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Chapter 13
Opioids
© 2006 McGraw-Hill Higher Education. All rights reserved.
Narcotics Are…
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The term narcotic currently refers to
naturally occurring substances derived
from the opium poppy and their synthetic
substitutes.
These drugs are referred to as the opioid
(or opiate) narcotics because of their
association with opium.
© 2006 McGraw-Hill Higher Education. All rights reserved.
Narcotics Are…
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For the most part, the opioid narcotics
possess abuse potential, but they also
have important clinical value (analgesic,
antitussive).
The term narcotic has been used to label
many substances, from opium to
marijuana to cocaine.
© 2006 McGraw-Hill Higher Education. All rights reserved.
History
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From an annual plant
Egyptian and Greek cultures
India and China
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Opioids dependence
Writers and Opium
Opium Wars
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Started by outside incidents
Britain given the island of Hong Kong for
winning
© 2006 McGraw-Hill Higher Education. All rights reserved.
Side Effects
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The principle side effects of the opioid
narcotics, besides their abuse potential,
include:
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Drowsiness
Respiratory depression
Nausea, vomiting, and constipation
Inability to urinate
Drop in blood pressure
© 2006 McGraw-Hill Higher Education. All rights reserved.
Pharmacological Effects
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The most common clinical use of the opioid
narcotics is as analgesics to relieve pain.
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The opioid narcotics relieve pain by activating the
same group of receptors that are controlled by the
endogenous substances called endorphins.
Activation of opioid receptors blocks the
transmission of pain through the spinal cord or
brain stem.
© 2006 McGraw-Hill Higher Education. All rights reserved.
Pharmacological Effects
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Morphine is a particularly potent pain reliever
and is often used as the analgesic standard by
which other narcotics are compared.
With continual use, tolerance to the analgesic
effects of morphine and other narcotics
develops.
Physicians frequently under-prescribe narcotics,
because of fear of causing narcotic addiction.
© 2006 McGraw-Hill Higher Education. All rights reserved.
Abuse, Tolerance, Dependence,
and Withdrawal
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All the opioid narcotic agents that
activate opioid receptors have abuse
potential and are classified as schedule
drugs.
Tolerance begins with the first dose of a
narcotic, but does not become clinically
evident until 2 to 3 weeks of frequent
use.
© 2006 McGraw-Hill Higher Education. All rights reserved.
Abuse, Tolerance, Dependence,
and Withdrawal
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Tolerance occurs most rapidly with high doses
given in short intervals
Doses can be increased as much as 35 times in
order to regain the narcotic effect
Physical dependence invariably accompanies
severe tolerance
Psychological dependence can also develop
with continual narcotic use
© 2006 McGraw-Hill Higher Education. All rights reserved.
Morphine
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1806 morphine was discovered
10 times as potent as opium
Hypodermic syringe and war time
medicine
“Soldier’s disease”
© 2006 McGraw-Hill Higher Education. All rights reserved.
Heroin
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Heroin is classified as a Schedule I drug
Heroin is the most widely abused illegal
drug in European and Far Eastern
countries
Until 15 years ago, Heroin was illicitly used
more than any other drug of abuse in the
U.S. (except for marijuana)
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What was it replaced by?
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Cocaine
© 2006 McGraw-Hill Higher Education. All rights reserved.
Methods of Administration
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Sniffing the powder
Injecting it into a muscle (intramuscular)
Smoked
Mainlining (intravenous injection)
© 2006 McGraw-Hill Higher Education. All rights reserved.
Heroin Addicts And AIDS
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Over 50% of IV heroin users have been
exposed to the AIDS virus
© 2006 McGraw-Hill Higher Education. All rights reserved.
Withdrawal Symptoms
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A single “shot” of heroin lasts 4 to 6 hours
After the effects of the heroin wear off, the addict
has only a few hours in which to find the next
dose before severe withdrawal symptoms begin
Withdrawal symptoms:
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runny nose, tears,
minor stomach cramps, loss of appetite, vomiting,
diarrhea, abdominal cramps,
chills, fever, aching bones, and muscle spasms
© 2006 McGraw-Hill Higher Education. All rights reserved.
Treatment
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Methadone, LAAM or buprenorphine are
frequently used to help narcotic addicts
Oral methadone relieves the withdrawal
symptoms
Methadone can cause psychological and
physical dependence
Buprenorphine
© 2006 McGraw-Hill Higher Education. All rights reserved.
Other Narcotics
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Morphine
Methadone
Fentanyl
Hydromorphone
Meperidine
© 2006 McGraw-Hill Higher Education. All rights reserved.
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MPTP
Codeine
Pentazocine
Propoxyphene