DESCRIPTION / DEFINITIONS: OxyContin® (oxycodone hydrochloride controlled-release) is a specific formulation of the Schedule II narcotic, oxycodone.
ABUSE : OxyContin is an opioid agonist and a Schedule II controlled substance with an abuse liability similar to morphine.
ADDICTION / DEPENDENCE: Oxycontin is very addictive and in some people is has been known to cause physical dependence after just 3 days.
SIDE EFFECTS: Respiratory depression (see list below).
WITHDRAWAL SYMPTOMS: Nausea, vomiting, diarrhea (see list below).
TREATMENT: Medical detoxification.
OxyContin® (oxycodone hydrochloride controlled-release) is a specific formulation of the Schedule II narcotic, oxycodone. OxyContin has a time-released coating that, if taken correctly, is intended to allow one pill’s effect to last longer. According to its label, “Oxycodone is a pure agonist opioid whose principal therapeutic action is analgesia.” In addition, its label says, “The precise mechanism of the analgesic action is unknown.”
According to the DEA, a Schedule II narcotic means that:
- The drug or other substance has a high potential for abuse.
- 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.
- Abuse of the drug or other substances may lead to severe psychological or physical dependence.
The Encarta Dictionary defines:
- therapeutic as “Used in treating disease”
- narcotic as, “A typically addictive drug, especially one derived from opium, that may produce effects ranging from pain relief and sleep to stupor, coma, and convulsions”
- analgesic as, “A type of medication that alleviates pain without loss of consciousness.” It is interesting to point out that the word analgesia is derived from the Greek “an” meaning without and “algesis” meaning sense of pain. Analgesic drugs are intended to take away the sense of pain but not to address the cause of the pain.
- an agonist is something that stimulates or produces an effect. Agonist is derived from the Late Latin agnista which means contender, which is derived from the Greek agonists which also means contestant which came from agon meaning contest.
OxyContin is an opioid agonist and a Schedule II controlled substance with an abuse liability similar to morphine.
HALF LIFE AND METABOLISM
The biological half-life of a substance is the time it takes for a drug to lose half of its pharmacologic activity. This is significant because it affects how soon withdrawal symptoms may appear.
The half life of OxyContin is 6.5 hours.
Oxycontin is mainly metabolized through the P450 pathway in the liver and the enzyme primarily handling the metabolism is the CYP2D6 enzyme. The CYP enzymes are the major enzymes involved in drug metabolism, and since many drugs may increase or decrease the activity of various CYP isozymes, this is a major source of adverse drug interactions, since changes in CYP enzyme activity may affect the metabolism and clearance of various drugs. For example, if one drug inhibits the CYP-mediated metabolism of another drug, the second drug may accumulate within the body to toxic levels, possibly causing an overdose.
BLACK BOX WARNING
The Food and Drug Administration (FDA) has decided that some drugs pose very serious risks, and require these drugs to carry what is called a “black box warning”.
OxyContin has this black box warning:
WARNING:OxyContin is an opioid agonist and a Schedule II controlled substance with an abuse liability similar to morphine.
Oxycodone can be abused in a manner similar to other opioid agonists, legal or illicit. This should be considered when prescribing or dispensing OxyContin in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse, or diversion.
OxyContin Tablets are a controlled-release oral formulation of oxycodone hydrochloride indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time.
OxyContin Tablets are NOT intended for use as a prn (take when needed) analgesic.
OxyContin 80 mg and 160 mg Tablets ARE FOR USE IN OPIOID-TOLERANT PATIENTS ONLY. These tablet strengths may cause fatal respiratory depression when administered to patients not previously exposed to opioids.
OxyContin TABLETS ARE TO BE SWALLOWED WHOLE AND ARE NOT TO BE BROKEN, CHEWED, OR CRUSHED. TAKING BROKEN, CHEWED, OR CRUSHED OxyContin TABLETS LEADS TO RAPID RELEASE AND ABSORPTION OF A POTENTIALLY FATAL DOSE OF OXYCODONE.
OxyContin® Tablets are available in 10 mg, 20 mg, 40 mg, 80 mg, and 160 mg tablet strengths for oral administration.
The following information is taken from the OxyContin label.
The safety of OxyContin® was evaluated in double-blind clinical trials involving 713 patients with moderate to severe pain of various etiologies. In open-label studies of cancer pain, 187 patients received OxyContin in total daily doses ranging from 20 mg to 640 mg per day. The average total daily dose was approximately 105 mg per day.
The following adverse experiences were reported in OxyContin®-treated patients:
Opioid-induced hyperalgesia: This is a condition where the opioids actually make the pain receptors more sensitive and, therefore, the pain greater. A person with this condition is required to take more and more of the opioid to try to address the pain but finds that the pain actually increases.
OxyContin is a highly addictive drug. Users of OxyContin for a time are likely to become either dependent on or addicted to the drug. If someone is dependent on a drug they will experience withdrawal symptoms. They normally continue taking the drug because they don’t want to experience withdrawal symptoms.
Here are some of the OxyContin withdrawal symptoms: