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Neuroscience > Neuroscience Week 7: ADHD and Stimulant Drugs > Flashcards

Neuroscience Week 7: ADHD and Stimulant Drugs Flashcards

1
Q

Uses of stimulants

4 main categories

A
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2
Q

ADHD was first identified in?

A
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3
Q

What structures are affected by ADHD?

A
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4
Q

What impairs PFC cognitive abilities?

A
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5
Q

ADHD pharmacology drug classes

4 listed

A
  • Stimulants
  • NE uptake inhibitior
  • α2 adrenergic agonists
  • antidepressants
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6
Q

Stimulants to treat ADHD

3 listed

A
  • Methylphenidate
  • D-amphetamine
  • Modafinil
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7
Q

NE Uptake inhibitor to treat ADHD

A

Atomoxetine (Strattera)

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8
Q

α2 adrenergic agonists to treat ADHD

A

Guanfacine

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9
Q

Antidepressants to treat ADHD

A

Bupropion

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10
Q

Methylphenidate AKA

2 listed

A
  • Ritalin
  • Metadate
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11
Q

Methylphenidate MOA

A
  • DAT Blocker
  • increases extracellular DA/NE by blocking reuptake (DAT and NET)
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12
Q

D-Amphetamine AKA

3 listed

A
  • Adderall
  • Dextrostat
  • Methamphetamine HCL
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13
Q

D-Amphetamine MOA

A
  • Desoxyn: DA/NE releaser taken up into vesicles
  • Increases extracellular DA by triggering transporter (DAT and NET) reversal
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14
Q

Modafinil AKA

A

Provigil

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15
Q

Modafinil MOA

A

inhibits NET and DAT (also increases 5HT and GABA levels (structurally different from amphetamine)

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16
Q

Atomoxetine AKA

A

Strattera

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17
Q

Atomoxetine MOA

A
  • Selective NET blocker
  • increases extracellular NE via reuptake blockade (non-stimulant)
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18
Q

Guanfacine MOA

A

Selective NE α2A receptor agonist

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19
Q

Bupropion MOA

A

unicyclic antidepressant (resembles amphetamine) elevates NE via NET

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20
Q

Amphetamine-like stimulants

4 listed

A
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21
Q

Stimulants like ADHD drugs are likely to?

A
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22
Q

Stimulant site of action

A
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23
Q

Question

A
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24
Q

Amphetamine-like agents CNS effects

4 listed

A
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25
Q

Amphetamine-like CNS actions

A
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26
Q

Amphetamine-like drugs side effects

6 listed

A
  • decreased sense of fatigue
  • increase in motor activity and mental alertness
  • mild euphoria
  • brighter spirits
  • mild anorexic effect
  • insomnia
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27
Q

Dextroamphetamine structure

A

is the d-isomer of amphetamine and is twice as potent a CNS stimulator on a weight basis than racemic amphetamine

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28
Q

Dextroamphetamine compared to other catecholamines

A

has a greater CNS-stimulating activity than epinephrine or other catecholamines

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29
Q

Dextroamphetamine clinical uses

A
  • Narcolepsy
  • ADD
  • ADHD
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30
Q

Methylphenidate MOA

A

Blocks DAT and NET leading to increased DA

and NE

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31
Q

Methylphenidate structure and properties

A
  • chemically similar to amphetamine
  • peripheral pharmacologic actions are milder than those of the amphetamines
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32
Q

Methylphenidate clinical uses

A
  • more noticeable effects on mental function than on motor activities
  • narcolepsy
  • ADHD
  • post-stroke depression
  • strong effect on measures of attention
  • distractibility
  • impulsivity
  • social and classroom behavior
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33
Q

Modafinil MOA

A

Increases DA and NE by blocking transporters but may also increase excitatory glutaminergic transmission

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34
Q

Modafinil addictive potential

A
  • lower addictive potential
  • can mitigate cocaine dependence
35
Q

Modafinil side effects

A
  • Rare cases - serious/life-threatening rash, including Stevens-Johnson Syndrome (Erythema multiforme an allergic reaction)
  • Toxic Epidermal Necrolysis (TEN)
  • Drug rash with Eosinophilia and systemic symptoms (DRESS) have been reported in adults and children
36
Q

Can mitigate cocaine dependence

A

Modafinil

37
Q

Stimulant-like drugs Pharmacokinetics

4 listed

A
38
Q

Question

A
39
Q

Amphetamine (stimulant) like agents Side effects and contraindications

A
40
Q

Amphetamine (stimulant) like agents Somatic Side effects

A
  • Problems sleeping
  • decreased appetite
  • Nausea
  • Weight loss
  • Headache
  • Growth suppression in children
  • Height and weight should be monitored
  • Use with caution or avoid in patients with glaucoma
41
Q

