General Information

Oxycodone moleculeOxycodone is an opioid derived from an alkaloid of opium, thebaine. It was first synthesized in the early twentieth century, some sources indicating the year 1916. We do know that oxycodone has been available in Europe for oral and intravenous use since 1917, but some historians believe it was one year earlier. The drug was released in the United States during the 1950s.[1] Some prescription drugs containing oxycodone include Percocet, Percodan, Roxicet, OxyContin, and Roxicodone. The effects most sought after are pain relief, euphoria, reduction in anxiety, and sedation. Other side effects can include constipation, and dizziness. Many users report feeling itchy after ingesting oxycodone; this results from the release of histamine in the brain.

In 1995, OxyContin, which is manufactured by Purdue and allows up to 12 hours of continuous pain relief, was approved for sale. OxyContin is available in 10, 20, 40, and 80 milligram pills. When it was first released on the market, a 160 milligram pill was manufactured, but Purdue eventually pulled it off the market. On the streets OxyContin is referred to as OC, hillbilly heroin, oxy, jawns, jimmies, "big guys" (refers to the 80 milligram pills), itchies, "Ocean City," or "Orange County." The growing OxyContin problem has become an epidemic in many parts of the United States. In southeastern Pennsylvania, users have been witnessed paying $80 for one 80 mg OxyContin pill. As habits grow, many people switch to heroin because of its availability and attractively lower prices.

FAST FACTS:

  • Oxycodone is not tested for in a standard drug screening; however, at very high doses it may cause a positive for opiates. It is typically in the urine for 3-4 days. Very rarely is it a part of extended drug screening.
  • Oxycodone is addicting, and causes tolerance. Moderate use is hard to maintain with any opiate. Most people who say they will "only use once a week" end up using more often than they want to. Using opiates on a regular basis will cause a physical and possibly mental dependency. After using oxycodone for a few days, a larger dose is often needed to achieve the same effects.
  • Those who have never done opiates or without a tolerance need to exercise extreme caution when dosing. It is not recommended that anyone take oxycodone without a proper prescription. Users beware, what one person can tolerate may kill another person.

Chemical Names. (5a)-4,5-epoxy-14-hydroxy-3-methoxy-17- methylmorphinan-6-one.
Classification. Opioid.
Primary Uses. Analgesia.
Other Names. OxyContin, Percocet, Percodan, Roxicodone, Roxicet, Endocet.
Urinalysis Detection Time. 3-4 days.

 

Pharmacology and Pharmacokinetics

Administration

Route
Bioavailability (Median)
Intranasal [2]
46-47%
Oral [3]
60-87%
Rectal
60-87%

 

Law

Schedule IIIn the United States, oxycodone is a Schedule II substance, making it illegal to use/possess without a prescription. Schedule II substances, such as dextroamphetamine, morphine, and cocaine, meet the following criteria according to the Controlled Substances Act:

  1. The drug or other substance has a high potential for abuse.
  2. The drug or other substance has a currently accepted medical use in treatment in the United States (or) a currently accepted medical use with severe restrictions.
  3. Abuse of the drug may lead to severe psychological or physical dependence.

 

Side Effects

  • Pain relief
  • Euphoria/dysphoria
  • Mood changes
  • Reduced anxiety
  • Sedation
  • Itching
  • Nausea/vomiting
  • Decreased libido (sex drive)
  • Constipation
  • Facial flushing
  • Vertigo

 

Withdrawal

Oxycodone, in any form, is highly addictive, and many users eventually become mentally and physically dependent. Withdrawal typically begins within 24-36 hours after the last dose, though it can start sooner for chronic users, and peaks in intensity around 72-96 hours. Withdrawal symptoms can include gooseflesh, restless legs/arms, anxiety, nausea, vomiting, depression, muscle aches, insomnia, diarrhea, headache, and dilated pupils.

 

Additional Information

 

Books

 

Sources

[1] Drew Pinsky, M.D., Marvin D. Seppala, M.D., Robert J. Meyers, Ph.D., John Gardin, Ph.D., William White, M.A., Stephanie Brown, Ph.D. When Painkillers Become Dangerous. Center City, Minnesota: Hazelden, 2004. pg 6.
[2] Takala A, Kaasalainen V, Seppala T, Kalso E, Olkkola KT. Pharmacokinetic comparison of intravenous and intranasal administration of oxycodone. Entrez PubMed [9062618]. Acta Anaesthesiol Scand. 1997 Feb;41(2):309-12. [link] Accessed: October 25, 2006.
[3] Oxycodone HCl: Clinical Pharmacology. RxList. 2006. [link] Accessed: October 25, 2006.

 

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