This document discusses the history and properties of opioids such as opium, morphine, heroin, and prescription painkillers. It describes how opioids are derived from the opium poppy, their medical uses for pain relief and other conditions, and how tolerance and dependence develop with prolonged use. The document also examines patterns of abuse over time, varying purity levels of heroin, and health risks of opioid use including overdose and infectious diseases.

1. Chapter 13
Opioids
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2. Opioids
 Naturally occurring substances derived
from the opium poppy have a 6,000-year
history of medical use
 Opioids relieve pain and suffering and
have other medicinal uses
 Opioids deliver pleasure and relief from
anxiety, so they also have a long history
of recreational use
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3. Cultivation of Opium
 Papaver somniferum is an annual flowering
plant that grows 3-4 feet high
 Most likely origin is the Middle East
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4. Cultivation of Opium
 Opium is produced and available for collection for only
a few days of the plant’s life
 Opium harvesters use a sharp, clawed tool to make shallow
cuts into the unripe seedpods
 The resinous substance that oozes from the cuts is scraped
and collected
 Raw opium is the substance from which morphine is extracted
and then heroin is derived
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5. History of Opium
 Egypt
 Papyrus (circa 1500 BC) described specific medical uses
 Greece and Rome
 Had an important role in Greek medicines
 Arabic world
 Opium used as a social drug
 Use spread to India and China through trade
 Arab physicians wrote widely about use of opium
preparations
 Europe
 Opium used widely beginning in the sixteenth century
 Physicians developed a preparation called laudanum, a
combination of strained opium and other ingredients
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6. History: Writers and Opium
 Writer Thomas De
Quincey drank
laudanum and wrote
a widely read book
(1823) about life as
an “opium eater”
 Other authors who
used laudanum
included Elizabeth
Barrett Browning
and Samuel Taylor
Coleridge
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7. History: Opium Wars
 1729: Opium smoking outlawed in China, but
smuggling was widespread
 British East India Company was involved in opium
trade, legally in India and illicitly (but indirectly) in China
 Pressure grew and eventually war broke out between
the British and Chinese
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8. Morphine
 1806: Active ingredient in opium
isolated
 10 times as potent as opium
 Named morphium after
Morpheus, the god of dreams
 1832: Another alkaloid of opium
discovered
 Named codeine from the Greek
word for “poppy head”
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9. Morphine
 Medically useful characteristics
 Clinically useful
 Pure chemical
 Known potency
 Use spread due to two developments
 1853: Hypodermic syringe allowed delivery
of morphine directly into the blood
 Widespread use during war provided relief
from pain and dysentery
 Many veterans were dependent on morphine,
and dependence was later called “soldier’s
disease” or “army disease”
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10. Heroin
 Two acetyl groups added to morphine in the
laboratory, creating diacetylmorphine
 Given the brand name Heroin
 Placed on the market in 1898 by Bayer
 Three times as potent as morphine due to
increased lipid solubility of the heroin molecule
 Acts like morphine except that it is more potent
and acts more quickly
 Marketed as a non-habit-forming substitute for
codeine
 Later linked to tolerance and dependence
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11. History of Opioids:
Patterns of Abuse
 Three types of opioid dependence
developed in the U.S. in the second
half of the 19th century
 Oral intake increased as patent medicines
spread
 Opium smoking increased after 1850, as
Chinese laborers arrived in the U.S.
