Transcript CNS Stimulants

WELCOME TO STREET
DRUG PHARMACOLOGY
Randall Webber, M.P.H.
ESSENTIAL ISSUES IN
UNDERSTANDING STREET DRUG
PHARMACOLOGY
Psychoactivity
Dependence
Tolerance
Toxicity
Psychiatric Impairment
Set and setting
Substance misrepresentation/misidentification
Psychoactivity = ability to affect
mood, thinking and/or behavior
CONTROLLED SUBSTANCES
Schedules I-V
Schedule I: High potential for abuse,
tendency to produce dependence, no
accepted medical use in US
Schedules II-V: Potential for abuse,
tendency to produce dependency, does have
accepted medical application
SCHEDULE I SUBSTANCES
LSD
Heroin
Cannabis
PCP
SCHEDULE II SUBSTANCES
Morphine
Cocaine
Short-acting barbiturates
Amphetamines
DESIGNATED PRODUCTS:
State of Illinois
Schedule II substances with a higher
potential for abuse and addiction
- amphetamines
-
cocaine
short-acting barbs
methadone
morphine
OxyCodone
DRUG NAMES
Chemical (7-chloro-1,3-dyhydro-1-methyl-5phenyl-2H-1,4-benzodiazepin-2-one
Generic: diazepam
Brand : Valium
Street: No common street names for Valium
DRUG MEASUREMENT
metric:
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micro = 1/1,000,000.
Microgram (mcg./m, also called a "gamma“) =
1/1,000,000 gram)
Street
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nickel/nickel bag & dime/dime bag = $5 or $10
worth of drug
eightball = 1/8 oz. (3.75 grams)
DRUG MEASUREMENT
Street
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sixteenth = either 1/16 oz (1.875 gm) or 1/16
gm (62.5 mg, about three lines of cocaine)
line = an elongated pattern of powdered drug.
Quantity = whatever the user decides.
joint = a marijuana cigarette.
DRUG FORMS
plant/botanical matter (marijuana, opium
poppies, khat, coca, peyote, psilocybin
mushrooms, jimsom weed).
liquids (alcohol, pure LSD, injectable
pharmaceuticals)
powders (cocaine hcl., heroin, PCP,
methamphetamine)
DRUG FORMS
pills (tablets, capsules, caplets of either
pharmaceutical or illicit origin)
other forms (ex: "rocks" of crack
cocaine).
Potency, purity & misrepresentation
of street drugs
potency = strength, compared to some
other drug of a similar type.
purity = the major determinant of potency.
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The more pure the drug, the more potent.
Street drugs are seldom pure, but are
commonly misrepresented in one of three
ways
DRUG MISREPRESENTATION
adulteration: (to adulterate = to "step
on"/"hit"/"dance on" "cut" a drug).
Substitution/misrepresentation-1: None of
the alleged drug is present, but another
drug/drugs is/are.
substitution/misrepresentation -2: None of
the alleged drug is present, and neither is any
other drug or active substance.
The Problem with Pill
Identifications:
New York City May 2000 Amphetamine
Chicago May 2000 MDMA
Portland Oct 2000 MDMA
Tucson AZ July 2000 PMA
TIME FACTORS
Onset of action: How quickly does the
drug produced it’s effect?
Duration of action: How long does the
drug’s effect last?
Residual effects: After-effects,
extended drug reaction, flashbacks
The route of circulation.
Blood flows in a circle according to this
pattern:
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Capillaries
vena cava
Lungs
Aorta
- veins
- right side of the heart
- left side of the heart
- body (capillaries, etc.)
