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Uppers, Downers &
All Arounders
Chapter 4
Downers: Opiates/Opioids &
Sedative-Hypnotics
Downers (depressants)
Opiates/Opioids
Opium, codeine, morphine, heroin
Vicodin , OxyContin 
Sedative-Hypnotics
Benzodiazepines, e.g., Valium 
Barbiturates, e.g., Seconal 
Others, e.g., Rohypnol ,
Miltown 
Alcohol
Beer, wine, hard liquor
Copyright 2004, CNS Productions,
Inc.
1
General Classification
• Downers induce:
– Sedation
– Muscle Relaxation
– Drowsiness
– Coma by depressing the Central Nervous
System
– Works more on the sites throughout the body
than uppers (which generally stimulate the
Neurochemicals
General Classification
•
Major Depressants
1. Opiates/opioids
a. Used to treat acute pain, diarrhea, coughs and
other ailments
b. Abused for the euphoric affect
c. For Physical & emotional relief
d. Suppression of withdrawal effects
•
Sedative-hypnotics
a. Synthesized drugs designed to treat anxiety and
insomnia
b. Can cause tissue dependence
•
Alcohol (Chapter 5)
General Classification
II.
Minor Depressants
1.Skeletal muscle relaxants
a.
b.
Synthetically designed to depress areas in the
brain responsible for muscle coordination and
activity
Prescribed for muscle tension and pain
2. Antihistamines
a.
b.
c.
d.
e.
Synthetic drugs used to treat allergies, ulcers,
shock, rashes and motion sickness
Produces drowsiness
Blocks the release of histamine
Can induce depression
Abused for depressant effects
General Classification
II.
Minor Depressants
1. Over-the-counter downers
a. Nytol, Sominex: marked as sleep aids and
sedatives
2. Lookalike downers:
•
•
Looked like prescription downers
Rarely found, except in magazine ads for
legal downers
Opiates/Opioids
• Oldest and best-domented of psychoactive
drugs
• Discovery of neurotransmitters/own body’s
natural painkillers:
– endorphins & enkephalins changed scientists
understanding of opiates/opioids
– & field of addiction
Opiates/Opioids
• Opium is processed from milky fluid of the opium poppy
plant producing
– Morphine, codeine & thebaine
• Semi-synthetic opiates include:
–
–
–
–
–
Heroin
Vicodin
OxyContin
Percodan
Dilaudid
• Fully synthetic opiate-like drugs include
– Demerol
– Darvon
– Methadone
• Antagonist that block effects are naloxone & natrexone
Opiates/Opioids
• Some opioids (opium,
morphine, codeine,
thebaine) are refined
directly from the milk of the
opium poppy.
Heroin, oxycodone
Percodan, OxyContin,
Dilaudid) are
semisynthetic, which means
that a refinement of the
opium poppy is manipulated
in the laboratory.
• Some opioids (e.g.,
methadone, Demerol,
Darvon) are completely
synthetic. (p. 142)
Opiates/Opioids
From Opium Semisynthetic
Synthetic
opium
morphine
methadone
propoxyphene
(Darvon )
meperidine
(Demerol )
fentanyl
(Sublimaze )
codeine
thebaine
heroin
hydrocodone
(Vicodin)
hydromorphone
(Dilaudid )
oxycodone
(OxyContin )
Copyright 2004, CNS Productions,
Inc.
3
Opiates/Opioids
• History of Use
– Used by ancient Sumerians, Egyptians & Chinese as
medicine, pleasure and poison
– Opium originally chewed, eaten and drunk in liquids
– Bitter taste limited addiction
– Used throughout Middle Ages
– Smoking opium:
•
•
•
•
•
increased nonmedical use
Increased intensity of effects
Multiplied its abuse potential
Actively promoted by British in China
Introduced to U.S. by Chinese immigrants
Opiates/Opioids
• Refinement of Morphine, codeine & heroin
from opium increasing its strength
• Codeine only 1/5 strength of morphine
• Used in cough syrups & other drugs
• Heroin was refined from morphine
• IV use began in 1853 with invention of
hypodermic needle
• Patent medicines introduced mid-1880s
• Used in tonic
• Physician induced addiction was common
Opiates/Opioids
• Snorting was popular method of taking heroin
• More than half of addicts that enter treatment began by
snorting
• 20th century
– Nonmedical use declared illegal at beginning of 20th century
– Pur Food and Drug Act 1906 and Harrison Narcotics Act in 1914
– Est. 3.5 million Americans use prescription opiates/opioids
monthly
– Est 120,00 to 800,000 heroin users in U.S.
– 5-10 milion regular users world wide
– U.S. consumes only 3%
– Afghanistan produces 70% of world supply
– China White (Golden Triangle in Asia)
– Black Mexican Tar
– Colombian cartels
HEROIN
• Block of refined heroin
weighing 1 kilogram.
