Oxycontin
Q.) What is OxyContin?
A.) OxyContin, approved by the FDA
in 1995, an opium derivative, which is the same active ingredient in Percodan
and Percocet. OxyContin is intended for use by terminal cancer patients and
chronic pain sufferers. It has been linked to at least 120 overdose deaths
nationwide. OxyContin (oxycodone hydrochloride controlled-release) tablets are
an opioid analgesic supplied in 10 mg, 20 mg,40 mg, and 80 mg tablet strengths
for oral administration. The tablet strengths describe the amount of oxycodone
per tablet as the hydrochloride salt. The structural formula for oxycodone
hydrochloride is as follows: The chemical formula is 4,
5-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one hydrochloride.
Oxycodone is a very strong narcotic
pain reliever similar to morphine. OxyContin is designed so that the oxycodone
is slowly released over time, allowing it to be used twice daily. You should
never break, chew, or crush the OxyContin tablet since this causes a large
amount of oxycodone to be released from the tablet all at once, potentially
resulting in a dangerous or fatal drug overdose.
Oxycodone is a white, odorless
crystalline powder derived from the opium alkaloid. Oxycodone hydrochloride
dissolves in water (1 g in 6 to 7 mL). It is slightly soluble in alcohol
(octanol water partition coefficient 0.7). The tablets contain the following
inactive ingredients: ammonium methacrylate copolymer, hydroxypropyl
methylcellulose, lactose, magnesium stearate, povidone, red iron oxide (20 mg
strength tablet only), stearyl alcohol, talc, titanium dioxide, triacetin,
yellow iron oxide (40 mg strength tablet only), and other ingredients.
OxyContin is an opiate agonist.
Opiate agonists provide pain relief by acting on opioid receptors in the spinal
cord, brain, and possibly in the tissues directly. Opioids, natural or
synthetic classes of drugs that act like morphine, are the most effective pain
relievers available. Oxycodone is manufactured by modifying thebaine, an
alkaloid found in opium. Oxycodone has a high abuse potential.
Oxycodone is a central nervous
system depressant. Oxycodone's action appears to work through stimulating the
opioid receptors found in the central nervous system that activate responses
ranging from analgesia to respiratory depression to euphoria. People who take
the drug repeatedly can develop a tolerance or resistance to the drug's
effects. Thus, a cancer patient can take a dose of oxycodone on a regular basis
that would be fatal in a person never exposed to oxycodone or another opioid.
Most individuals who abuse oxycodone seek to gain the euphoric effects,
mitigate pain, and avoid withdrawal symptoms associated with oxycodone or
heroin abstinence.
Q.) How is OxyContin used?
A.) The power painkiller OxyContin
is being abused by more and more people across the nation. The heroin-like
effects of the drug attract both legitimate and illegitimate users.
When used properly, OxyContin
contains a time-release mechanism that spreads the release of the drug over a
12-hour period. The time-release mechanism can be circumvented by crushing the
tablet and the drug can be used in one of the following ways:
…
The tablets can be chewed
…
The tablets can be crushed, then snorted like
cocaine
…
The
tablets can be crushed, dissolved in water, then injected like heroin
OxyContin abuse is spreading for a
variety of reasons. First, the elevated opiate dosage makes it highly
addictive. Second, in contrast to drugs such as cocaine or heroin that can be
laced with other substances, with OxyContin you know how much of the drug you
are getting; the dosage is consistent, so it is a dependable high. Finally,
OxyContin is covered by most health insurance plans, so it is significantly
cheaper than street drugs. (OxyContin has been referred to as "hillbilly heroin"
or "the poor man's heroin.")
Q.) What are the effects of
OxyContin?
A.) Respiratory depression is the
chief hazard from all opioid usage. Respiratory depression occurs most frequently
in elderly or debilitated patients, usually following large initial doses in
non-tolerant patients, or when opioids are given in conjunction with other
agents that depress respiration. Common opioid side effects are constipation,
nausea, sedation, dizziness, vomiting, headache, dry mouth, sweating, and
weakness.
Oxycodone should be used with
extreme caution in patients with significant chronic obstructive pulmonary
disease and in patients having a substantially decreased respiratory reserve,
hypoxia, hypercapnia, or preexisting respiratory depression. In such patients,
even usual therapeutic doses of oxycodone may decrease respiratory drive to the
point of apnea. In these patients alternative non-opioid analgesics should be
considered, and opioids should be employed only under careful medical
supervision at the lowest effective dose. Oxycodone causes miosis, even in
total darkness. Pinpoint pupils are a sign of opioid overdose but are not
pathognomonic. Marked mydriasis rather than miosis may be seen due to hypoxia
in overdose situations.
Gastrointestinal Tract and Other
Smooth Muscle
Oxycodone causes a reduction in motility associated with an increase in smooth
muscle tone in the antrum of the stomach and duodenum. Digestion of food in the
small intestine is delayed and propulsive contractions are decreased.
Propulsive peristaltic waves in the colon are decreased, while tone may be
increased to the point of spasm resulting in constipation. Other opioid-induced
effects may include a reduction in gastric, biliary and pancreatic secretions,
spasm of sphincter of Oddi, and transient elevations in serum amylase.
Cardiovascular System
Oxycodone may produce release of histamine with or without associated
peripheral vasodilation. Manifestations of histamine release and/or peripheral
vasodilation may include pruritus, flushing, red eyes, sweating, and/or
orthostatic hypotension.
Concentration--Efficacy
Relationships (Pharmacodynamics)
Studies in normal volunteers and patients reveal predictable relationships between
oxycodone dosage and plasma oxycodone concentrations, as well as between
concentration and certain expected opioid effects. In normal volunteers these
include pupillary constriction, sedation and overall "drug effect"
and in patients, analgesia and feelings of "relaxation." In
non-tolerant patients, analgesia is not usually seen at a plasma oxycodone
concentration of less than 5&endash;10 ng/mL.
