3. We have completed one half of this
entire class. How are you doing in
this class?
Michelle’s office hour:
11:30-12:30 M-F
Email through Canvas
Call/text 872-701-0007
A. Awesome!
B. I’m keeping up.
C. I’m lost…help!
8. Heroin Abuse
Heroin is classified as a Schedule I drug.
One of the most widely abused illegal drugs in
the world; accounts for >$120 billion sales/year
Illicitly used more than any other drug of abuse
in the United States (except for marijuana)
until 20 years ago, when it was replaced by
cocaine
Some of the recent increases in heroin use
likely due to increased abuse of prescription
opioid painkillers
9. Heroin Combinations
Pure heroin is a white powder.
More than 90% of world’s
heroin is from Afghanistan.
Heroin is usually “cut” (diluted)
with lactose.
When heroin first enters the
United States, it may be 95%
pure; by the time it is sold, it
may be 3% to 70% pure.
If users are unaware of the
variance in purity and do not
adjust doses accordingly,
results can be fatal.
10. Heroin Combinations (continued)
Heroin has a bitter taste and is often cut with
quinine, which can be a deadly adulterant.
Heroin plus the artificial narcotic fentanyl can
be dangerous due to its unexpected potency.
Heroin is most frequently used with alcohol.
Heroin combined with cocaine is called
“speedballing.”
11. Facts About Heroin Abuse
What is the estimated number of heroin addicts in the United
States?
600,000
What are “shooting galleries”?
Locations that serve as gathering
places for addicts
12. Heroin and Crime
Factors related to crime:
Pharmacological effects encourage
antisocial behavior that is crime-related
Heroin diminishes inhibition
Addicts are often self-centered, impulsive,
and governed by need
Cost of addiction
Similar personality of criminal and addict
13. Patterns of Heroin Abuse
Heroin has become purer (60% to 70% purity) and cheaper
(~$10/bag).
Greater purity leads users to administer heroin in less efficient ways.
Many youth believe that heroin can be used safely if not injected.
14. Patterns of Heroin Abuse
(continued)
Because of its association with popular fashions and entertainment,
heroin has been viewed as glamorous and chic, especially by many
young people, although lately this attitude has been changing.
Emergency room visits due to narcotic overdoses were over 190,000
in 2009.
15. Stages of Dependence Initially, the effects of heroin are often unpleasant.
Euphoria gradually overcomes the aversive effects.
The positive feelings increase with narcotic use, leading to
psychological dependence.
In addition to psychological dependence, physical dependence occurs
with daily use over a 2-week period.
If the user abruptly stops taking the drug after
physical dependence has developed, severe
withdrawal symptoms result.
17. Heroin Addicts and AIDS
More than 250,000 patients in United States contracted AIDS by drug
injection, of which most were heroin users.
Fear of contracting HIV from IV heroin use has contributed to the
increase in smoking or snorting heroin.
Many who start by smoking or snorting progress to IV administration
due to its more intense effects.
18. Heroin and Pregnancy
Heroin use by a pregnant woman leads to:
Physical dependence on heroin in the
newborn
Withdrawal symptoms after birth in the
newborn (Note: similar withdrawal occurs in
newborns of any woman who uses
significant amounts of opiate drugs during
pregnancy, including prescribed opiate
painkillers)
19. At one time, heroin
was given to morphine
addicts to help them
break their addiction to
morphine.
A. True
B. False
20. 1914 Harrison Act
Made opioids difficult to obtain
Oral use declined
Cost and risk increased
View of addicts changed
22. Review: Which two compounds
are in the opium plant resin?
A. Oxycontin and
heroin
B. Morphine and
heroin
C. Morphine and
codeine
D. Hydrocodone and
codeine
Oxycontin
and
heroin
M
orphine
and
heroin
M
orphine
and
codeine
Hydrocodoneand
codeine
0%
10%
76%
14%
23. Review: What impact did the
Harrison Act have on opium use?