 Injection of morphine—the most dangerous
form of use
 Number and proportion of Americans
dependent on opioids peaked at the
start of the 20th century
 Possibly as high as 1 percent of the
population
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12. History of Opioids:
Patterns of Abuse
 Initially, opioid dependence was not viewed as a major
social problem
 Opium smoking was limited to certain groups
 Patent medicines were socially acceptable
 Opioid dependence was viewed as a “vice of middle life”
 Typical user was a 30-to-50-year-old
middle class white woman, wife, and
mother
 Drugs purchased legally in patent
medicines
 High drugs levels in patent medicines
meant that withdrawal symptoms
were severe and relieved only by
taking more
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13. History of Opioids:
Patterns of Abuse
 Supreme Court decisions about enforcement of the
1914 Harrison Act made opioids difficult to obtain
 Result: Changes in the pattern of opioid use
 Oral use declined; the primary remaining group of users
were those who injected morphine or heroine
 Only sources of drugs were illegal dealers
 Cost and risk of use increased, so the most potent method
(intravenous injection) was favored
 Addicts were looked upon as weak and self-indulgent
rather than as victims
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14. History of Opioids:
Patterns of Abuse
 After the 1914 Harrison Act
 Oral use among the white middle class declined
 Use between World War I and World War II was
limited to particular social groups
 After World War II, use of heroin
increased in low-income areas of
large cities
 The 1960s
 Regular and irregular heroin use
increased in large cities
 Heroin use was associated with
crime and considered socially
unacceptable
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15. History of Opioids:
Patterns of Abuse
 Heroin use by American troops in Vietnam
 Rate of use = about 5 percent
 Heroin was
 Inexpensive
 About 95 percent pure (compared to 5 percent in the U.S.)
 Easy to obtain
 Most users smoked or sniffed the drug
 Most users stopped when they returned to the U.S.
 Vietnam experience showed
 Under certain conditions, a relatively high percent
of individuals will use opioids recreationally
 Opioid dependence and compulsive use are not
inevitable among occasional users
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16. History of Opioids:
Patterns of Abuse
 Production and Purity
 Efforts made to lower the number of heroin users
 End of the “French connection” in the early 1970s:
heroin grown in Turkey, converted to heroin in
southern France, and imported into the U.S.
 By 1975, most U.S. heroin came
from Mexico
 Opium processed into morphine by a
different process, resulting in pure
heroin with a brown or black color,
so-called Mexican brown or black tar
heroin
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17. History of Opioids:
Patterns of Abuse
 Today
 Heroin used in U.S. is currently produced mostly
in South America, Mexico, and Southeast Asia
 Purity of heroin from South America is higher than
heroin from Mexico
 Average purity of street heroin has increased from about
5 percent to 25 percent since the 1970s
 In 2008, the estimated retail purity for Mexican heroin
was 40% and 57% for South American Heroin.
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18. Opioids: Current
Patterns of Abuse
 Heroin: 0.2 percent of Americans report past-year
use
 Recent deaths of celebrities, like Michael Jackson
and Heath Ledger has reignited concerns about
Physicians over prescribing opiod pain medications
 Prescription pain relievers (nonmedical use): 5
percent of Americans report past-year use
 Most are taken orally
 Dependence and toxicity can occur from misuse of
prescription opioids
 The most popular types are hydrocodone and OxyContin
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19. Pharmacology: Chemical
Characteristics
 Raw opium is about 10 percent morphine by
weight, and a smaller amount of codeine
 With the added acetyl groups, heroin can pass
through the blood-brain barrier faster, making
heroin more potent than morphine
 Researchers searching (unsuccessfully) for
ways to separate the analgesic and
dependence-producing effects of opioids have
developed a variety of prescription pain killers
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20. Pharmacology: Chemical
Characteristics
Narcotic agents isolated or derived from opium
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21. Prescription Narcotic
Analgesics
 Natural products  Synthetics
 Morphine  Methadone
 Codeine  Meperidine
 Semisynthetics  Oxycodone
 Heroin  Oxymorphone
 Diamorph (unavailable in U.S.)  Hydrocodone
 Hydromorphone
 Dihydrocodeine
 Propoxyphene
 Pentazocine
 Fentanyl
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22. Pharmacology: Chemical
Characteristics
 Opioid antagonists = drugs that block
the action of opioids
 Examples: Naloxone (Narcan) and
nalorphine
