. In the United States, the wholesale cost per dose is less than US$0.30 as of 2018.[16] In 2016, it was the 54th most prescribed medication in the United States, with more than 14 million prescriptions. Oxycodone has been a common drug of abuse. A number of abuse-deterrent formulations are available, such as in combination with naloxone

Medical uses

Oxycodone is used for managing moderate to severe acute or chronic pain when other treatments are not sufficient. It may improve the quality of life in certain types of pain. It is unclear if use in chronic pain results in improved quality of life or ongoing pain relief.

Oxycodone is available as a controlled-release tablet, intended to be taken every 12 hours. A July 1996 study independent of Purdue Pharma, the drug’s originator, found the controlled-release formulation had a variable duration of action ranging from 10–12 hours. A 2006 review found that controlled-release oxycodone is comparable to immediate-release oxycodone, morphine, and hydromorphone in the management of moderate to severe cancer pain, with fewer side effects than morphine. The author concluded that the controlled-release form is a valid alternative to morphine and a first-line treatment for cancer pain. In 2014, the European Association for Palliative Care recommended oxycodone by mouth as a second-line alternative to morphine by mouth for cancer pain.

In the U.S., extended-release oxycodone is approved for use in children as young as 11 years old. The approved uses are for the relief of cancer pain, trauma pain, or pain due to major surgery, in children already treated with opioids, who can tolerate at least 20 mg per day of oxycodone; this provides an alternative to Duragesic (fentanyl), the only other extended-release opioid analgesic approved for children.

Available forms

Oxycodone is available in a variety of formulations for by mouth or under the tongue:

  • Immediate-release oxycodone (OxyFast, OxyIR, OxyNorm, Roxicodone)
  • Controlled-release oxycodone (OxyContin, Xtampza ER) – 10-12-hour duration
  • Oxycodone tamper-resistant (OxyContin OTR)
  • Immediate-release oxycodone with paracetamol (acetaminophen) (Percocet, Endocet, Roxicet, Tylox)
  • Immediate-release oxycodone with aspirin (Endodan, Oxycodan, Percodan, Roxiprin)
  • Immediate-release oxycodone with ibuprofen (Combunox)
  • Controlled-release oxycodone with naloxone (Targin, Targiniq, Targinact) – 10-12-hour duration
  • Controlled-release oxycodone with naltrexone (Troxyca) – 10-12-hour duration

In the U.S., oxycodone is only approved for use by mouth, available as tablets and oral solutions. Parenteral formulations of oxycodone (brand name OxyNorm) are also available in other parts of the world however and are widely used in Europe. In Spain, the Netherlands and the United Kingdom, oxycodone is approved for intravenous (IV) and intramuscular (IM) use. When first introduced in Germany during World War I, both IV and IM administrations of oxycodone were commonly used for postoperative pain management of Central Powers soldiers

Side effects

Main side effects of oxycodone

Two tablets (10 mg) of oxycodone and safety blisters

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. Most side effects generally become less intense over time, although issues related to constipation are likely to continue for the duration of use. The oxycodone in combination with naloxone in managed-release tablets has been formulated to both deter abuse and reduce “opioid-induced constipation”.

Dependence and withdrawal

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.

Hormone levels

As with other opioids, chronic use of oxycodone (particularly with higher doses) often causes concurrent hypogonadism (low sex hormone levels