• This block of heroin was
processed in the jungles of the
Golden Triangle (Myanmar
[Burma], Northern Thailand,
and Laos) and packaged for
easy smuggling. Golden
Triangle heroin, known as
“China White,” is extremely
pure. (pp. 145–147)
•
•
Copyright 2004, CNS Productions,
Inc.
8
Picture of Mexican “tar” heroin.
“Tar” heroin is most prevalent in
the western United States. It is
often 40–80% pure but also has
more plant impurities. A small
chunk the size of a match (2–5
doses) sells for $20–25. It
dissolves easily in water for
injection. (p. 146).
Copyright 2004, CNS Productions,
Inc.
10
Effects of Opioids
• Prevents the transmission of Substance “P”.
• Painkilling: effects include lower anxiety,
serenity, drowsiness and deadening of unwanted
emotions
• Pleasure: Artificially activate the
reward/reinforcement center by slotting into
receptor sites meant for endorphions
• Heroin has strongest effects of any of the
opioids on the reward pathway
• Psychoactive drugs disrupts the CUT-OFF
switch in the brain that says that’s enough,
thereby reinforcing the desire to continue to use
Side effects of Opioids
• Physical:
–
–
–
–
–
Felt in almost every part of body
Noticeable: Droopy eyelids, nodding, slurred speech
Suppression of cough center
Digestive and hormonal
Nausea and constipation
• Tolerance:
– Occurs when body tries to neutralize heroin
•
•
•
•
•
Speeds-up metabolism
Desensitizes nerve cells
Excreting drug from body
Altering the brain and body to compensate of effects of drug
Develops at different rate for different body systems
Side effects of Opioids
• Tissue Dependence
– Adaptation to the effects can alter brain
chemistry temporarily or permanently
– Body relies on drug to stay normal
• Withdrawal
– Acute withdrawal occurs 2-3 weeks after
abstinence
– Protracted or Post Acute Withdrawal (PAWS)
can occur for months
– Heroin & morphine more severe
Side effects of Opioids
• Neonatal: Opioids cross the placenta resulting
in risk of miscarriage,
–
–
–
–
–
placenta separation,
premature labor,
stillbirth,
Seizures
Addiction of infant: withdrawal is severe (death in
some cases)
• Overdose in older users can be fatal
– Severe respiratory depression
– Opioid antagonist: Narcan can counteract overdose
but victim will still experience severe withdrawal
Side effects of Opioids
• Dirty/Shared Needles:
– Risk of adulteration
– Bacteria and viral infections
– (Hepatitis C, HIV/AIDS)
•
•
•
•
50-90% of IV users carry Hep. C virus
25% OF HIV/AIDS cases used needles
10% of AIDS transmitted through sex
70% of children with HIV from mothers who were
IV users or had sexual contact with IV users
Side effects of Opioids
• Abscesses & other
infections
• Necrotizing fasciitis
– Destroys the fascia
& subcutaneous
tissues
• Endocardistis
– Infection of heart
valves
• Cotton Fever
– Endotoxins that
thrive in cotton
Needle Use Infections
Abscesses
Septicemia
Cotton fever
Hepatitis B & C
Endocarditis
Embolism
HIV & AIDS
Copyright 2004, CNS Productions,
Inc.
11
Opioids
• Cost:
– $20 - $200 daily depending on level of use
– 60% of cost through consensual crime
– 73% of heroin users are gainfully employed
• Polydrug use:
–
–
–
–
Stop withdrawal symptoms
Speed to get energetic
Mixing drugs
Morphing use of multiple drugs to counter the effects
of original drug
– Cycling: giving up drug to lower tolerance
– Sequential: using one drug then to another drug
Morphine & Other Opioids
• Morphine:
– Refined from opium
– Liver converts morphine into metabolites
– Can be detected in urine fro several days
– Therapeutic pain control
– Patient become more sensitive to pain after
long-term use because the body produces
fewer of its own painkillers
– Down regulates opioid receptor sites
Morphine & Other Opioids
• Codeine
– Extracted from opium or refined from morpjine
– Analgesic use to control coughs
– Most widely prescribed and abused
prescription drug
– Vicodin now more prescribed (produces less
nausea)
– Last 3 hours in system
– Detectable in urine 2 to 3 days
Morphine & Other Opioids
• Methadone (Dolophine)
– Long-lasting opiod taken to control heroin addiction
– 200,000 heroin addicts involved in methadone
treatment in 950 clinics
• Hydromorphine (Dilaudid)
–
–
–
–
Short-acting semisynthetic opioid
Prescribed as an alternative to morphine
7-10 times stronger than morphine
Mixed with cocaine to make speedballs
Morphine & Other Opioids
• Oxycodone (OxyCondin, Percodan)
– Much stronger than codeine, but weaker than
morphine or Dilaudid
– Time-released version
– When crushed, time-release effect destroyed
• Meperidine (Demoral, Pethidine, Mepergan)
– Most widely used analgesics: 1/6 strength of
morphine
– Most often abused by medical professionals
• Pentazocine (Talwin NX) Opioid antagonist and
agonist
– When combined with antihistamine gives heroin like
high
Morphine & Other Opioids
• Propoxyphene (Darvon, Darvocet)
– Prescribed for mild-moderate pain
– Last 4-6 hours
– Can be used to detox heroin addicts
• Fentanyl (Sublimaze)
– Most powerful opioid (50-100 X’s as strong as
morphine)
– Used right after surgery for severe pain
Morphine & Other Opioids
• Designer heroin
– Street versions of fentanyl
– 100-20,000 Xs stronger than regular heroin
– Can contain MPTP (street demerol) that
destroys dopamine-producing cells that
control voluntary muscular movements
– Mimics Parkinson Disease
– Causes condition called “frozen addict.”
