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Flashcards in Cocaine and Amphetamine Deck (34)
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Cocaine Formulation- Powder

Cocaine hydrochloric salt
White flakes, or powdery form
Relatively stable, transports well
Dissolves easily in water
Intranasal and intravenous routes
Most common form
Often "cut" with many chemicals until final product is 12% cocaine


Alduterants to Cocaine

Mannitol- Mild baby laxative, low toxicity
Inositol- B vitamin, harmless but irritates nasal passages
Lidocaine- "active" adulterant is also a local anesthetic so difficult to detect; no euphoria but is self administered
PPA- phenylpropanolamine, an OTC nasal decongestant, high toxicity at high doses
Lactose- harmless, cheap and easy to get


Cocaine Formulation- other

Pure alkaloid waxy paste becomes oil
Not very stable, breaks down easily
Dissolves in lipid or fat
Must be smoked
Special small pipes are used


Crack Formulation

Freebase, less dangerous to make
Smoked in special crack pipes
Marketed in single doses
Epidemic in 1980


Cocaine Mechanism of Action

Dopamine is released --> Cocaine blocks reuptake inhibitors --> Increased dopamine levels in the synapse - Positive reinforcement Blocks sodium ion channels in the cell


Medical Uses- Cocaine

Schedule II
Local anesthetic for ophthalmic surgery and testing due to direct blockade on nerve impulses
Very effective in nasal, laryngeal and esophagus mucus membranes
Causes vasoconstriction, reduces bleeding
Can cause positive urine screening 2 days later
CNS energizing use ended due to short duration of action, rapid tolerance, dependence and side effects


Cocaine Absorption

Rapidly absorbed through IV, smoking, intranasal, oral
Short plasma life of 40-60 minutes


Cocaine Metabolism

Plasma and liver esterases metabolizes cocaine
50% metabolized within an hour
Rapid rise and fall of cocaine plasma levels causes a crash, leaves user wanting more


Cocaine Effects on CNS

Euphoria- sense of well being, greater self-esteem, alertness, energy


Cocaine Physiological Effects

Increased heart rate and increased blood pressure


Cocaine Patterns of Use

Chippers- Occasional use
"Binge"- finish all cocaine available
Other behaviors reduce- sleep, eating, sexual
If supply is limited than human and animals use until death
Crash at the end of use



Cocaine + heroine
Heroine takes the edge of cocaine high
Can result in death if dose is too high



Cocaine + Ethyl Alcohol
Major metabolite benzoylecgonine is transesterified by ethanol to produce this
More toxic than cocaine and may contribute to overdoses when cocaine is used with alcohol


Tolerance- Cocaine

Unclear whether there is tolerance or sensitization
Sensitization to locomotor, stereotypic behaviors and convulsions
Tolerance to constant use
Sensitization- interval in between uses
No tolerance to blood pressure effects


Withdrawal- Cocaine

Thought that dependence did not occur
Abstinence causes crash, intense craving to cocaine
Individual will sleep and eat, but depressed, thoughts consumed by cocaine
More rapid of a crash= more frequent use


Treatment Cocaine

No approved medications, trials still being conducted
New knowledge of how the brain is changed by cocaine provides newer targets, ex- disturbes GABA glutamate balance
D3 receptors constitute novel molecular target of high interest
vigabatrin- anti- epileptic
modafinil- anti-nacrolepsy
tiagabine- anti-epileptic
disulfiram- ALDH inhibitor


Programs cocaine

Contingency Management and/or Motivational Incentive Program
Voucher or based prize system that rewards people from abstaining for cocaine
Drug free urine tests --> points or chips that can be exchanged for healthy lifestyle prizes


Phases of Cocaine Withdrawal

Crash (24-48 hr)- agitated, depressed, suicidal, fatigue/exhaustion, no cravings
Withdrawal (1-10 weeks) mood swings, sleep returns, anhedonia, drug seeking anxiety
Extinction (indefinite)- mood swing, cue induced cravings


Stimulant- Cocaine

Slow release form of cocaine should reduce cocaine use
Transdermal path or transbccal
Open trial of oral cocaine tea was found effective in Peru
Not likely to be accepted



Inhibits dopamine-beta-hydroxylase
Patients with normal DBH dropped from a 84 to a 56, while patients with a low DBH genotype had no disulfiram effect
DBH genotype of a patient could be used to identify whether nor not treatment may be effective


Current Cocaine Treatment Strategiees

Long term dopamine agonists
GABAb agonist
cocaine vaccine
Bind to DA transporter


Cocaine Vaccine

Antibodies made to cocaine
Likely an adjunct treatment
Need 47% of the DA transporter to be occupied for cocaine to feel effects
Vaccine reduces this to 20%
Cocaine antibodies persist for one year
Cocaine use was lower after subjects had received higher dose vaccine- needs further testing


Profile of Use Amphetamine

Primarily diverted legal tablets that were meant for prescription use
Similar effects as cocaine, longer duration of action because metabolized slowly
Different mechanism of action
Injected as speed and d-methamphetamine


Medical Use Amphetamine

Weight reduction- limited use for this


Designer Amphetamine

Chemically similar to amphetamine
Underground chemist alter structure to have psychoactive effects
Very common in 1970s and 1980s
Because they were not amphetamine, they were not illegal, made illegal in 1986


Amphetamine Mechanism of Action

Amphetamine enters terminal, causes dopamine to be released from terminal
Dopamine concentrations in synapse increases and continue to bind to receptor



Non-Amphetamine behavioral stimulant
Used primarily to treat ADHD
Blocks reuptake of dopamine- similar to cocaine
Promotes dopamine release- like amphetamine
Sluggish effect, takes 60% to block 50% of the transporter, accounts for lower abuse liability


Ritalin Abuse

Growing trend for non-medical use for individuals without a prescription
Derived from belief that it is a cognitive enhancer- increases learning and memory


Trends of Ritalin Abuse

White male college students
In frats and sororities
NE United States, more competitive admission rates
More likely to also report abuse of alcohol, drugs, and ecstasy

Studies also show that it does not increase learning capacity or memory
Only promotes wakefulness, alertness, reduces sleep



Recently developed but has taken over 40% of the ADHD market
Once a day treatment
MPH coating, rigid membrane covering high concentration MPH with a hole drilled through