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Psychopharmacology > Lecture 11: Psychostimulants > Flashcards

Lecture 11: Psychostimulants Flashcards

1
Q

3 therapeutic effects of psychostimulants

A
  1. local anesthetic
  2. ADHD treatment
  3. narcolepsy
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2
Q

how do stimulants exert their behavioral effect? where?

A

augmenting DA action

activity in NA

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3
Q

low dose effects of PS induce ___

A

behavior-activating response akin to normal emergency reaction (sympathomimetic drugs)

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4
Q

3 physiological effects of sympathomimetic drugs

A
  1. increased BP and HR
  2. blood flow shifts from skin and organs to muscles
  3. oxygen and blood glucose levels rise
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5
Q

4 positive CNS effects of PS

A
  1. elevated mood
  2. reduced fatigue/increased energy
  3. decreased appetite
  4. improved task performance
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6
Q

3 negative effects of PS

A

anxiety
irritability
insomnia

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7
Q

3 high dose negative effects of PS

A

anxiety
irritability
psychotic behavior

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8
Q

PS used historically for 5 reasons

A
  1. endurance
  2. sense of wellbeing
  3. reduce fatigue
  4. increased stamina
  5. alleviate hunger
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9
Q

cocaine is the ___ most popular illegal drug in US

A

2nd

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10
Q

estimated cocaine market in US exceeds ____

A

$70 billion

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11
Q

Harrison Narcotic Act

A

1914; banned incorporation of cocaine into medicines and beverages

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12
Q

cocaine related ER visits were second only to ___

A

illicit drug use combined with alcohol

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13
Q

3 types of cocaine

A

E. coca leaves
Cocaine HCl
Cocaine base (crack, freebase)

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14
Q

crack is soluble in (3)

A

alcohol
acetone
ether

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15
Q

% cocaine in coca paste

A

60-80%

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16
Q

% cocaine in E. coca leaves

A

1%

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17
Q

how many mgs of cocaine per line?

A

25mg; snort 50-100mg at a time

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18
Q

how much of cocaine HCl is absorbed through snorting? what inhibits it?

A

20-30%

cocaine is a vasoconstrictor

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19
Q

plasma level peak of cocaine

A

30-60 min

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20
Q

how long does cocaine persist in plasma?

A

6 hours

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21
Q

for smoked cocaine freebase, absoprtion is ___

A

rapid and complete

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22
Q

onset and persistance of smoked freebase

A

5 min; 30 min

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23
Q

onset of IV powder cocaine

A

30-60s

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24
Q

cocaine metabolite. how long can it be detected in urine?

A

benzoylecgonine

detected in urine 48h after use; 2 weeks in chronic users

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25
Q

when combined with alcohol, cocaine is metabolized to…

A

cocaethylene

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26
Q

effects of cocaethylene (3)

A
  1. can be more active/longer lasting than cocaine
  2. blocks DA reuptake transporter
  3. increases risk of toxicity
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27
Q

cocaine MoA

A

potentiates actions of DA and 5HT by blocking active reuptake

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28
Q

mice lacking ___ do not self administer cocaine

A

dopamine reuptake transporter

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29
Q

8 low-dose cocaine effects

A
  1. alertness
  2. motor hyperactivity
  3. tachycardia
  4. vasoconstriction
  5. hypertension
  6. bronchodilation
  7. increased blood glucose levels
  8. blood flow shift to muscles
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30
Q

cocaine psychological response first 30 min

A
  1. euphoria

2. enhanced self-consciousness and boastfulness

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31
Q

cocaine psych response next 60-90 min

A

mild euphoria mixed with protracted anxiety

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32
Q

8 risks/complications of acute cocaine use

A
  1. racing thoughts/speech
  2. depression
  3. suppressed appetite
  4. delayed sleep
  5. movement disorders
  6. seizures
  7. depletion of oxygen (cerebral ischemia)
  8. intracranial hemorrhage
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33
Q

toxic paranoid psychosis (4)

A
  1. anxiety
  2. sleep deprivation
  3. repetitive compulsive behavior
  4. altered perception of reality, violent responses to imagined persecution
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34
Q

cocaine psychosis (8)

A
  1. paranoia
  2. impaired reality testing
  3. stereotyped, compulsive, repetitive behavior
  4. vivid hallucinations
  5. irritability
  6. extreme psychomotor activation
  7. impaired relationships
  8. disturbances in eating and sleeping
35
Q

how old do cocaine dependent people tend to be?

A

12-39 years

36
Q

cocaine users are usually dependent on at least ___ drugs

A

3

37
Q

___ of cocaine users are male

A

75%

38
Q

on personality tests, cocaine users tend to be (4)

A

reckless
rebellious
low tolerance for frustration
craving for excitement

39
Q

___ of cocaine users have anxiety disorders

A

30%

40
Q

___ of cocaine users are clinically depressed

A

67%

41
Q

___ of cocaine users exhibit paranoia

A

25%

42
Q

cocaines vasoconstrictive effects can cause what in the fetus? (3)

A
  1. increased blood pressure
  2. intracerebral hemorrhage
  3. premature birth
43
Q

fetus exposure to cocaine can lead to (2) later in life

A
  1. behavioral/emotional problems

2. increased vulnerability to substance use in adolescence

44
Q

when cocaine crosses the placental barriers, can lead to (2)

A
  1. destructive brain lesions

2. sudden infant death syndrome

45
Q

effects of cocaine neurotoxicity (3)

A
  1. psychomotor slowing and slowed reactions
  2. subclinical brain damage; early onset demention
  3. upregulation of heat shock protein expression, causes damage in BBB
46
Q

