Exam 2: Cocaine Flashcards

1
Q

produce modest stimulatory effects in the CNS

nicotine, caffeine, not scheduled

A

low-efficacy stimulants

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2
Q

increase CNS activity by a significant amount
strong behavioral effects
addiction liability greater
abuse potential inc

A

high-efficacy stimulants

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3
Q

cocaine

A

psychoactive substance extracted from leaves of coca plant

  • coca leaves have 0.6-1.8% cocaine
  • coca paste extracted from soaked and mashed leaves has 60-80% cocaine
  • discovered and processed in 1860s

cocaine created from coca paste

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4
Q

2nd most abused controlled substance

A

cocaine

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5
Q

what schedule drug is cocaine

A

schedule 2 drug

  • high potential for abuse
  • known established medical uses
  • severe psychological or physical dependence liability
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6
Q

major current problem with cocaine

A

lack of purity!!
it is laced with ther substances only 50% is actually cocaine
- phentanol is a common laced substance - lethal = toxic

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7
Q

forms of cocaine

A

cocaine salt, cocaine HCl : mixture of coca paste with HCl, readily water soluble

basic cocaine:
- freebase: dissolve cocaine HCl and ammonia, extract cocaine and ether (organic solvent)

crack: dissolve cocaine HCl mix with baking soda, heat, dry

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8
Q

absorption of cocaine

A

route of administration:

  • nasal (insufflation, snorting) - cocaine HCl
  • IV injection, mainlined
  • inhalation, smoking
  • oral - rare since poor bioavailability
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9
Q

nasal absorption of cocaine HCl

- bioavailability, onset of action, peak levels in brain, duration of action

A

bioavailability: 70%
onset: 30s-5min - snorting cocaine constricts blood vessels, slowing the absorption
peak in brain: 10-20 min
duration of action: 60-90 min

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10
Q

injection absorption of cocaine HCl

bioavailability, onset of action, peak levels in brain, duration of action

A

bioavailability: 90%
onset: 10-60s
peak in brain: 3-5min
duration of action: 20-60 min

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11
Q

another absorption f cocaine HCl besides nasal and injection

A

topical

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12
Q

inhalation absorption - freebase/crack cocaine

bioavailability, onset of action, peak levels in brain, duration of action

A

bioavailability: 90%
onset: 1-2s
peak in brain: 10s-30min
duration of action: 5-15 min

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13
Q

distribution of cocaine

A

cocaine = lipophillic - easily penetrates BBB and placental barrier

brain concentrations FAR exceed blood plasma levels
- important for addiction - bc of the speed

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14
Q

metabolism of cocaine

A

rapidly broken down in about 2 hrs

by enzymes in BLOOD and liver into metabolites

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15
Q

cocaine metabolites

A

benzoylecognine - broken down in bloodstream, inactive metabolite

ecgnonine methyl ester - broken down in liver - inactive metabolite

norcocaine - active metabolite broken down in liver - cytochrome p450s
- acute intoxication

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16
Q

metabolism: alcohol and cocaine

A

alcohol slows cocaine metabolism

react together to form cocaethylene - greater effects than cocaine

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17
Q

cocaethylene

A
  • only known example where body forms new psychoactive compound from 2 others
  • longer half life, but lower LD50
  • more euphoria, increased cardiac toxicity
  • seizures, liver damage, compromised immune system
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18
Q

elimination of cocaine

A

-SLOWLY removed from brain but RAPIDLY removed from blood

1-5% excreted unchanged in urine

rapid fall of blood cocaine level: rush followed by a crash

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19
Q

half lifes cocaine

IV, nasal, benzoylecognine

A

IV half life: 30-90min
Nasal: 30min-4.5 hr
Benzoylecognine: 14.5-52 hrs - detected in urine 2-3 days later if nasal, if chronic IV can detect for up to 10 days

20
Q

speed runs

A

to get the rush and avoid withdrawal
- short half life - snort every 40 min or inject every hr
=blood levels accummulate to toxic levels
- run continues until out of drug or something bad happens - seizure, overdose, heart stops

21
Q

eyes of a cocaine user

A

dilated!!!

sympathetic response

22
Q

stimulants are sympathomimetic - what does this mean?

