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
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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
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Cocaine Formulation- other
Freebase
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
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Crack Formulation
Freebase, less dangerous to make
Smoked in special crack pipes
Marketed in single doses
Epidemic in 1980
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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
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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
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Cocaine Absorption
Rapidly absorbed through IV, smoking, intranasal, oral
Short plasma life of 40-60 minutes
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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
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Cocaine Effects on CNS
Euphoria- sense of well being, greater self-esteem, alertness, energy
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Cocaine Physiological Effects
Increased heart rate and increased blood pressure
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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
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Speedball
Cocaine + heroine
Heroine takes the edge of cocaine high
Can result in death if dose is too high
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Cocaethylene
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
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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
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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
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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
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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
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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
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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
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Disulfiram
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
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Current Cocaine Treatment Strategiees
Long term dopamine agonists
GABAb agonist
cocaine vaccine
Bind to DA transporter
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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
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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
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Medical Use Amphetamine
Narcolepsy
ADHD
Weight reduction- limited use for this
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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
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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
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Methylphenidate
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
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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
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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
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Methylphenidate(Concerta)
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
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Methylphenidate and SUD
Through that those with ADHD given drugs would have a higher rate of substance abuse
Study found that two fold lowered risk in having substance use disorder when receiving medication during childhood, as well as a similar decrease in risk in alcohol and other drug abuse disorders
Greater risk of SUD if medications not administered before puberty
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Health Consequences of Cocaine
High abuse liability
Problems at school, work, job
Increased blood pressure can increase strokes
Arrhthmias due to direct effects of the heart
Convulsions typically only occur after high doses
CRACk smoking may damage lung tissue
Cocaine use during pregnancy can harm fetus
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Crack Baby Syndrome
Small heads, agitated, prone to agitation, lack of social skills
Through studies, found confounding issues of alcohol and tobacco, poverty
Cocaine still isn't good for babies, but it is not inevitable that they grow into addicts and criminals
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