3 pharmacological strategies in cocaine dependency

A
  1. block euphoria
  2. reduce withdrawal/depressive symptoms
  3. enhance PFC cortical projections
47
Q

compounds that regulate ____ are in early clinical trial for cocaine dependency (2 examples)

A

glu transmissions from frontal cortex to VTA and NA

topiramate and lamotrigine

48
Q

7 drugs for cocaine dependency

A
  1. disulfiram (antabuse, blocks aldehyde dehydrogenase)
  2. naloxone (opiate antag)
  3. methylphenidate
  4. wellbutrin
  5. modafinil
  6. antidepressants (not SSRIs)
  7. antiepileptic neuromodulators (increase GABA by inhibiting GABA transminase enzyme; attenuates DA levels in NA and reduces cravings)
49
Q

3 problems with cocaine vaccine

A
  1. need enough antibodies to bind to all bloodstream cocaine
  2. long lasting needed to reduce number of readministrations
  3. vaccine should be well tolerated
50
Q

only ___ of those vaccinated for cocaine attained high enough antibody levels

A

38%

51
Q

MoA of amphetamine (3)

A
  1. DA and NE release from presynaptic nerve terminals

2. amphet causes transporters to run in reverse, leading to release of vesicular DA into cytoplasm and synaptic cleft

52
Q

what causes stereotypical, repetitive, compulsive behavior from amphetamines?

A

increased DA in basal ganglia

53
Q

4 low dose effects of amphet

A
  1. increased BP and HR
  2. increased alertness, euphoria, excitement, wakefulness
  3. loss of appetite
  4. improved task performance
54
Q

4 moderate dose effects of amphet (not BP/HR, alertness/euphoria, appetite loss, task perform)

A
  1. tremors/restlessness
  2. worsening production of anxiety disorders/panic disorders/obsessive behavior
  3. paranoid psychosis
  4. insomnia
55
Q

6 chronic use, high dose effects of amphet (not anxiety, insomnia, tremors)

A
  1. stereotypical behaviors
  2. sudden violent outbursts
  3. paranoid delusions
  4. severe anorexia/weight loss
  5. skin sores from neglected healthcare
  6. indirect negative fx by poor eating and sleeping
56
Q

2 withdrawal symptoms of amphet?

A
  1. increased appetite/weight gain

2. severe depression

57
Q

methamphetamine can be easily synthesized from obtainable chemicals like ___

A

pseudoephedrine

58
Q

ice

A

crystalline, smokable form of meth (like crack)

59
Q

half life of meth

A

12 hours

60
Q

2 high dose effects of meth

A

violent behavior

paranoid/psychotic behavior

61
Q

2 effects of meth repeated dosing

A
  1. long lasting decrease in DA and 5HT in brain from damage to 5HT and DA nerve terminals
  2. neuronal death; replacement with astroglia and microglia
62
Q

chronic meth use has what 4 effects on the brain?

A
  1. reduces hippocampal volume
  2. increases size of ventricles
  3. decreases gray matter
  4. increases white matter
63
Q

how does meth cause BBB breakdown? what are the effects?

A

causes hyperthermia

increases numbers of WBCs in brain, initiating neuronal damage

64
Q

6 nonamphet behavioral stimulants

A
  1. ephedrine
  2. pseudophedrine
  3. ritalin
  4. provigil (modafinil)
  5. nuvigil (armodafinil)
  6. kat
65
Q

use of ephedrine

A

anesthesiology to increase BP

releases epinephrine, elevating BP and heart rate

66
Q

use of pseudoephedrine

A

used to relieve nasal congestion

67
Q

2 actions of ritalin

A
  1. blocks presynaptic DA transporter

2. slightly increases DA release

68
Q

after 60 min of oral admin, ritalin effect is ___

A

blocks 50% of DA transporters

69
Q

what accounts for low rate of positive reinforcement from ritalin?

A

slow uptake into brain

70
Q

modafinil MoA (2)

A
  1. blocks dopamine transporter

2. elevation of hypothalamic histamine levels

71
Q

3 FDA approved uses of modafinil

A
  1. narcolepsy
  2. shift-work sleep disorder
  3. obstructive sleep apnea
72
Q

khat; how is it consumed?

A

east african flowering shrub

can be chewed or brewed as tea

73
Q

3 effects of khat

A
  1. excitement
  2. loss of appetite
  3. euphoria
74
Q

active ingredients in khat

A
  1. cathinone

2. cathine

75
Q

what does cathinone do?

A

increases DA levels in CNS

76
Q

what does cathine do?

A

mild psychostimulant

77
Q

differences in cocaine vs. amphetaine action

A
  1. cocaine: potentiates action of DA and sereotonin by blocking active reuptake
  2. amphetamine: causes release of DA from vesicles and cause DAT to run in reverse
78
Q

effects of meth related 5HT damage (3)

A
  1. anxiety
  2. depression
  3. aggression
79
Q

DA damage from meth use makes users vulnerable to ___

A

neurodegenerative disorders like parkinson’s

80
Q

what 3 parts of the brain are most damaged by meth BBB breakdown?

A

most severe in

  1. amygdala,
  2. hippocampus, and
  3. caudate-putamen
81
Q

where does cocaine increase DA activity?

A

nucleus accumbens

82
Q

where does amphetamine increase DA activity?

A

nucleus accumbens

83
Q

meth MoA (2)

A
  1. release of DA from vesicles

2. causes DAT to run in reverse

Psychopharmacology (22 decks)

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