A. Opium use
increased
B. Opium was no
longer readily
available
C. Illegal IV use
decreased
D. Oral use
increased
Opium
use
increased
Opium
wasno
longerrea...
IllegalIV
use
decreasedOraluse
increased
15%
0%0%
85%
24. Review: Upon returning to the US, soldiers
who used opiates in Vietnam:
A. 70% were
arrested for illegal
drug use
B. 67% became
homeless
C. 95% stopped
using the drug
70%
w
ere
arrested
forill...67%
becam
ehom
eless
95%
stopped
usingthe
drug
0%
100%
0%
27. Pharmacology
Raw opium is about 10% morphine, smaller
amount of codeine
Heroin is made by adding two acetyl
groups
Allows passing through blood-brain barrier faster
Mouse Party
Enkephalins – adrenal gland
Endorphins – pituitary gland
31. Opioid Side Effects
Drowsiness
Respiratory depression
Nausea/vomiting
Inability to urinate
Constricted pupils
Constipation
Physical dependence and withdrawal
32. Emotional Effects
Relief from anxiety, hostility, feelings of
inadequacy, and aggression
Difficulty regulating inhibitions and
frequently make risky decisions
33. Social Effects
Alienated from and hostile toward friends
and family
Correlated with criminal behavior,
unemployment, and violence
35. Review: which of the following is
NOT a medical use for narcotics?
A. Cough
suppressant
B. Stop diarrhea
C. Induce sleep
D. Pain relief
Cough
suppressant
Stop
diarrhea
Inducesleep
Pain
relief
30%
0%
30%
40%
36. Dependency
About half of narcotic abusers
become dependent:
Tolerance
Positive reinforcement
Negative reinforcement
Can develop in less than two weeks
Average addiction is six to eight years
(aging out)
39. Which is an example of chronic
physiologic toxicity?
A. Making bad decisions
while high
B. Committing crimes to
obtain the drug
C. Acquiring an HIV
infection through use of
unclean needles
D. Depressed respiration
M
akingbad
decisionsw
h...
Com
m
ittingcrim
esto
ob...
Acquiringan
HIV
infecti..
Depressed
respiration
10%
15%
60%
15%
40. Withdrawal
Factors affecting the difficulty of withdrawal:
Social support network
Desire to stop
Physical environment during withdrawal
Alternative opiates
41. Signs Heroin or
Morphine
Methadone
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
muscles, loss of appetite
16 48-72
Increased intensity of above, plus insomnia; raised blood
pressure; increased temperature, pulse rate, respiratory
rate and depth; restlessness; nausea
24-36
Increased intensity of above, plus curled-up position,
vomiting, diarrhea, weight loss, spontaneous ejaculation
or orgasm, hemoconcentration, increased blood sugar
36-48
(hours after last dose)
Narcotic
Withdrawal
44. Opinion: Do you agree with the
use of suboxone or methadone to
help a person quit using opioids?
A. Yes
B. No
45. Which drug has the most
dangerous withdrawal syndrome?
A. Heroin
B. Morphine
C. LSD
D. Alcohol
Heroin
M
orphine
LSD
Alcohol
43%
57%
0%0%
46.
47. I think Needle Exchange
Programs are a good idea.
A. True
B. False
True
False
0%0%
Editor's Notes
Sometimes called opioids. Some texts differentiate between opioids = naturally derived from opium (morphine/codeine), opiates – synthetic reproductions of opioids: heroin, methadone, fentanyl, oxycontin, hydrocodone, and others. Cultivated from an annual flowering plant. Origin in the Middle East. Only available for collection for a few days of the plant’s life.
Collectors use a sharp, clawed tool to make shallow cuts into the unripe seedpods.
Resinous substance oozes out and is scraped and collected – raw opium.
Today most heroin is produced in South America, Mexico and Southeast Asia.
