Pharmacology of stimulants, depressants, and hallucinogens

Dr. Dawn-Elise Snipes PhD, LPC-MHSP, NCC

 Define stimulants, depressants and
hallucinogens
 Discuss their
◦ Mechanism of action
◦ Symptoms of intoxication
◦ Symptoms of withdrawal
◦ Short and long term effects
◦ Common street names
 Differential diagnosis

 Method of administration greatly effects the
intensity and duration of onset for various
drugs
◦ Oral (slowest)
◦ Inhalation/Snorting
◦ Inhalation/Smoking
◦ Injection
◦ Rectal suppository
◦ Skin patches
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 Drugas affect everyone differently, based on:
◦ Size, weight and health
◦ Whether the person is used to taking it
◦ Whether other drugs are taken concurrently
◦ The amount taken
◦ The strength of the drug (varies from batch to
batch with illegally produced drugs)

 Stimulants are substances that act to excite
the central nervous system
◦ Caffeine
◦ Amphetmines
◦ Cocaine

 Stimulants increase alertness, attention, and
energy, as well as elevate blood pressure,
heart rate, and respiration.
 Used to treat asthma and other respiratory
problems, obesity, neurological disorders,
ADHD, narcolepsy, and occasionally
depression

 Stimulants enhance norepinephrine and
dopamine.
 Increase in dopamine can induce a feeling of
euphoria when stimulants are taken
nonmedically.
 Norepinepherine also increases blood pressure
and heart rate, constricts blood vessels, increases
blood glucose, and opens up breathing passages.

 Mechanism of action
◦ Increase noradrenaline/norepinepherine &
dopamine in the brain in 4 ways
 Bind to the presynaptic membrane causing the
release of dopamine
 Interact with dopamine containing synaptic vesicles,
releasing free dopamine into the nerve terminal

 Mechanism of action
◦ 4 ways cont…
 Bind to monoamine oxidase in dopaminergic
neurons and prevent the degradation of
dopamine, leaving free dopamine in the nerve
terminal
 Bind to the dopamine re-uptake transporter,
causing it to act in reverse and transport free
dopamine out of the nerve terminal.

 Generalized State Of
Euphoria
 Increased Energy
 Confidence
 Mental Alertness
 Sexual Arousal
 Itching And
Scratching
 Large Pupils
 Dry Mouth
 Fast Heart Beat And
Breathing
 Teeth Grinding
 Reduced Appetite
 Excessive Sweating

 In the 4 to 6 days after stimulant use, the
following effects may be experienced:
◦ Restless sleep and exhaustion
◦ Headaches
◦ Dizziness and blurred vision
◦ Paranoia, hallucinations and confusion
◦ Irritability, mood swings and depression
◦ Anxiety
◦ Insomnia

 Methamphetamine has a substantially longer
half-life than cocaine, thus leading to more
intense and protracted withdrawal.
 Chronic methamphetamine users may have
episodes of violent behavior, paranoia,
anxiety, confusion, and insomnia.

 A study in April, 2015 analyzed 21 supplements
labelled as containing Acacia rigidula, a type of
shrub native to Texas.
◦ Eleven of them were found to contain beta-
methylphenylethylamine, or BMPEA, an isomer of
amphetamine whose effect on humans has never been
studied.
◦ Only 3 in which the chemical was found indicated its
presence on their labels, and none of them specified the
amount of BMPEA in each pill, according to the study.
http://onlinelibrary.wiley.com/doi/10.1002/dta.1793/abstract
 DoD list of Supplements to Avoid

 Toxic doses, over 5 grams per day for an
adult,
◦ A cup of coffee contains 80–175 mg of caffeine,
depending on the bean and preparation method
◦ Redbull: 80mg
◦ Monster: 86mg
◦ Starbucks (short) brewed coffee 8oz: 180mg
◦ Stacker II (1capsule) 200mg
◦ Vivarin (1 tablet) 200mg

 Possible side effects for stimulants, include:
◦ Hostility
◦ Paranoia
◦ Psychotic symptoms
◦ Unsafely elevated body temperature
◦ Irregular heartbeat, heart failure
◦ Seizures
◦ Exacerbation of existing anxiety

