Drugs can be beneficial or harmful, depending on the dose, duration and drive. Clearly, the proper dose for one person can be harmful to another. And many drugs are designed to be short-term treatments.
Drive and motivation are often the most important elements in determining usage. But the drugs you take can change your brain chemistry in odd ways. What was rewarding before the drug becomes less rewarding after it. People can end up taking drugs without knowing why they started or why they continue.
Here are my notes on this topic:
1. Drug addiction
- symptoms
- tolerance
- delta-Fos B
- reward system
- cravings
2. Drug administration
- methods
- intravenous (IV)
- intraperitoneal (IP)
- intramuscular
- subcutaneous (SC)
- oral administration
- sublingual
- intrarectal
- inhalation
- topical
- intracerebroventricularl (ICV)
- factors
- lipid solubility
- depot binding
- inactivation-excretion
- dose response curve
- therapeutic index
- half-life
- affinity
- instant recovery
- tolerance
- sensitization
- protagonist
- antagonist
- efficacy
3. Stimulants
- uppers
- analeptics
- psychological dependence
- physical addiction
- euphoria
- heart failure
- anxiety
- facilitate norepinephrine
- counteract fatigue
- suppress appetite
- improve concentration
- Xanthine
- caffeine
- world’s most widely used drug
- added to some medications (reduce drowsiness)
- theobromine
- theophylline
- Nicotine
- crosses BBB
- reaches brain in 10-20 secs
- half-life of 2 hrs
- dose
- rate on inhalation
- tobacco type
- filter
- small concentrations = increase receptor activity
- large concentrations = toxic
- respiratory paralysis
- death
- affinity for melamine
- Cocaine
- “in” drug
- snob appeal
- Amphetamines
- dopamine transport backwards
- symptoms
- grandiose ideas
- rapid eye movement
- jitters
- crash
- itchy skin
- “go pills”
- cheaper
- longer lasting effects
- suicidal thoughts
- withdrawal can last months
4. Depressants
- depress brain activity
- increases dopamine
- blocks glutamate receptors
- downers
- facilitate GABA
- Alcohol
- Type I (type A) alcoholism
- men & women equally
- less genetic
- gradual onset
- late onset (25+ yrs)
- Type II (type B) alcoholism
- before 25
- rapid onset
- more severe
- more genetics
- more men (2-3x)
- Sons of alcoholic mothers
- prenatal environment
- trying to get back to “normal”
- Withdrawal can kill you
- Opioids
- Withdrawal is painful; probably won’t die
- inhibits GAGA
- blocks norepinephrine
- morphine
- codeine
- most widely used opiate
- heroin
- semi-synthetic
- oxycodone
- buprenorphine
- hydromorphone
- intense rush is probably social
- methadone
- to get off heroin
- chronic pain treatment
- Barbiturates
- Benzodiazepines
5. Hallucinogenics
- Psychedelics
- LSD
- serotonin receptors
- at inappropriate times
- for longer than normal
- flashbacks (30%)
- bad trip (anxiety attack)
- Marijuana
- Psilocybin
- Mescaline
- Dissociates
- Schedule I drug
- limits research
- intense sensory experiences
- dopamine release
- impairs ability to form new memories
- impairs ability to shift focus
- alters how info processes in hippocampus
- limits firing of all neurons
- excitatory
- inhibitory
- dream-like or unreal
- don’t recognize self in mirror
- distort reality
- PCP
- angel dust
- Schedule II drug
- ionotropic glutamate receptors (NMDA)
- inhibits nicotinic acetylcholine receptors
- schizophrenia-like symptoms
- Nitrous Oxide
- vapor huffing
- deprives body of oxygen
- euphoria
- seizures
- Ketamine
- DXM
- Deliriants
- Deadly nightshade
- atropine & scopolamine
- Roman eye drops (dilates eyes)
- 2 berries can kill child
- 20 can kill adult
- paralyzes nerve endings
- Jimson weed
- Mandrake
- Nutmeg
- I. Stimulants
- Mostly psychological dependence
- No physiological addiction
- Also called analeptics
- Invigorating or restorative
- Effects
- Temporary improvement in:
- alertness, wakefulness, endurance, productivity & motion
- Referred to “uppers”
- Increased arousal, heart rate & blood pressure
- Perceive less need of food-sleep
- Improved mood, less anxiety
- Euphoria
- Heart failure
- Anxiety
- Most facilitate norepinephrine
- Increase dopamine
- Inhibit transporter (less reuptake)
- Why Taken
- Counteract fatigue
- Make it through work
- Reduce sleepiness
- Treat narcolepsy
- Decrease appetite