By 1906, opium and its derivatives were found in more than 50,000 medicines
The hypodermic needle hastened the effects of morphine
By the late 1800s, an estimated 4.59 per 1,000 people were dependent on opiates
Ironically, the drug promoted to help people overcome morphine dependency was heroin
The opium poppy, Papaver somniferum, is cultivated throughout Asia and the Middle East
When the seedpod is cut open, it exudes a white, milky sap which dries to a brown, thick, gummy resin (opium)
There is only a ten-day window in which opium can be made from the resin of the opium poppy
In 1803, Friedrich Serturner of Germany synthesized morphine from opium and called it morphium
Morphine is about ten times more potent than opium, although physicians thought it was safer and purer
Codeine was isolated from opium 30 years later
How morphine is administered and its dosage has a bearing on its effectiveness
Heroin (diacetylmorphine) was first synthesized from morphine in 1874
When heroin was introduced, it was believed not to be addicting
When smoked, its effects are rapid – it is ineffective when ingested
Heroin is three to ten times more powerful than morphine because it is more lipid-soluble
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.
Abuse rate for prescribed opioid narcotics has gone from 2.2% to 10% in the past 10 years
Although opioid narcotics possess abuse potential, they also have important clinical value (e.g., analgesic, antitussive, antidiarrheal).
The term narcotic has been used to label many substances, from opium to marijuana to cocaine.
HISTORY
A 6000-year-old Sumerian tablet
The Egyptians
The Greeks
Arab traders
China and opium trade
The Opium War of 1839
American opium use
Abuse problems often associated with war
Available in patent medications
Increased in 1850 as Chinese laborers arrived in the US
Dependence 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
Thomas de Quincey 1823 drank laudanum and wrote a book Life of an Opium Eater.
Seen as a vice of middle age.
By 1906, opium and its derivatives were found in more than 50,000 medicines
The hypodermic needle hastened the effects of morphine
By the late 1800s, an estimated 4.59 per 1,000 people were dependent on opiates
Ironically, the drug promoted to help people overcome morphine dependency was heroin
Opium was outlawed in China in 1729
The British East India Company was involved in opium trade in India & China, eventually led to war between British and Chinese
Morphine is the active ingredient in opium and was isolated in 1806. It’s 10 times as potent as opium. It was named morphium after Morpheus the God of Dreams.
In 1832 another alkaloid of opium was discovered and named codeine “poppy head”
The hypodermic syringe was invented in 1853 allowing for IV use of 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”
Two acetyl groups added to morphine given the brand name Heroin and marketed by Bayer 1898. 3X more potent than morphine because the increased lipid solubility of the heroin molecule easily passes the Blood-Brain Barrier. Acts more quickly. Was originally marketed as a non-habit forming substitute for codeine. Most of today’s heroin comes from South America, Mexico and Southeast Asia. Average purity has increased from about 5% to 25% since the 70s. In 2008, retail purity for Mexican heroin 40% and South American heroin 57%.
With the invention of the hypodermic syringe, increased IV use.
68% of heroin addicts admitted into treatment are male, 59% are White, and ¾ have been in treatment previously
Increase in abuse is significantly higher in rural areas than in metropolitan areas
During the Vietnam War, 10-15% of US troops were addicted to heroin
More than 15 million people worldwide illegally use opium, morphine, and heroin
Afghanistan is the largest heroin producer worldwide
China is believed to have the largest number of narcotic addicts
An estimated 24 million to 34 million people throughout the world use opium
Made these drugs available only by prescription. This changed the pattern of opioid use. The only source for these drugs without a prescription was illegal drug dealers. Oral use declined and the primary remaining users were IV users of morphine or heroin. Cost and risk of use increased and so the most potent method of use was favored. Addicts were seen as weak and self-indulgent. Oral use declined and use in low-income areas of large cities increased. By the 60s, heroin use was associated with crime and considered socially unacceptable.
The Harrison Act of 1914 made narcotic use without a prescription illegal
The typical opiate addict shifted from a middle-class woman to a young, lower-class man
Perceptions of the opiate addict went from unfortunate victim to a deviant criminal who was a threat to society
During the 1930s, morphine abuse exceeded heroin abuse – by the 1940s, heroin addiction was greater
Heroin use increased greatly beginning in the late 1960s and early 1970s.