 Effects:
 Reverse depressed respiration from opioid
overdose
 Precipitate withdrawal syndrome
 Prevent dependent individuals from
experiencing a high from subsequent opioid use
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23. Pharmacology:
Mechanism of Action
 Opioids act on selective receptors in the brain
 Naturally occurring opioid-like products of the
nervous system and endocrine glands activate
brain opioid receptors
 Enkephalins: morphinelike neurotransmitters found
in the brain and adrenals
 Endorphins: morphinelike neurotransmitters found
in the brain and pituitary gland
 Natural and synthetic opioid drugs as well
endogenous opioids act on multiple types of
opioid receptors in the brain
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24. Medical Uses
 Pain relief
 Reduces the emotional response to pain
and diminishes the patient’s awareness
of, and response to, the aversive stimulus
 Typically causes drowsiness but does not
induce sleep
 Treatment of intestinal disorders
 Reduces colic and counteracts diarrhea
and the resulting dehydration
 Acts by decreasing the number of
peristaltic contractions
 An opium solution known as paregoric is
still available for relief of diarrhea
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25. Medical Uses
 Cough suppressant
 Codeine has long been used to reduce coughing
 It remains available in prescription cough
medications
 Nonprescription cough remedies contain the opioid
analogue dextromethorphan
 It produces hallucinogenic effects at high doses
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26. Dependence Potential
 Tolerance
 Tolerance develops to most effects from
both medical and recreational usage
 Higher doses needed to maintain effects
 Cross-tolerance exists among all the opioids
 Psychological processes play a key role in
tolerance
 Dependent individuals develop a conditioned
reflex response to the stimuli associated with
taking the drugs
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27. Dependence Potential
 Physical dependence
 Symptoms of withdrawal appear in sequence
following the timing of the most recent dose and the
individual’s history of use
 Opioid withdrawal is unpleasant but rarely life-
threatening
 Methadone (long-lasting synthetic opioid) produces
withdrawal symptoms that appear later and are less
severe than those from heroin
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28. Withdrawal Syndrome
Symptoms
Approximate hours after
previous dose
Signs Heroin or Methadone
Morphine
Craving for drugs, anxiety 6 24
Yawning, perspiration, running nose, teary eyes 14 34-48
Increase in above signs plus pupil dilation, goose bumps,
tremors, hot and cold flashes, aching bones and 16 48-72
muscles, loss of appetite
Increased intensity of above, plus insomnia; raised blood
pressure; increased temperature, pulse rate, respiratory 24-36
rate and depth; restlessness; nausea
Increased intensity of above, plus curled-up position,
vomiting, diarrhea, weight loss, spontaneous ejaculation 36-48
or orgasm, hemoconcentration, increased blood sugar
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29. Dependence Potential
 Psychological dependence
 Positive reinforcement
 Positive effects reliably follow use
of the drug
 Negative reinforcement
 Use of the drug removes
withdrawal symptoms
 Fast-acting injectable opioids
are most likely to lead to
dependence
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30. Toxicity Potential
 Acute toxicity
 Opioids depress respiratory centers in the brain
 Breathing becomes slower and shallower
 Effects with alcohol are additive
 Opioid overdose triad
 Coma
 Depressed respiration
 Pinpoint pupils
 Clouding of consciousness
 Occasionally, nausea and vomiting
 Can be counteracted with naloxone
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31. Toxicity Potential
 Chronic toxicity is associated with
injection method of use
 Infections and the spread of blood-borne
diseases
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32. Life of a Heroin User
 Three to four injections needed daily to
prevent withdrawal
 Expensive habit (cost of drugs and
paraphernalia)
 Risk of overdose due to variable potency of
different batches
 Health problems associated with injection
habit
 Skin infections
 Blood-borne infections
 Masking of early symptoms of illness
 Some users “mature out”
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33. Misconceptions and
Preconceptions
 Not all users experience euphoria from initial dose
 Tolerance to negative effects may develop more
rapidly than tolerance to positive effects
 Withdrawal is often similar to a mild case of the
intestinal flu
 People usually don’t become dependent after one
dose
 Current users:
 Probably about one million opioid-dependent Americans and
two to three times that many heroin chippers (occasional
users)
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34. Chapter 13
Opioids
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