As with all opioids, the minimum
effective plasma concentration for analgesia will vary widely among patients,
especially among patients who have been previously treated with potent agonist
opioids. As a result, patients need to be treated with individualized titration
of dosage to the desired effect. The minimum effective analgesic concentration
of oxycodone for any individual patient may increase with repeated dosing due
to an increase in pain and/or the development of tolerance.
Q.) Is OxyContin addictive?
A.) The powerful prescription pain
reliever has become a hot new street drug that has resulted in more than 120
deaths nationwide. It will give you a high much like HIGH GRADE heroin but with
worse consequences. 5mg of OXY has has as much active ingredient (oxycodone) as
One percocet. So chewing/snorting a 40mg OXY is like taking 8 percocets at once
or a 80mg Oxy is like taking 16 percocets all at once. Overdose Symptoms: Slow
breathing, seizures, dizziness, weakness, loss of consciousness, coma,
confusion, tiredness, cold and clammy skin, and small pupils.
OxyContin should be used to fight
extreme pain. Doctors commonly prescribe it to cancer patients as an
alternative to morphine. The drug is addictive, expensive, and when misused, it
can be lethal. OxyContin abuse is becoming an epidemic in several rural states.
Physical dependence, which is
sometimes unavoidable, develops when an individual is exposed to a drug at a
high enough dose for long enough that the body adapts and develops a tolerance
for the drug. This means that higher doses are needed to achieve a drug's
original effects. If the patient stops taking the drug, withdrawal will occur.
Just like heroin it is almost impossible to do alone as the withdrawal symptoms
of OxyContin are worse than heroin and last longer. Professional help from a
heroin detox center is the best and safest way to do this but there is NO
painless way.
Drug craving is the result of the
drug's imprinting in the memory of a pleasant association of euphoria with the
drug. The subconscious memory then motivates the individual to seek this drug
because of the false imprint. The brain, in effect, has been trained that using
the drug is the fastest way to feel good. This learning process then produces a
new appetite or drive to seek the drug which we call craving. This craving is
most often activated by, a) memory of pleasure, b) when we feel bad and have a
habit of using the drug to rapidly feel good, c) when we are in a situation
with people, places and activities in which a previous habit pattern of drug
use has been established.
Prescription drugs, like other
addictive drugs, are able to short-circuit your survival system by artificially
stimulating the reward center, or pleasure areas in your brain, without
anything beneficial happening to your body. As this happens, it leads to
increased confidence in the drug, and less confidence in the normal rewards of
life. This first happens on a physical level. Then, it affects you
psychologically. The big drug lie results in decreased interest in other
aspects of life, as you increase your reliance and interest in the drug.
People, places and activities involved with using drugs become more important.
People, places and activities or lifestyles that worked through your normal
reward system, before using the drug, become less important to you. After a
while, a heavy drug user will actually resent people, places, and activities
that do not fit in with that drug use.
Addictive drugs mimic the action
of chemicals your brain produces to send messages of pleasure to your brain's
reward center. They produce an artificial feeling of pleasure. Most addictive
drugs are able to produce pleasurable effects by chemically acting like certain
normal brain messenger chemicals, which produce positive feelings in response
to signals from the brain.
The result is a dependence on the
immediate, fast, predictable drug which, at the same time, short circuits
interests in and the motivation to make life's normal rewards work. More and
more confidence is placed in the drug while other survival feelings are ignored
and bypassed. The result of this addiction cycle is a lack of concern for, and
confidence in, other areas of life.
Oxycodone hydrochloride
Oxycodone hydrochloride (Roxicodone)
Oxycodone hydrochloride
(ox-ee-KOH-dohn)
Pregnancy Category: C 
Classification: Narcotic
analgesic, morphine type
See Also: See also Narcotic
Analgesics.
Action/Kinetics:
Semisynthetic opiate causing mild sedation and little or no antitussive effect.
Most effective in relieving acute pain. Onset: 15-30 min. Peak
effect: 60 min. Duration: 4-6 hr. t1/2: 3.2 hr for immediate-release product and 4.5 hr for
extended-release. Dependence liability is moderate. Oxycodone terephthalate is
available but only in combination with aspirin (e.g., Percodan) or
acetaminophen.
Uses: Moderate to severe
pain. The extended-release product (OxyContin) is indicated for moderate to
severe pain, including that due to cancer, injuries, arthritis, lower back
problems, and other musculoskeletal conditions that require treatment for more
than a few days. NOTE: The 80 mg extended-release tablet is only for use
in opiate-dependent clients.
Additional Contraindications:
Use in hypercarbia, paralytic ileus, children or during labor. Clients with
gastric distress, such as colitis or gastric or duodenal ulcer, and clients who
have glaucoma should not receive Percodan, which also contains aspirin.
Special Concerns: OxyContin 80
mg controlled release is indicated only for opiate-tolerant clients.
Additional Drug Interactions:
Use with protease inhibitors 
CNS and
respiratory depression.
How Supplied: Capsule:
5 mg; Solution, Concentrate: 20 mg/mL; Solution, Oral: 5 mg/5 mL;
Tablet: 5 mg; Tablet, Extended Release: 10 mg, 20 mg, 40 mg, 80
mg
Dosage
ïCapsule,
Oral Concentrate, Oral Solution, Tablet, Controlled Release Tablet Analgesia.
Adults: 10-30 mg q 4 hr (5 mg q 6 hr for OxyIR and OxyFAST, as needed).
Individualize dose.