- Weight loss
- Treat obesity
- Improve concentration
- work or school; treat ADHD
- Decrease depression
- Treatment-resistant
- Non-typical
- Counteract fatigue
- 10 Common Stimulants
- 1. Xanthine
- Mild stimulants
- Make less sleepy
- Bronchodilators (was used to treat asthma)
- Caffeine Coffee & tea
- Theobromine Chocolate
- Theophylline Tea & chocolate
- Caffeine
- World’s most widely used drug
- Used by 85% of US daily
- Coffee, tea, soda & tablets
- In some medications
- Enhance drug
- Reduce drowsiness
- 2. Nicotine
- Active chemical in tobacco
- Available in:
- cigarettes, cigars
- chewing tobacco
- nicotine patches
- nicotine gum
- electric cigarettes
- Distribution
- Inhaled
- Distributed quickly thru blood
- Crosses blood-brain barrier
- Reaches brain 10-20 secs
- Half-life is 2 hours
- Effects
- Most is burned when smoked
- Enough inhaled to cause pharmacological effects
- Amount absorbed depends on
- Rate of inhalation: none, fast, slow
- Type of tobacco
- Filter
- Nicotonic Ach receptors
- Ganglion nicotinic receptors
- Adrenal medulla
- Brain
- Nicotinic receptor
- In small concentrations
- Increases activity of receptors
- Impacts other neurotransmitters thru in-direct mechanisms
- Volume control
- At toxic levels
- Muscle contractions & respiratory paralysis
- Impacts dopamine
- Dopamine connection is addictive
- Relaxation
- Euphoria
- Nicotine activates SNS (sympathetic nervous system)
- Adrenal medulla
- Stimulates release of epinephrine
- Affinity for melanin
- More dependence
- Harder to stop smoking in darker-pigmented individuals
- Like cocaine
- Repeated use reduces dopamine response to reinforcement
- Some find it helpful to take antidepressants when quitting
- 3. Amphetamines
- Schedule II drug
- High likelihood for dependence
- Used under severe restrictions
- Some accepted medical use
- High potential for abuse
- Increase NE & dopamine
- Inhibits reuptake
- Direct release of nonepinephrine and dopamine from vesicles
- Pushes dopamine into synapse
- Uses dopamine transporter
- Goes thru cell membrane
- Experience
- Elevated mood & euphoria
- Alertness & concentration
- Increased libido
- Higher self-esteem & confidence
- More social interaction
- More energy
- More awake & focused
- Increased weight loss
- Decreased appetite
- Also
- Rebound depression-anxiety
- Dilated pupils & blood shot eyes
- Hyperactive & restless
- Flushing & headaches (vasoconstriction)
- Tachycardia & tremors
- Dry mouth & itchy skin
- Blurred vision, dizziness
- Insomnia
- Fever
- Symptoms
- Talking fast & nervousness
- Rapid eye movements
- “the jitters,” & shifting
- “Munchies”
- Obsessive behaviors
- Grandiose ideas
- Paranoia
- Psychosis
- Might not sleep for several days
- “Crash“
- lying down on floor, go to sleep
- in middle of activity around them
- in middle of a sentence
- Eventually look thin & gaunt; starved
- Cardiac arrest and death
- Often Abused
- Availability
- Fast-acting effects
- Amphetamines kill better than cocaine
- Speed is cheaper & longer lasting
- Cocaine is an “in” drug
- like champagne; snob appeal
- Extremely dangerous when combined with alcohol
- Withdrawal symptoms
- Depression
- Appetite
- Fatigue
- Deep REM sleep
- Suicidal thoughts
- Vivid dreams
- Agitation
- Can last for day or months
- Used in WWII
- Pilots got “go pills“
- II. Depressants
- Depress function or activity in the brain
- Downer
- Pain relief
- Sedatives
- Muscle relaxation
- Use different pharmacological mechanism
- Most facilitate GABA or opioid receptors
- Inhibit glutamate
- Common depressants
- Alcohol
- Opioids
- Barbituates
- Benzodiazepines
- Depress function or activity in the brain
- 1. Alcohol
- Effects
- Inhibits sodium flow across cell membrane
- More sodium in the cells expands membrane
- Decreases serotonin activity
- Increases dopamine activity
- Blocks glutamate receptors
- Facilitates GABA
- Effects
- Alcoholism
- Type A (Type I)
- Fewer genetic relatives with alcoholism
- Men and women about equally
- Later onset (usually after 25)
- Generally less severe
- Gradual onset
- Type B (Type II)
- Earlier onset (before 25)
- More rapid onset, more severe
- More genetic relatives with alcoholism
- Far more men than women
- Genetic predisposition
- 9% of population
- Unpredictable variables
- Quantity, frequency & regularity