Route of Circulation
METHOD OF
ADMINISTRATION
Ingestion (oral): slower onset/longer
duration
Insufflation (sniffing/snorting): faster
onset/shorter duration
Intravenous (I.V.) Injection: faster onset
(seconds)/shortest duration
Smoking: fastest onset/shortest duration
METHOD OF
ADMINISTRATION
Ingestion (oral): slower onset/longer
duration
Insufflation (sniffing/snorting): faster
onset/shorter duration
Intravenous (I.V.) Injection: faster onset
(seconds)/shortest duration
Smoking: fastest onset/shortest duration
METHOD OF
ADMINISTRATION
Ingestion (oral): slower onset/longer
duration
Insufflation (sniffing/snorting): faster
onset/shorter duration
Intravenous (I.V.) Injection: faster onset
(seconds)/shortest duration
Smoking: fastest onset/shortest duration
THE “RUSH” OR “FLASH”
A highly pleasurable sensation
produced by the instantaneous effect
of i. v. injection or smoking*
* If entire dose administered at once
METABOLISM AND EXCRETION
The break-down of a drug into
simpler substances
The removal of the drug from the
body
TOLERANCE
Homeostasis
The human body’s natural
tendency to move toward a
state of equilibrium or
constancy
SET POINT RESPONSE TO DRUG
USE
TOLERANCE
Need to increase the dose of a drug in order
to obtain the desired effect
Decreased effect of drug after repeated
administration
Dependent on prior dosage level
Develops in hours (cocaine), days (LSD), or
weeks
TOLERANCE
Effective dose (ED)
Intoxicating dose (ID)
Lethal dose (LD)
TYPES OF TOLERANCE
Enzyme induction
Pharmacodynamic
Behavioral Need to increase the dose
of a drug in order to obtain the desired
effect
DEPENDENCE
Addiction
Physical dependence
ADDICTION POTENTIAL
What percentage of first-time users will
enjoy the effect of the drug enough that
they will seek it out again?
If an individual uses the drug on a
regular basis, how likely is it that s/he
will become dependent on the
substance?
ADDICTION POTENTIAL
After being introduced to the drug, do sub-human
animals (e.g., monkeys, rats, mice) seek out
opportunities to self-administer the substance? Do
they do so to the exclusion of eating, consuming
water and engaging in reproductive behavior?
ADDICTION POTENTIAL CAN ALSO BE PREDICTED IN
PART BY OBSERVING ANIMAL SELFADMINISTRATION
ADDICTION POTENTIAL
Ability to stimulate the brain’s reward
circuits
Ability to meet a individualized
neurochemical need
Physical dependency potential
Intensity of withdrawal symptoms
ADDICTION POTENTIAL
Ability to stimulate the brain’s reward
circuits
Ability to meet a individualized
neurochemical need
Physical dependency potential
Intensity of withdrawal symptoms
Dopamine Levels in the Shell of the Nucleus
Accumbens
(% of baseline)
400
350
300
250
200
Dopamine
150
100
50
0
Morphine
Nic
Coke
Dopamine Levels in the Shell of the Nucleus
Accumbens
(% of baseline)
160
140
120
100
80
Dopamine Levels
60
40
20
0
Food
Dopamine Levels in the Shell of the Nucleus
Accumbens
(% of baseline)
250
200
150
Dopamine Levels
100
50
0
Food
Sex
Dopamine Levels in the Shell of the Nucleus
Accumbens
(% of baseline)
200
180
160
140
120
100
80
60
40
20
0
Dopamine
Morphine
Dopamine Levels in the Shell of the Nucleus
Accumbens
(% of baseline)
240
230
220
210
Dopamine
200
190
180
Morphine Nicotine
