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Drugs
and Chemicals of Concern > Oxycodone
> Summary
OXYCODONE
(Trade Names: Tylox ®,
Percodan®, OxyContin®)
September 2007 DEA/OD/ODE
Introduction:
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.
Licit Uses:
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™).
Chemistry/Pharmacology:
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%).
User Population:
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.
Illicit Distribution:
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.
Control Status:
Oxycodone products are in schedule II of
the federal Controlled Substances Act of 1970.
Comments and additional information are welcomed by the Drug and Chemical
Evaluation Section, FAX 202-353-1263; telephone 202-307-7183.
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