Exam 3 - Amphetamines and Cocaine Flashcards

1
Q

What accounted for the rise and fall of meth use?

A

its changes in potency

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2
Q

What are amphetamine and cocaine?

A

stimulants

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3
Q

What are amphetamines structurally similar to?

A

dopamine

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4
Q

Khat/Cathinone

A
  • active components are cathinone and cathine
  • stimulant properties similar to amphetamine and cocaine
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5
Q

Bath salts

A
  • synthetic cathinone
  • 10x more powerful than cocaine
  • triggers release of dopamine
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6
Q

MDPV

A
  • main ingredient in bath salts, detected in urine of users
  • first synthesized in 1968 to counteract chronic fatigue
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7
Q

What are the desired effects of bath salts?

A
  • euphoric high with a rush
  • appetite suppression
  • study aid
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8
Q

What are the adverse effects of bath salts?

A
  • combative
  • hallucinations
  • hyperthermia
  • anxious/paranoia
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9
Q

Ephedrine

A
  • comes from ephedra
  • only use today is anesthesiology to increase BP
  • can be toxic/fatal when combined with other stimulants
  • pseudoephedrine used in cough and cold medicines
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10
Q

Basic pharmacology of amphetamines

A
  • absorption from GI tract is slow, I.V. is rapid
  • methamphetamine is more potent than amphetamine
  • amphet and metham are metabolized by liver at slow rate
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11
Q

What are amphetamines mechanism of action?

A
  • release DA independently of an action potential, and also releases NE and DA
  • block reuptake of NE and DA
  • addiction comes from the release of DA in the mesolimbic pathway
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12
Q

What are the behavioral effects of amphetamines?

A
  • confident
  • highly alert/don’t sleep
  • low appetite
  • improves performance on simple repetitive tasks
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13
Q

What are the psychological effects of amphetamines?

A
  • sympathomimetic agents - mimic actions of epinephrine
    • sympathetic nervous system (increase HR, BP, RR, dilate pupils)
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14
Q

What are the therapeutic uses of amphetamines?

A
  • narcolepsy
  • obesity - suppresses appetite
  • ADHD - causes release of DA in areas that control attention
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15
Q

Tolerance/Dependence of amphetamines

A
  • reverse tolerance of motor effects
  • withdrawal symptoms include: increased appetite/weight gain, decreased energy, increased need for sleep (amphets block REM)
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16
Q

Amphetamine psychosis

A
  • psychotic reaction occurring in substantial number of high dose users
  • resembles paranoid schizophrenia (hallucinations, behavioral disorganization, paranoia, formication - picking at skin)
17
Q

Neurotoxicity of amphetamines

A
  • neuronal death of both dopaminergic and serotonergic neurons in animal models
18
Q

Cocaine

A

stimulant that comes from the coca plant

19
Q

What were the leaves of E. coca used for historically? When was the active alkaloid isolated? What was this alkaloid named?

A
  • increase endurance/stamina, promote sense of well being, induce euphoria
  • 1850’s
  • cocaine
20
Q

Coca paste was combined with hydrochloric acid to form:

A

less potent, water soluble salt cocaine hydrochloride

21
Q

Who typically uses cocaine? Why do they use it?

A
  • young males that are typically dependent on other drugs
  • tend to have coexisting psychopathology that they are self-medicating for
22
Q

What are the two ways that cocaine is absorbed?

A
  • snorted, slow absorption, low concentration in blood
  • inhalation and IV, rapid absorption, high concentration in blood
23
Q

Distribution of cocaine

A
  • penetrates brain rapidly, initial brain concentrations exceed blood concentrations
  • freely crosses the placental barrier
24
Q

Metabolism and excretion of cocaine

A
  • biological half-life of 20-90 minutes
  • major metabolite is benzoylecgonine, makes cocaethylene
25
Q

What does cocaine do?

A
  • potent local anesthetic
  • vasoconstrictor
26
Q

What are the adverse effects of cocaine

A
  • convulsions/seizures
  • hemorrhagic stroke (vasocontrictor and also a stimulant)
  • cardiac arrhythmias
27
Q

What are some consequences of use of cocaine during pregnancy?

A
  • everything that can happen to mom can happen to baby
  • premature birth
  • respiratory distress
  • cerebral infarctions
  • seizures
28
Q

What are the 3 phases of withdrawal of cocaine?

A
  • crash (1-14 days): intense craving, exhaustion, agitation
  • withdrawal (1-10 weeks): intense craving, mod to severe depression, inability to feel normal pleasure
  • extinction (months to years): cravings occurs by exposure to environment cues
29
Q

Mechanism of action of cocaine

A
  • blocks reuptake of DA, NE and 5-HT
30
Q

Baseline DA release of reinforcing effects of psychostimulants

A
  • b/c cocaine doesn’t cause release of DA, it depends on the baseline levels of DA
  • body begins to compensate by releasing less and less DA
31
Q

Neurotoxicity of cocaine

A
  • damage axon terminals: change memory function
  • predisposition to early onset dementia/parkinson’s
32
Q

What are some medicinal treatments for cocaine dependency?

A
  • dopaminergic agonists to treat withdrawal symptoms, relapse, and craving (disulfiram, antabuse)
  • antidepressants (tricyclic like despiramine)
  • Gamma-vinyl-GABA for anti-craving effects (inhibit endorphin areas that become excited w/ use)
33
Q

What are some new approaches to cocaine dependency treatment?

A
  • dopamine reuptake inhibitors to reduce craving and relapse
  • cocaine vaccine: antibody that will bind to and inactivate cocaine, slow entry to brain and inhibit euphoria
    - can be overridden by taking more cocaine