 Reduced appetite
 Restless sleep
 Dry mouth/dental
problems
 Reduced immunity
 Trouble concentrating
 Difficulty breathing
 Muscle stiffness
 Anxiety and paranoia
 Depression & Suicidal
Ideation
 Heart/kidney problems
 Increased risk of stroke
 Tolerance
 Confusion
 Sexual dysfunction
 Chest pain or palpitations
 Seizures and delirium

 Amphetamines
◦ R-ball
◦ Skippy
◦ The smart drug
◦ Vitamin R
◦ Kibbles and bits
◦ Speed
◦ Truck drivers
◦ Bennies
◦ Black beauties
◦ Crosses
◦ Hearts
◦ LA turnaround
◦ Uppers
◦ Amps
◦ Pick-me-ups
 Cocaine and Crack
◦ coke
◦ Snow
◦ 8-ball
◦ flake
◦ powder
◦ dust
◦ candy
◦ white
◦ kryptonite
◦ cookies
◦ strong
◦ Speedball is cocaine + heroin

 Depressants exert the opposite effect of
stimulants.
◦ They s-l-o-w everything down

 Mechanism of Action
◦ Depressants exert their effects through a number of
different pharmacological mechanisms, the most
prominent of which include facilitation of GABA,
and inhibition of glutamatergic or monoaminergic
(dopamine, noradrenaline and serotonin) activity

 Types include
◦ Barbiturates (Sedatives, -barbitals)
◦ Benzodiazapines (-lam, -pam)
◦ Inhalants (Aerosols, paint, gasoline, glue)
◦ Muscle relaxants
◦ Non-Benzodiazapine hypnotics (Lunesta, Sonata)
◦ Opiates

 Americans use
◦ 80% of global opioid supply
◦ 99% of global hydrocodone
 Direct healthcare costs are 8.7x higher for
opiate abusers
 Annual cost of opioid abuse
◦ 2001: $8.6 Billion
◦ 2007: $55.7 Billion

 Class of Drugs: Analgesic (pain killer); CNS
Depressant, antitussive (cough suppressant)
 Types of Drugs
◦ Natural
◦ Synthetic
◦ Semi-synthetic.

 Opiates may be detected in urine for 2-4 days
 Heroin contains acetylcodeine
 Codeine is metabolized to morphine, both
substances may appear in the urine following
codeine ingestion
 Oxycodone does not produce a positive response
to routine screens for opiates, which generally
target morphine and/or codeine

 If patients are taking opiates or benzos for a
medical purpose, send urine to the lab and
monitor levels.
 Buprenorphine can be abused, although it has a
ceiling effect.
 Buprenorphine needs to have it’s own test as it
produces a unique metabolite.
 Suboxone is buprenorphine + naloxone and is
harder, but not impossible to abuse

 Short term impact (up to 5 hours)
◦ Depends heavily on the dose of morphine or heroin, the
route of administration, and previous exposure
◦ Including
 Psychological: Euphoria, feeling of well-being, relaxation,
drowsiness, sedation, disconnectedness, delirium.
 Physiological: Analgesia, depressed heart rate and
respiration depression, constipation, flushing of the skin,
sweating, pupils fixed and constricted, diminished reflexes

 Complications and Side Effects
◦ Medical complications among abusers arise
primarily from adulterants and in non-sterile
injecting practices
◦ Include skin, lung and brain abscesses, collapsed
veins, endocarditis, hepatitis and HIV/AIDS.

 Complications and Side Effects
◦ Alcohol or depressants such as benzodiazepines,
hypnotics, and antihistamines increase the CNS
effects of opiates such as:
 Sedation/drowsiness
 Decreased motor skills.
 Respiratory depression, hypotension

 Long term impact
◦ Vein collapse
◦ Depression
◦ Brain changes/damage
◦ Reduction of the production of natural pain killers

 Symptoms of intoxication
◦ Constricted pupils
◦ Agitation
◦ Scratching and picking

 Symptoms of withdrawal
◦ Begin within 6-12 hours; last 5-10 days; peak
between 48-72 hours
◦ Yawning
◦ Drug Craving
◦ Irritability/dysphoria/depression
◦ Flu like Symptoms: Runny nose, sweating. vomiting,
chills, abdominal cramps, body aches, muscle and
bone pain, muscle spasms, insomnia.

