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Oxycodone

Oxycodone is synthesized from thebaine. Like morphine and hydromorphone, oxycodone is used as an analgesic.

It is effective orally and is marketed alone in 10, 20, 40, 80, and 160 mg controlled-release tablets (OxyContin), or 5 mg immediate-release capsules (OxyIR®), or in combination products with aspirin (Percodan®) or acetaminophen (Percocet®) for the relief of pain. All oxycodone products are in Schedule II. Oxycodone is abused orally or the tablets are crushed and sniffed or dissolved in water and injected. The use of oxycodone has increased significantly. In 1990, nearly three tons of oxycodone were manufactured in the United States. In 2000, about 47 tons were manufactured. In 2011, 105 tons were manufactured.

Oxycodone abuse has been a continuing problem in the United States since the early 1960’s. In passing the Controlled Substances Act of 1970, Congress placed oxycodone in Schedule II (CII). In spite of its CII status, oxycodone continued to be abused. The abuse of the sustained-release formulation of oxycodone has escalated over the years.

Drug abuse treatment centers, law enforcement personnel, and health care professionals have reported a dramatic increase in the abuse of these sustained release products in Maine, Virginia, West Virginia, Ohio, Kentucky and Maryland. Recently, abuse has spread to other states such as Pennsylvania and Florida. The estimated number of emergency department (ED) episodes involving oxycodone were stable from 1990 through 1996. However, the number of ED episodes more than tripled from 1996 to 2000: 3,190 episodes in 1996 to 10,825 in 2000. By 2009, the number of emergency department visits due to oxycodone had increased to 175,949.

Licit Uses

Oxycodone is an effective analgesic for mild to moderate pain control, chronic pain syndromes, and for the treatment of terminal cancer pain. Five mg of oxycodone is equivalent to 30 mg of codeine when administered orally. Oxycodone and morphine are equipotent for pain control in the normal population; 10 mg of orally-administered oxycodone is equivalent to 10 mg of subcutaneously administered morphine. Oxycodone is considered to be similar to morphine, in all respects, including its abuse and dependence liabilities. Oxycodone in dosages of 5 to 10 mg in combination with acetaminophen or aspirin are abused orally. High dose single entity sustained release formulations containing 10 to 80 mg of oxycodone are abused by crushing or chewing the tablet and then swallowing, snorting or injecting the drug.

Chemistry/Pharmacology

Oxycodone is a semisynthetic opioid structurally related to codeine and is approximately equipotent to morphine in producing opiate-like effects. The first report that oxycodone, sold under the brand name Eukodal, produced a “striking euphoria” and habituation symptoms was published in Germany in the 1920’s. While oxycodone is metabolized by the liver to oxymorphone, the physiological and behavioral effects are not related to, nor dependent on, the formation of this metabolic by-product.

Oxycodone will test positive for an opiate in the available field test kits.

Illicit Uses

Oxycodone is abused for its opiate-like effects. In addition to its equipotency to morphine in analgesic effects, it is also equipotent to morphine in relieving abstinence symptoms from chronic opiate (heroin, morphine) administration. For this reason, it is often used to alleviate or prevent the onset of opiate withdrawal by street users of heroin and methadone. In early studies by the Addiction Research Center in Lexington, Kentucky in the 1960’s, it was discovered that the subjective and physiological effects of oxycodone were greater than an equivalent dose of morphine in opiate substance abusers. Many dosage forms are available. Oxycodone’s behavioral effects can last up to 5 hours. The drug is most often administered orally. The sustained-release formula has a longer duration of action (8-12 hours). A recent study comparing controlled released products containing oxycodone (Oxycontin) and morphine (MS Contin) reported that Oxycontin was twice as potent as MS Contin.

As with most opiates, the adverse effects of oxycodone abuse are dependence and tolerance development. Oxycodone’s co-formulation with acetaminophen has also increased the likelihood of acetaminophen-induced hepatic (liver) necrosis with chronic dosing. Its availability in sustained release formulations has increased the dosage forms from 10 to 160 mg per tablet making it more attractive than oxycodone to opiate abusers and doctor-shoppers. The original idea of polymer-formulations of oxycodone was to reduce the likelihood of misuse with high dose formulations. Opiate abusers quickly learned the ease of extraction of the molecule from the polymer formula and have been injecting or snorting the crushed and/or dissolved tablets because of its higher dosage formulations.

User Population

Every age-group has been affected by the relative ease of oxycodone availability and the perceived safety of these products by professionals. Sometimes seen as a “white-collar” addiction, oxycodone abuse has increased among all ethnic and economic groups.

Illicit Distribution

Oxycodone-containing products are in tablet, capsule and liquid forms. A variety of colors, markings, and packaging are available.

The major source of oxycodone to the street has been through forged prescriptions, professional diversion through unscrupulous pharmacists, doctors, and dentists, “doctor-shopping,” and large-scale thefts.