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Oxycodone

Oxycodone is a very powerful and potentially addictive opioid analgesic medication synthesized from thebaine. more...

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It is effective orally and is marketed in combination with aspirin (Percodan, Endodan, Roxiprin) or acetaminophen (Percocet, Endocet, Roxicet, Tylox) for the relief of pain. More recently, ibuprofen has been added to oxycodone (Combunox). It is also sold in a sustained-release form by Purdue Pharma under the trade name OxyContin as well as generic equivalents, and instant-release forms OxyIR, OxyNorm and Percolone . OxyContin is available in 10, 20, 40, and 80 mg tablets, and, due to its sustained-release mechanism, is effective for eight to twelve hours. (The 160 mg formulation was discontinued in May 2001.) OxyNorm is available in 5, 10, and 20 mg capsules and tablets; also as a 1 mg/1 ml liquid in 250 mg bottles and as a 10 mg/1 ml concentrated liquid in 100 mg bottles.

In the United States, oxycodone is a Schedule II controlled substance both as a single agent and in combination products containing acetaminophen or aspirin.

Chemical structure

The chemical structure of oxycodone is the methylether of oxymorphone: 3-Methyl-oxymorphone. It could be also described as 14-Hydroxy-Codeinone. It is principally supplied as its hydrochloride salt: oxycodone hydrochloride

Medical use

Oxycodone is one of the most powerful medications for pain control that can be taken orally. Percocet tablets (oxycodone with acetaminophen) are routinely prescribed for post-operative pain control. Oxycodone is also used in treatment of moderate to severe chronic pain. When used at recommended doses for relatively short periods (several weeks), it provides effective pain control with manageable side effects.

Nausea, constipation, lightheadedness, rash, dizziness, and emotional mood disorders are the most frequently reported side effects.

Tolerance and physical dependence occurs after several months of treatment, with larger doses being required to achieve the same degree of analgesia.

According to the DEA and the companies that manufacture the drug, psychological addiction as a result of medical use is extremely rare. However, there are several lawsuits underway brought by plaintiffs who claim that they became addicted to the drug as a result of medical use.

Abuse

The introduction of OxyContin in 1995 resulted in increasing patterns of abuse. Unlike Percocet, whose potential for abuse is limited by the presence of acetaminophen, OxyContin contains only oxycodone and inert filler. Abusers crush the tablets to defeat the time-release mechanism, then either ingest the resulting powder orally, intranasally, via intravenous/intramuscular/subcutis injection, or rectally to achieve rapid absorption into the bloodstream. The vast majority of OxyContin-related deaths are attributed to ingesting substantial quantities of OxyContin or ingesting OxyContin along with another depressant of the central nervous system such as alcohol or benzodiazepines. While high doses of oxycodone can be fatal to an opiate-naïve individual in and of itself, this is (comparatively) rarely the case. It was once felt that "combination" opioids (those that contain one or more additional, non-narcotic ingredients) would be less subject to abuse, since, for example, the amount of acetaminophen present in large overdoses of Percocet would cause stomach upset and liver damage. However, it has been demonstrated that abusers seeking the euphoric "high" are not deterred by these potential side effects or toxicities. Abusers soon discovered that extremely simple methods to separate the ingredients exist, particularly due to the widely disparate solubility of the alkaloids and analgesics in water ("cold water extraction").

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Oxycodone/Oxycontin
From Maine Nurse, 11/1/03

The vast majority of drug abuse deaths involving oxycodone are related to the ingestion of multiple drugs (96.7 percent), not solely oxycodone (3.3 percent), according to an analysis of more than 1,000 deaths published in the March issue of the Journal of Analytical Toxicology.

In Maine, despite anecdotal accounts to the contrary, there has not been a great surge in overdose deaths due to the abuse of Oxycontin. According to the Medical Examiner's office, in the year 2000, of 66 overdose deaths in Maine, nine involved the use of Oxycodone, the drug in Oxycontin. Some of these deaths included multiple drugs and it is impossible to determine that any one of the drugs was the cause of death. Unless the pills are found at the site of death, it is also difficult to determine what oxycodone-coritaining product was used. For example, someone could have Oxycodone, heroin, and methadone all in his blood at the time of death, and the medical examiner could not tell which drug was the cause of death, or whether the person had ingested Oxycontin, or Tylox.

As cited earlier, admissions to substance abuse treatment due to synthetic opiates such as Oxycontin have risen from 232 in 1995, the year Oxycontin was introduced, to 1,299 in state fiscal year 2001. Heroin use has also been on the rise since 1998, nearly doubling in the past three years. As has been feared by some treatment providers and law enforcement officials alike, Oxycontin seems to be a gateway drug to heroin. Opiate addicts have gone from constituting 2% of the treatment population in 1995, to making up 12% of the treatment population in 2001. This is an unprecedented change.

While arrests due to the possession or sale of synthetic opiates have doubled in the past five years, law enforcement officials in some parts of the state say they are also plagued by property and personal crimes related to use of the drug. The Washington County sheriff's office reports an increase of 50% in crime, all due to prescription drug abuse. They have assigned two deputies to work exclusively on drug enforcement. This leaves the work they once performed to be picked up by other officers or to be left undone.

Pharmacy hold-ups have been well publicized. Across the state, desperate drug addicts have broken into pharmacies or committed armed robberies in the middle of the day in order to get specific drugs including Oxycontin and Dilaudid. In some parts of the state, DEA agents spend nearly all of their time on investigating the diversion of legal prescription drugs for illegal purposes, leaving little time to chase down illegal drugs.

Hospital admissions for opiate related illness tripled between 1996 and 2000. In contrast, during the same period of time, admissions to the hospital for alcohol related causes remained steady. Maine is not alone in the increase in hospital visits due to opiate misuse. The national Drug Abuse Warning Network (DAWN) reports a 108% increase in emergency room mentions of oxycodone in the period from 1998 - 2000 (See Figure 4). Hydrocodone, the drug found in Dilaudid, has also caused a dramatic increase in Emergency Room visits. (from www.state.me.us/bds/osa/pubs/osa/2002/oxy/part2.htm)

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