 Detoxification Issues
◦ Tolerance decreases rapidly, so overdosing during
relapse is easy
◦ Biggest focus during opiate withdrawal is to provide
palliative care
◦ In general, opiate withdrawal is not life threatening

 Current state of Use/Abuse
◦ Fentanyl is 30-50x stronger than heroin. Overdose
rates are
◦ Difficulty getting prescription opioids has led to
increases in demand for heroin
◦ Nearly 6% of 12th graders report using narcotics
other than heroin for recreational purposes

 Class of Drugs: Antianxiety/Depressant
◦ Sedative, hypnotic (sleep-inducing), anxiolytic (anti-
anxiety), anticonvulsant, and muscle relaxant properties.
 Types of Drugs
◦ Short acting
◦ Long Acting
 Benzodiazepines enhance the effect of the
neurotransmitter gamma-aminobutyric acid
(GABA) at the GABAA receptor

 Ingestion of therapeutic dosages may be detectable
for 1-3 days while extended usage over a period of
months or years can extend excretion times up to 4-
6 weeks after cessation of use
 Different tests are required to identify different
benzos
 benzodiazepines such as alprazolam (Xanax®),
lorazepam (Ativan®), and clonazepam (Klonopin®) do
not share this metabolic pathway

 Due to individual differences between people
and drugs, a standard therapeutic level is
often hard to identify
 Many abusers accentuate the effects of
benzodiazepines by the using alcohol or
other CNS depressants

 Short term impact
◦ Drowsiness
◦ Blurred vision
◦ Poor coordination
◦ Amnesia
◦ Hostility/Irritability
◦ Disturbing dreams
◦ Reduced inhibition
◦ Impaired judgment

 Short term impact in the elderly
◦ Confusion
◦ The appearance of dementia
◦ Benzodiazepine overdose
 Combining with other depressants has an
exponential additive effect
 Rohypnol is a benzodiazepine

 Long term impact
◦ Impairment in several cognitive domains, such as
visuospatial ability, speed of processing, and verbal
learning J Clin Psychiatry. 2005;66 Suppl 2:9-13.
◦ Benzodiazepine use for 3 months or more was
associated with an increased risk of Alzheimer's
disease of up to 51%. Benzodiazepine use and risk
of Alzheimer’s disease: case-control study BMJ
2014; 349

 Symptoms of withdrawal
◦ Sleep disturbance
◦ Irritability, increased tension and anxiety, panic attacks,
hand tremor, sweating, palpitations
◦ Difficulty in concentration
◦ Dry heaves and nausea, headache, muscular pain and
stiffness
◦ Seizures
◦ Psychosis

◦ Symptoms appear around the end of the half-life
period
◦ Rebound anxiety and insomnia peak within a couple
of days
◦ Withdrawal symptoms can last for 2-4 weeks
depending on the drug
◦ Protracted withdrawal is not uncommon in heavy
and/or long-term users.

◦ “A grand mal seizure may occur in as many as 20-30% of
individuals undergoing untreated withdrawal from these
substances.” Diagnostic and Statistical Manual of Mental Disorders, 5th Ed.
◦ Flumazenil (Romazicon) is a competitive antagonist that
can reverse the sedative and overdose effects of
benzodiazepines but not of alcohol or other sedative-
hypnotics. (SAMHSA TIP 45)

 Current state of Use/Abuse
 Most frequently used class of drugs for
anxiety disorders. An estimated past year
prevalence of use in the USA has been
reported at 12.9% Archives of Clinical Neuropsychology Volume 19, Issue 3,
April 2004, Pages 437–454

 GHB (gamma-Hydroxybutyric acid)
◦ Acts on GHB and GABAB Receptors
◦ Some athletes also use GHB, as GHB has been
shown to elevate human growth hormone
◦ Date-rape drug

 Non-benzodiazepine sleep medications, such as
Ambien, Lunesta, and Sonata, have a different
chemical structure, but act on some of the same
brain receptors as benzodiazepines.
 Barbiturates (-barbitals) i.e. phenobarbital are
used to reduce anxiety or to help with insomnia.
◦ Readily available in many hospice-involved patients

 Inhalants
◦ Types
 Paint and paint thinners
 Markers
 Glues
 Shoe polish
 Gasoline
 Cleaning fluids
 Aerosols