In 2010, about 200,000 Americans had used heroin in the previous month
In the US, more than 800,000 people are addicted to heroin and other narcotics
Heroin was inexpensive and relatively pure. 95%. Most users smoked or sniffed the drug. Contrary to popular opinion, Vietnam showed that under certain conditions a relatively high number of individuals will use opioids recreationally and that dependence and compulsive use are not inevitable among occasional users.
5% report non-medical use – given as prescription pain relievers/analgesic
Most are given orally as prescriptions
Dependence & toxicity from misuse – users misuse by crushing and smoking or snorting the pills
Police in WW report that prescription opioids are selling for high prices on the street. $1 per mg, so a 20 mg pill would sell for $20.
Have seen an increase in opioid abuse/dependency. Most anecdotal stories involve individuals who began with prescription drug use, misused or abused the prescription, and found it expensive to obtain on the streets/illegally. Many then turn to heroin in order to avoid withdrawal. Heroin is much cheaper, but is also unpredictable as far as potency and purity.
Morphine
Methadone
Fentanyl
Hydromorphone
Oxycodone (OxyContin)
Meperidine
Dextromethorphan: OTC antitussive
Clonidine: Relieves some of the opioid withdrawal symptoms
Naloxone/Naltrexone: Narcotic antagonist; used for narcotic overdoses
Buprenorphine
MPTP
Codeine
Pentazocine
Tramadol
Naturally occurring opioid-like products of the nervous system and endocrine glands activate brain opioid receptors
Enkephalins: morphine like neurotransmitters found in the brain and adrenals
Endorphins: morphine like neurotransmitters found in the brain and pituitary gland
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
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
PHARMACOLOGICAL EFFECTS
The most common clinical use of the opioid narcotics is as analgesics to relieve pain.
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 but can also reduce the effects of stress.
Morphine is a particularly potent pain reliever and often is used as the analgesic standard by which other narcotics are compared.
With continual use, tolerance develops to the analgesic effects of morphine and other narcotics.
Physicians frequently underprescribe narcotics, for fear of causing narcotic addiction.
The principle side effects of opioid narcotics, besides their abuse potential, include:
Drowsiness, mental clouding
Respiratory depression
Nausea, vomiting, and constipation
Inability to urinate
Drop in blood pressure
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)
68% of heroin addicts admitted into treatment are male, 59% are White, and ¾ have been in treatment previously
Increase in abuse is significantly higher in rural areas than in metropolitan areas
During the Vietnam War, 10-15% of US troops were addicted to heroin
More than 15 million people worldwide illegally use opium, morphine, and heroin
Afghanistan is the largest heroin producer worldwide
China is believed to have the largest number of narcotic addicts
An estimated 24 million to 34 million people throughout the world use opium
Physical and psychological dependence, and tolerance develop quickly
Positive reinforcement
Negative reinforcement
Withdrawal symptoms can be severe
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
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
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
Factors affecting the difficulty of withdrawal:
Availability of a social support network
Addict’s desire to stop
Physical environment during withdrawal
Convenience and practicality of alternative opiates
About half of narcotic abusers become dependent:
People can become drug-dependent in less than two weeks if they take increasing amounts of narcotics
Average addiction is six to eight years
Narcotics relieve psychic distress arising from anxiety, hostility, feelings of inadequacy, and aggression
Heroin addicts have difficulty regulating inhibitions and frequently make risky decisions
Users sometimes ignore or become alienated and hostile toward friends and family members
Heroin use has been associated with criminal behavior, unemployment, and violence
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
Narcotics cause drowsiness, vomiting, nausea, and difficulty concentrating
Euphoria is followed by gradually anesthetizing sensations, then sleep and lethargy
Opiates impede the ability to urinate, and can cause potentially serious constipation
Male addicts have difficulty achieving an erection
Chronic toxicity is associated with injection method of use
Infections and the spread of blood-borne diseases
Narcotics are capable of depressing the respiratory system to the point of death
According to the CDC, painkillers kill twice as many people as cocaine and five times more people than heroin
Synergistic effect of narcotics and other drugs can be fatal
Death from an overdose of heroin is slow – people who die quickly are likely to die from anaphylactic shock
ABUSE/DEPENDENCY
All the opioid narcotic agents that activate opioid receptors have abuse potential and are classified as scheduled drugs.