– Addict can lose the ability to make any
physical movements
Morphine & Other Opioids
• LAAM
– Long lasting opioid used for heroin replacement
therapy
– Unsuitable for pain management
• Naloxone (Narcan) & Natrexone (Revia)
– Opioid antagonist that block effects of opioids
– Effective in treating overdoses
– Revia can be used to treat craving for cocaine and
alcohol
• Buprenorphine
– Power opioid agonist at low doses and antagonist at
high doses
– Alternative to methadone
Sedatives/Hypnotics
• 60 million prescriptions written in 2001
• Used for psychiatric medication for
depression
• Two groups of sedative/hypnotics
– Benzodiazeohines
– Barbituates
• Calming and sleep inducing
• Include Bromides introduced in 1850’s
used for sedation and hypnotic
Sedatives/Hypnotics
• Chlora hydrate: sedative or anticonvulsive
• Paradehyde: to control alcohol withdrawal
• Barbiturates: popular in 1940s and 50s
– Low margin of safety
• Meprobamate (Miltown) AKA “Mothers little
helper”
• Benzodiazepines discovered in 1957
– Less toxic than barbituarates
Benzodiazepines
• Most widely used as:
– anti-anxiety drugs,
– Sleep aids,
– Sedatives
– Control seizures
•
•
•
•
•
Prescribed for panic attacks
Insomnia
Skeletal muscular spasms
Control seizures
Anesthetic for seizures
Benzodiazepines
• Non Medical Use:
– Often abused with other drugs
•
•
•
•
To come down off fo methamphetamine, cocaine
Substitute as heroin
To prevent alcohol withdrawal symptoms
Abusers then to be over 30 years, White, weel-educated and
female
– Neurotransmitter GABA
– Converted by live to metabolites more strong that
original drug
– Tolerance develops as liver becomes more efficient in
processing drug
– Younger person can tolerate higher doses
Benzodiazepines
• Tissue Dependence
– Addiction develops 10-20 times the normal
dosage is taken for several months
• Withdrawal
– Can be severe
– Can involve seizures, convulsions and death
– Takes several months to taper off drug
– Withdrawal can come in cycles separated
from 2-10 days
– Symptoms may persist several months
(PAWS)
Benzodiazepines
• Overdose
– Takes 700 Xs the therapeutic dose to be lethal
– Symptoms include
•
•
•
•
•
Drowsiness
Loss of consciousness
Depressed breathing
Coma
Death if left untreated
• Rohhyponal (Date Rape Drug)
– Memory impairment
– 1996 banned in America
– Used to sexually assault someone or commit violence
Barbiturates
• Developed in 1903
• Phenobarbital in 1913
• Effects
– Long-acting, intermediate-acting, short-acting
– Induce feeling of dis-inhibitory euphoria,
similar to alcohol
– Effects often depend on the mood of the
person and setting
Barbiturates
• Tolerance
– Develops in variety of ways
– Dispositional tolerance increase the efficiency
of metabolism
– Pharmacodynamic tolerance
• Reduces nerve cell and tissue sensitivity to the
drug
– Tissue dependence occurs when 8-10 Xs the
dosage is taken daily for 30 days
Barbiturates
• Withdrawal
– Anxiety,
– Agitation,
– Loss of appetite,
– Vomiting
– Increased heart rate
– Excessive sweating
– abdominal cramps
– Tremors
– Can result in in convulsions within 12 hours to
1 week from last dose
Other Sedative/Hypnotics
• GHB:
– Popular among bodybuilders
– Has a similar effect to methaqualone or alcohol
intoxication
– Popular in rave clubs
– Has been used a date rape drug
• GBL:
– Metabolized to GBH in the body
– Also an ingredient in paint strippers
• Methaqualone (Quaaludes, Mandrax)
– Withdrawn from the market in 1984
– Counterfeit versions on market
– Sought for overall sedative effect
Other Sedative/Hypnotics
• Ethchlorynol (placidyl)
– Older sedative-hypnotic “green weenies”
• Synergism
– Occurs when the combined effects of different
drugs are greater on the individual effects
– 4,000 deaths & 50,000 hospital emergency
room visits per year
• Cross-tolerance & Cross-dependence
– Development of tolerance to other drugs
when addiction of one drug increases liability
to using other drugs