OXYCODONE

(Trade Names: Tylox®, Percodan®, OxyContin®)

Oxycodone is a schedule II narcotic analgesic and is widely used in clinical medicine. It is marketed either alone as controlled release (OxyContin^®) and immediate release formulations (OxyIR^®, OxyFast^®), or in combination with other nonnarcotic analgesics such as aspirin (Percodan^®) or acetaminophen (Percocet^®). The introduction in 1996 of OxyContin^®, commonly known on the street as OC, OX, Oxy, Oxycotton, Hillbilly heroin, and kicker, led to a marked escalation of its abuse as reported by drug abuse treatment centers, law enforcement personnel, and health care professionals. Although the diversion and abuse of OxyContin^® appeared initially in the eastern U.S., it has now spread to the western U.S. including Alaska and Hawaii. Oxycodone-related adverse health effects increased markedly in recent years. In 2004, Food and Drug Administration (FDA) approved generic forms of controlled release oxycodone products for marketing.

Products containing oxycodone in combination with aspirin or acetaminophen are used for the relief of moderate to moderately severe pain. Oxycodone controlled-release tablets are prescribed for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time. Oxycodone is a widely prescribed in the U.S. Prescriptions for OxyContin^® (1.57 million) and similar controlled release products accounted for 7.6 million of the 42.3 million total prescriptions for oxycodone in 2006 (IMS Health^™).

Oxycodone, [4,5-epoxy-14-hydroxy-3-methoxy-17-methyl-morphinan-6-one, dihydrohydroxycodeinone] is a semi-synthetic opioid agonist derived from thebaine, a constituent of opium. Oxycodone will test positive for an opiate in the available field test kits. Pharmacology of oxycodone is essentially similar to that of morphine, in all respects, including its abuse and dependence liabilities. Pharmacological effects include analgesia, sedation, euphoria, feelings of relaxation, respiratory depression, constipation, papillary constriction, and cough suppression. A 10 mg dose of orally-administered oxycodone is equivalent to a 10 mg dose of subcutaneously administered morphine as an analgesic in the normal population. Oxycodone’s behavioral effects can last up to 5 hours. The drug is most often administered orally. The controlled-release product, OxyContin^®, has a longer duration of action (8-12 hours). As with most opiates, oxycodone abuse may lead to dependence and tolerance. Acute overdose of oxycodone can produce severe respiratory depression, skeletal muscle flaccidity, cold and clammy skin, reduction in blood pressure and heart rate, coma, respiratory arrest, and death.

Illicit Uses:

Oxycodone abuse has been a continuing problem in the U.S. since the early 1960s. Oxycodone is abused for its euphoric effects. It is 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. The large amount of oxycodone (10 to 80 mg) present in controlled release formulations (OxyContin^®) renders these products highly attractive to opioid abusers and doctor-shoppers. They are abused either as intact tablets or by crushing or chewing the tablet and then swallowing, snorting or injecting. Products containing oxycodone in combination with acetaminophen or aspirin are abused orally. Acetaminophen present in the combination products poses an additional risk of liver toxicity upon chronic abuse. According to the Florida Department of Law Enforcement, oxycodone was found in 5.6% (716) of the total drug-related deaths in Florida in 2005. Based on the toxicology reports, oxycodone was cited as a causative drug in 340 deaths. The manner of oxycodone deaths cited included accidental (65%), suicide (16%), natural (13%) and undetermined (4%).

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

Oxycodone-containing products are in tablet, capsule, and liquid forms. A variety of colors, markings, and packaging are available. The main sources of oxycodone on the street have been through forged prescriptions, professional diversion through unscrupulous pharmacists, doctors, and dentists, "doctor-shopping," armed robberies, and night break-ins of pharmacies and nursing homes. The diversion and abuse of OxyContin^® has become a major public health problem in recent years. In 2006, 4.1 million people aged 12 or older used OxyContin^® for nonmedical use at least once during their life time (National Survey on Drug Use and Health, 2006). According to reports from DEA field offices, oxycodone products sell at an average price of $1 per milligram, the 40 mg OxyContin® tablet being the most popular. According to the System to Retrieve Information from Drug Evidence, DEA forensic laboratories analyzed 51 items (38 cases) and 607 items (237 cases) of oxycodone in 1998 and 2006, respectively. According to the National Forensic Laboratory Information System, state and local forensic laboratories analyzed 19,056 oxycodone drug items in 2006.

Oxycodone products are in schedule II of the federal Controlled Substances Act of 1970.