 Herbs and Supplements
◦ Valerian
◦ Melatonin
◦ Passion Flower
◦ GABA
 Muscle relaxants (Flexeril)
 Atypical antipsychotics (Seroquel, trazadone)
 Mood stabilizers (Depakote)

Barbs
Candy
Downers
Phennies
Reds
Red Birds
Sleeping pills
Tooies
Tranks
Yellows
Yellow Jackets

 Hallucinogens are a class of drugs that cause
hallucinations—profound distortions in a
person’s perceptions of reality.
 Hallucinogens can be found in some plants and
mushrooms (or their extracts) or can be man-
made
 Commonly divided into two broad categories
◦ classic hallucinogens (such as LSD)
◦ dissociative drugs (such as PCP).

 Hallucinogens interfere with the action serotonin and/or
glutamate, which regulate:
◦ Mood
◦ Sensory perception and response
◦ Sleep
◦ Hunger
◦ Body temperature
◦ Sexual behavior
◦ Muscle control
◦ Pain perception
◦ Learning and memory

◦ PCP (Phencyclidine)—
 Also known as ozone, rocket fuel, love boat, hog,
embalming fluid, or
 Usually sold as a liquid or powder.
 PCP can be snorted, smoked, injected, or swallowed.

 Ketamine—also known as K, Special K, or cat Valium—is
odorless and tasteless and has amnesia-inducing and
dissociative properties. (Can facilitate sexual assault.)
 DXM (Dextromethorphan)—also known as robo—is a cough
suppressant and expectorant
 Salvia divinorum—also known as diviner’s sage, Maria
Pastora, Sally-D, or magic mint—is a psychoactive plant
typically ingested by chewing fresh leaves or by drinking their
extracted juices.

 LSD (d-lysergic acid diethylamide)
◦ AKA: acid, blotter, doses, hits, microdots, sugar cubes, trips, tabs,
or window panes
◦ Potent mood & perception-altering hallucinogenic drugs
◦ It is a clear or white, odorless, water-soluble material
◦ Produced as
 Tablets known as “microdots”
 Thin squares of gelatin called “window panes.”
 Diluted with water or alcohol and sold in liquid form.
 LSD-soaked paper punched into small individual squares, known as
“blotters.”

 Peyote (Mescaline)
◦ Also known as buttons, cactus, and mesc—
◦ Is a small, spineless cactus with mescaline as its
main ingredient.
◦ The top, or “crown,” of the peyote cactus has disc-
shaped buttons that are cut out, dried, and usually
chewed or soaked in water to produce an
intoxicating liquid.

 The effects of hallucinogens can begin within 20 to 90 minutes
and can last as long as 6 to 12 hours.
 Other short-term general effects include:
• Increased heart rate
• Nausea
• Intensified feelings and
sensory experiences
• Changes in sense of time
(for example, time passing
by slowly)
• Increased bp, respiration,
or body temperature
• Loss of appetite
• Dry mouth
• Sleep problems
• Mixed senses (such as
"seeing" sounds or
"hearing" colors)
• Spiritual experiences
• Feelings of relaxation or
detachment
• Uncoordinated
movements
• Excessive sweating
• Panic
• Paranoia—extreme and
unreasonable distrust
• Psychosis—disordered
thinking detached from
reality

 Repeated use of PCP can result in long-term
effects that may continue for a year or more
after use stops, such as:
◦ speech problems
◦ memory loss
◦ weight loss
◦ anxiety
◦ depression and suicidal thoughts

 Though rare, long-term effects of some
hallucinogens include the following:
◦ Persistent psychosis—a series of continuing mental
problems, including:
 visual disturbances
 disorganized thinking
 paranoia
 mood changes
 Flashbacks—recurrences of certain drug experiences.
hallucinogen persisting perceptual disorder (HPPD).

 Stimulants range from caffeine to methamphetamine and “amp
up” the system
 Opiates, benzodiazepines, barbiturates, alcohol, inhalants are all
CNS depressants
 Combinations of depressants have an exponential additive effect
 Evaluate patients for exposure to all CNS depressants intentional
and incidental
 Hallucinogens include LSD, PCP, Peyote, Ketamine and
Dextromethorphan
 Recent research has indicated that HPPD is not due to “traces of
the drug being freed up”

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Pharmacology of stimulants, depressants, and hallucinogens