Dopamine Levels in the Shell of the Nucleus
Accumbens
(% of baseline)
1200
1000
800
600
Dopamine
400
200
0
Morphine
Nic
Coke
Amphet
Dopamine Levels in the Shell of the Nucleus
Accumbens
(% of baseline)
160
140
120
100
80
Dopamine Levels
60
40
20
0
Food
Dopamine Levels in the Shell of the Nucleus
Accumbens
(% of baseline)
250
200
150
Dopamine Levels
100
50
0
Food
Sex
Dopamine Levels in the Shell of the Nucleus
Accumbens
(% of baseline)
1200
1000
800
600
Dopamine Levels
400
200
0
Food
Sex
Meth
NEUROTRANSMITTERS
Naturally-occurring brain chemicals
Many psychoactive drugs resemble
neurotransmitters:
NEUROTRANSMITTERS
DRUG
NEUROTRANSMITTER
LSD
Serotonin
Methamphetamine
Norepinepherine
heroin
Endorphins
NEUROTRANSMITTERS
DRUG
NEUROTRANSMITTER
THC
Anandamide
PCP
Receptor site identified
but not associated
neurotransmitter
ADDICTION
Compulsive drug-taking
Loss of control
Continued use despite negative
consequences
Tolerance and physical dependence
not required but may be part of the
addiction picture
TOXICITY
Ability to produce physical damage to
the human body
Long-range = months, years
Short-range = days, weeks
Physical vs behavioral
TOXICITY
Physical
Behavioral
Acute Vs Long-Term
PSYCHIATRIC IMPAIRMENT
Ability of drug to produce negative
changes in thinking, learning,
perception, mood or behavior
Acute vs chronic
PSYCHIATRIC IMPAIRMENT
Short-term
Long-term
Affective Disorders
Thought Disorders
CNS Stimulants
Amphetamines/Similar-Acting Stimulants
Cocaine
Khat
OTC Stimulants
CNS Stimulants
 pulse, breathing, BP
Alertness/Reversal of fatigue
Reduction in appetite
Dilated pupils
Euphoria, elation, grandiosity, confidence
Talkativeness
Racing thoughts
CNS Stimulants
(Amphetamines)
"speed", "white cross", "black beauties",
"357's", "purple hearts“
amphetamine sulfate (Obetrol)
dextroamphetamine (Dexedrine)
methampetamine (Desoxsyn) ("meth", "crystal",
“crank”, “go fast")
Mixed amphetamine: (Adderall)
Methamphetamine “Crystal”
Methamphetamine “Ice”
WHITE CROSS
CRANK
ICE
CNS Stimulants
(Non-Amphetamines)
benzphetamine (Didrex)
mazindol (Sanorex)
methylphenidate (Ritalin)
phenmetrazine (Preludin/Prelud-2)
diethylpropion (Tenuate)
phedimetrazine (Plegine/Bontril)
phentermine (Fastin)
Ritalin
CNS Stimulants
(Cocaine)
Local anesthesia
coca (Erythoxlum Coca)
cocaine hydrochloride (hcl) ("coke",
"toot", "nose/nose candy", "blow",
"freeze", "snow", "girl", "white lady", "la
mujer blanca")
alkaloidal cocaine ("free base", "crack",
"rock/ready rock", "basuco")
ERYTHROXYLOM COCA FLOWER
COCA FARMER
MAKING COCAINE
Cocaine Hcl
COCAINE PARAPHERNALIA
VIALS OF CRACK
MORE CRACK
Crack Packaged for Sale
Crack Pipes
CNS Stimulants
(General Characteristics)
Addiction potential high (Except OTCs)
Physical dependence absent or mild
Tolerance develops (for cocaine,
tachyphylaxis)
Immediate and long-range toxicity
moderate to high (low for OTCs)
CNS Stimulants
(General Characteristics)
High potential for acute psychiatric
impairment (except OTCs)
 Paranoid psychosis, confusion, violence
 “Crash”: depression, anhedonia
Moderate potential for persistent
psychiatric impairment (Depression,
anhedonia)
CNS Stimulants
(General Characteristics)
Methamphetamine: Potential for acute and
persistent cognitive impairment due to
neurological damage.
