Cocaine and Amphetamine Flashcards by Adhana Asfaw

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

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

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

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

Narcolepsy
ADHD
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

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

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

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

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

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

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

Toxic Psychosis

Dose related progression from nervousness, aggression, irritability, tremors Acute psychotic reaction that resembles schizophrenic psychosis Typically occurs in chronic users Urine screen for differential diagnosis Supportive treatment