A

they produce symptoms of sympathetic nervous system activation: dilated pupils, inc HR, vasoconstriction, hypertension, hyperthermia

low doses not harmful, high doses toxic or fatal

23
Q

what are some acute behavioral effects

A
feelings of exhilaration or euphoria
sense of wellbeing
inc alertness and energy
great self-confidence
inc aggression - not good impulse control 

immediately after smoking or IV: intense rush that is pleasurable
after oral or intranasal: euphoria without the rush - not as exhilarating

24
Q

behavioral effects of chronic cocaine use

A

panic attacks - sympathetic activation

temporary paranoid psychosis:

  • hallucinations of touch, sight, taste, smell
  • confusion, anxiety
  • formication syndrome: people think bugs crawling all over their skin - may take chunks out of their skin
25
Q

physiological effects of chronic cocaine use

A

malnutrition and weight loss due to appetite suppression in sympathetic activation

snorting: cocaine HCl
- septal necrosis (tissue in nose dies off) or perforated septum (hole on inside of nose)

26
Q

vasoconstriction brain interrupts… which can lead to ….

A

blood flow to brain

stroke

27
Q

cocaine blocks what reuptake transporters

A

DA, NE, 5-HT

28
Q

cocaine has highest binding affinity for

A

5-HT

but DA is most important for reinforcing and addictive properties

29
Q

cocaine increases…

A

DA in the nucleus accumbens indirectly through PFC

30
Q

glutamate neurons in the PFC ecite

A

DA neurons in the VTA

31
Q

more NE leads to

A

inc glutamate and inc activation of VTW dopamine neurons

32
Q

what is PET imaging used for

A

estimates DAT occupancy by cocaine

once a certainminimum level is reached the subject may feel a high

33
Q

intensity of the high depends on

A

amount of DAT occupancy

  • rate at which DAT occupancy occurs - distribution speed
  • baseline level of DA activity in mesolimbic pathway
34
Q

increased NE levels activates

A

arousl centers and sympathetic nervous system - dilates pupils

35
Q

increased DA lvels associated with

A

euphoria, inc energym psychosis, sense of confidence

36
Q

at high concentrations, cocaine inhibits…

A

voltage gated NA channels in axons, blocking nerve conduction

37
Q

when cocaine is applied locally what does it act a

A

anesthetic

prevents transmission of signals along sensory nerves

38
Q

what two numbing agents were developed from cocaine

A

procaine (novacaine) and lidocaine (xylocaine)

39
Q

when using occaine most start by what route of administration

A

smoking

40
Q

abstinence syndroe and cocaine (3steps)

A

crash: user feels exhausted and depressed mood
withdrawal: anhedonia, anergia, anxiety, crave cocaine
extinction: symptoms subside

41
Q

intermittent access to self administered cocaine causes

A

behavioral sensitiztion instead of tolerance

42
Q

sensitization is more likely following _______ in brain as opposed to high, constant concentrations

A

repeated spikes

43
Q

disulfiram

A

used to treat alcoholism showing promise in clinicl trials since people frequently use cocaine and alcohol together
it prevents conversion of DA to NE
inc DA prevents cocaine cravings by blocking withdrawal effects

44
Q

cocaine vaccine

A

cocaine is attached to a toxin
immune system produces antibodies aainst toxin and cocaine
prevents cocaine from reaching brain
no high - lose interest

45
Q

cognitive behavioral therapyy (CBT)

A

restrcting thught processes and training perso to avoid their triggers

46
Q

structural abnormalities in chronic cocaine users

A
PFC
ACC
insula
dorsal striatum
amygdala
thalamus
47
Q

functional changes in chronic cocaine users

A

impulse control and working memory - PFC
verbal learning an memory - temporal lobe
performance on psychomotor tasks - dorsal striatum
decision making - PFC