- Risk factors
- Social environment
- Emotional health
- Sensation seeking
- Genetics
- Sons of alcoholic mothers
- After moderate drinking
- Feel less drunk, have less body sway
- Show less change in EEG
- Feel less tense
- Smaller than normal amygdala
- Connects emotions to senses
- Get brain chemistry back to “normal”
- Sons of alcoholic mothers
- Stress
- Gender
- Men 2-3 times more likely
- Women more impacted by long-term use
- Age = Under 16
- Hangovers
- 50% of Chinese-Japanese have gene that slows metabolism of acetaldehyde
- Increases effects of hangover
- Makes hangover immediate
- Less alcoholics
- High rate of suicide in alcoholics & drug abusers
- Distortion of brain chemistry
- Social isolation
- Intoxicated (not thinking clearly)
- 1 in 4 teen suicides is alcohol abuse related
- More crimes
- Abuse, rape, burglaries, assaults
- Chronic use
- Symptoms similar to mental illness when drunk
- When not
- Severe anxiety
- Depression
- Type A (Type I)
- 2. Opioids
- Types
- Natural
- Morphine
- Codeine
- Semi-synthetic opiates
- Heroin
- Synthetic opiates
- Methadone
- Natural
- Highly additive
- Increases release of endorphins
- Decreases pain
- Inhibits GABA
- Causes increase in dopamine
- Blocks release of norepinephrine
- Psychological dependence
- Physical addiction
- Withdrawal not usually fatal
- Tolerance
- Used To Treat
- Post-operative pain
- Cancer pain
- Rheumatoid arthritis
- Morphine
- Treats acute and chronic pain
- Heart pain
- Labor pain
- Lasts 3-4 hrs
- Abusers don’t have a preference for morphine or heroin
- Codeine
- Most widely used opiate
- 3-methylmorphine
- natural isomer of methylated morphine
- Used To Treat
- Mild-moderate pain
- Relieve cough
- Diarrhea & irritable bowel syndrome
- Abused
- Phenergam with codeine
- Anti-nausea medication
- Semi-synthetic opiates
- Oxycodone
- Buprenorphine
- Hydromorphone
- Heroin
- Diacetylmorphine or morphine diacetate
- Synthesized from morphine
- Schedule I drug
- Effects
- “transcendent relaxation”
- Euphoria
- Tolerance quickly develops
- Users perceive it has different effects from morphine
- Intense rush
- Probably not physical; social
- Synthetic opiates
- Meperidine/pethidine
- Fentanyl
- Methadone
- Compared to morphine or heroin
- Chemically different
- Acts on same receptors
- Use To Treat
- Chronic pain
- Maintenance drug for heroin reduction
- Types
- III. Hallucinogenics
- Subjective perceptual changes
- Disrupt
- Thinking, emotion, consciousness
- Induce experiences
- Not just enhance
- 1. Psychedelics
- LSD
- Stimulates serotonin receptors
- at inappropriate times
- for longer than normal duration
- Marijuana
- Leaves contain THC
- intensify sensory experience
- Impacts release of dopamine
- Impairs ability to form new memories
- Impairs ability to shift focus
- Disrupts coordination and balance
- Binds to receptors in cerebellum and basal ganglia
- Impairs ability to learn new skills
- Dance, sports or driving
- Alters how info processed in hippocampus
- Doesn’t affect breathing and heart rate as many substances
- Only few receptors in medulla & brain stem
- Limits firing of all neurons
- Both excitatory and inhibitory
- Hypothalamus doesn’t increase appetite when starving
- Disrupts sense of time
- Stays in system for 4 weeks
- Leaves contain THC
- LSD
- 2. Dissociatives
- Feel detached from the environment
- Feel dream-like or unreal
- “out of body”
- Don’t recognize self in mirror
- Ketamine
- DXM
- PCP
- angel dust
- Schedule II drug
- Impacts ionotropic glutamate receptors
- NMDA receptors
- also inhibits nicotinic acetylcholine receptors
- NMDA receptors
- Brain damage
- Schizophrenia-like symptoms
- “embalming fluid” = cigarette dipped in PCP
- Effects
- Varies by dose
- Loss of ego boundaries
- Paranoia
- Hallucinations
- Suicidal impulses
- Nitrous Oxide
- Colorless, sweet, non-flammable gas
- Laughing gas or sweet air
- Oxide of nitrogen
- Oxidizer in rocketry
- Aerosol spray propellant
- Street names: whip-its, poppers or snappers
- Vapor is “huffed“
- Deprives body of oxygen
- Euphoric effect
- Seizures
- 3. Deliriants
- Examples
- Deadly nightshade
- Jimson weed
- Mandrake
- Nutmeg
- Effects
- Stupor, confusion, confabulation
- Disrobing and plucking
- Conversation with imagined people
- Don’t recognize self in mirror
- Examples