CNS Depressants
Barbiturate Hypnotics
Non-Barbiturate Hypnotics
Minor Tranquilizers (benzodiazepines)
Ethyl Alcohol (Ethylene)
Opiates
CNS Depressants
(Barbiturates Hypnotics)
("barbs", "beans", "downers")
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secobarbital (Seconal) ("reds")
pentobarbital (Nembutal) ("yellow jackets")
apobarbital (Alurate)
mephobarbital (Mebaral)
phenobarbital (Luminal)
CNS Depressants
(Non-Barbiturate Hypnotics)
triazalam (Halcion)
ethchlorvynol (Placidyl)
flurazepam (Dalmane)
estazolapam (ProSom)
profol injection (Diprivan)
tempazepam (Restoril)
quazepam (Doral)
CNS Depressants
(Non-Barbiturate Hypnotics)
zolpidem tartrate (Ambien)
Rohypnol (“roofies”)
GHB/gamma hydroxy amino acid (Liquid
G/Somatomax/G-riffic)
CNS Depressants
(Hypnotics)
Addiction potential moderate to high
Physical dependence possible.
Severity of withdrawal = moderate to
high/potentially life-threatening (A & B),
Tolerance develops, but at a different rate for
intoxicating Vs lethal dose
Potential for immediate toxicity = moderate to
high/very high mixed with alcohol
CNS Depressants
(Hypnotics)
Potential for long-range toxicity = mild to
moderate
Potential for immediate and persistent
psychiatric impairment low except for
during withdrawal
CNS Depressants
Minor Tranquilizers (benzodiazepines)
chlorazepam (Tranxene)
chlordiazepoxide (Librium)
clonazepam (Klonopin)
diazepam (Valium)
oxazepam (Serax)
prazepam (Centrax)
alprazolam (Xanax)
lorazepam (Ativan)
Xanax
Valium
Klonopin
CNS Depressants
Minor Tranquilizers (benzodiazepines)
Addiction potential moderate to high
Physical dependence possible.
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High dose/short duration
Low/therapeutic dose/long duration
Severity of withdrawal = low for low
dose/moderate to high for high dose
Tolerance develops
Potential for immediate toxicity = moderate to
high/high when mixed with alcohol
CNS Depressants
Minor Tranquilizers (benzodiazepines)
Potential for immediate toxicity = moderate
to high/high when mixed with alcohol
Potential for long-range toxicity = mild
Potential for immediate psychiatric
impairment = low
Potential for chronic psychiatric
impairment = low
CNS Depressants
(Ethyl Alcohol)
Beer/Wine coolers
Wine
Fortified wines
Distilled spirits
CNS Depressants
(Ethyl Alcohol)
Addiction potential moderate to high
Physical dependence possible.
Severity of withdrawal = moderate to
high/seldom life-threatening
Tolerance develops
Potential for immediate toxicity = moderate
to high
Potential for long-range toxicity = high
CNS Depressants
(Ethyl Alcohol)
Potential for immediate psychiatric
impairment except for alcohol-related
personality change/pathological
intoxication/hallucinosis and psychiatric
impairment during withdrawal
Potential for chronic
psychiatric/neurological = high
CNS Depressants
(Opiates)
Organic/semisynthetic opiates
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opium
codeine (Tylenol/Empirin w/codeine, some Rx
cough syrups)
hydrocodone (Vicodin)
morphine sulfate (M.S.-Contin)
diacetylmorphine (Heroin) ("junk", "smack",
"boy", "chicle", "black tar", "china white")
"Thou has the keys of Paradise, oh just,
subtle and mighty opium"
Thomas de Quincy
Confessions of an English Opium-Eater
Brown & White Heroin
Black Tar Heroin (“El Chicle”)
CNS Depressants
(Opiates)
Synthetic opiates
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oxycodone (Percodan/Percocet/OxyContin)
oxymorphone (Numorphan)
hydromorphone (Dilaudid)
meperidine (Demerol)
oxycodone (Percodan)
dolophine (Methadone)
levorphanol (Levo-Dromoran)
fentanyl (Sublimaze)
CNS Depressants
(Opiates)
Synthetic opiates
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diphenoxylate/atropine (Lomotil)
pentazocine/pentazocine w/ naloxone
(Talwin/Talwin-NX)
"Karachi" (Chicago area): Drug
composition varies. Usually includes an
opiate (ex: Methadone) and at least one
sedative (ex: diazepam, phenobarbital).
OxyContin
Methadone