Tolerance begins with the first dose of a narcotic, but does not become clinically evident until after 2 to 3 weeks of frequent use.
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 and typically expresses when these drugs are used for more than 2–4 weeks.
Psychological dependence can also develop with continual narcotic use.
RECOMMENDATIONS TO AVOID DEPENDENCY
Only use opioid analgesics when pain severity warrants
Doses and duration of use should be as conservative as possible
Patients should store these medications securely to prevent their theft and misuse
Do not share with anyone else
Doctors should screen patients for abuse risk before prescribing opioid drugs
Patients should be educated about potential abuse problems prior to being prescribed opioid drugs
If significant abuse is suspected, the clinician should discuss concerns with patient to find appropriate steps to stop the abuse
Physical and psychological dependence, and tolerance develop quickly
Positive reinforcement
Negative reinforcement
Withdrawal symptoms can be severe
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
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
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
Factors affecting the difficulty of withdrawal:
Availability of a social support network
Addict’s desire to stop
Physical environment during withdrawal
Convenience and practicality of alternative opiates
About half of narcotic abusers become dependent:
People can become drug-dependent in less than two weeks if they take increasing amounts of narcotics
Average addiction is six to eight years
Narcotics relieve psychic distress arising from anxiety, hostility, feelings of inadequacy, and aggression
Heroin addicts have difficulty regulating inhibitions and frequently make risky decisions
Users sometimes ignore or become alienated and hostile toward friends and family members
Heroin use has been associated with criminal behavior, unemployment, and violence
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
Narcotics cause drowsiness, vomiting, nausea, and difficulty concentrating
Euphoria is followed by gradually anesthetizing sensations, then sleep and lethargy
Opiates impede the ability to urinate, and can cause potentially serious constipation
Male addicts have difficulty achieving an erection
Chronic toxicity is associated with injection method of use
Infections and the spread of blood-borne diseases
Narcotics are capable of depressing the respiratory system to the point of death
According to the CDC, painkillers kill twice as many people as cocaine and five times more people than heroin
Synergistic effect of narcotics and other drugs can be fatal
Death from an overdose of heroin is slow – people who die quickly are likely to die from anaphylactic shock
After the effects of the heroin wear off, the addicts have only a few hours in which to find the next dose before severe withdrawal symptoms begin.
A single “shot” of heroin lasts 4 to 6 hours.
Withdrawal symptoms: runny nose, tears, minor stomach cramps, loss of appetite, vomiting, diarrhea, abdominal cramps, chills, fever, aching bones, and muscle spasms.
Reverse depressed respiration from opioid overdose
Precipitate withdrawal syndrome
Prevent dependent individuals from experiencing a high from subsequent opioid use
SUBOXONE is a combination of two drugs: Buprenorphine: an opiate that acts to fill up the brain’s opiate receptors without causing sleepiness or “high” feelings. It has a low risk of overdose.
Naloxone , a drug that is not absorbed orally but helps persuade people not to inject Suboxone in the vein as it causes instant withdrawal.
Methadone (long-lasting synthetic opioid) produces withdrawal symptoms that appear later and are less severe than those from heroin. Usually administered orally. Can be abused if concentrated and injected.
TREATMENT
Methadone or buprenorphine are frequently used to help narcotic addicts.
These drugs block withdrawal symptoms.
Treatment should also include regular counseling and other supplemental services such as job training.
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”
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)