Amphetamine (stimulant) like agents Neurologic Side effects

5 listed

A
  • Hallucinations
  • Psychosis
  • Tics
  • Tourette’s Syndrome
  • Seizure
42
Q

Amphetamine (stimulant) like agents Cardiovascular Side effects

A
  • increase systolic and diastolic blood pressure or respiratory stimulation
  • at higher dosages and in overdose: heart rate may increase or reflexively decrease in response to blood pressure
  • Cardiac arrhythmias may occur secondary to increased sympathomimetic effects
  • sudden cardiac death especially where there are structural abnormalities
43
Q

Amphetamine (stimulant) like agents and MAOI

A

can be a risk of serotonin syndrome and avoid in patients on MAOI

44
Q

Amphetamine (stimulant) like agents Cardiovascular

A

recommend all children with ADHD have a thorough cardiovascular assessment prior to initiation of drug therapy

45
Q

Atomoxetine structure and description

A

a SNRI and the first-nonstimulant drug approved for attention-deficit hyperactivity disorder

46
Q

Atomoxetine is strucutrally similar to?

A

Fluoxetine

47
Q

Atomoxetine promiscuity

A

minimal affinity for other neurotransmitter’s transporters or receptor sites

48
Q

Atomoxetine abuse potential

A

no potential for abuse and is not classified as a controlled substance

49
Q

Atomoxetine cardiovascular concerns

A
  • safe in adolescents and children
  • Little effect on CV
50
Q

Atomoxetine clinical use

A

considered an alternate ADHD therapy in patients where psychostimulants are not an option

51
Q

Question

A

B.

52
Q

Atomoxetine Pharmacokinetics

A
  • rapidly absorbed from the GI tract
  • Cmax 1-2 hours
53
Q

Atomoxetine side effects: Children

A
  • Nausea/Vomiting
  • anorexia or a decrease in appetite
  • Dizziness and growth suppression
54
Q

Atomoxetine Side effects: Adults

8 listed

A
  • Headache
  • sleepiness
  • dizziness
  • irritability
  • change in libido
  • erectile and ejaculatory dysfunction
  • menstrual changes
  • urinary dysfunction
55
Q

Atomoxetine GI Side effects

A
  • dry mouth
  • Nausea
  • abdominal pain
  • Vomiting
  • serious liver problems (increased hepatic enzymes and bilirubin
56
Q

Atomoxetine serious risks

A

increased risk of suicidal ideation (children and adolescents)

57
Q

Atomoxetine Cardiovascular

A
  • patients with hypertension or cardiac abnormalities should be closely observed while on Atomoxetine as it can increase blood pressure and heart rate
  • Avoid in patients with narrow angle Glaucoma
58
Q

Atomoxetine avoid in patients with?

A

Narrow angle Glaucoma

59
Q

Bupropion AKA

A
  • -Zyban
  • Wellbutrin
60
Q

Bupropion description

A
  • Antidepressant drug of the aminoketone class
  • NOT a tricyclic antidepressant and is unrelated to other known antidepressants
61
Q

Bupropion MOA

A
  • Inhibitor of neuronal uptake of NE
  • Some activity at SE and DA reuptake
  • Bupropion and its amphetamine-like active metabolites inhibit dopamine and norepinephrine transport
  • The blockade of NE and 5HT reuptake at the neuronal membrane but also SERT actions are weaker for bupropion than for tricyclic antidepressants
62
Q

Bupropion structurally similar to

A

Amphetamine

63
Q

Bupropion avoid in patients with?

A

Taking MAOIs

64
Q

Bupropion Off-label use

A

Neuropathic pain

65
Q

Bupropion orthostatic hypotension

A

well tolerated in patients experiencing orthostatic hypotension with TCAs

Does not inhibit MAO

66
Q

Bupropion other effects

A

moderate anticholinergic effects and produces a mild local anesthesia on the oral mucosa

67
Q

Bupropion clinical uses

A
  • smoking cessation
  • off-label addiction to smokeless tobacco
  • off-label multiple neurological/psychological uses
  • off-label neuropathic pain
68
Q

Bupropion Pharmokinetics

A
69
Q

Bupropion GI Side effects

A
  • Dry mouth
  • constipation
  • Nausea
  • Vomiting
  • Weight loss
  • Weight gain
  • Anorexia
70
Q

Bupropion Neurologic Side effects

A
  • headache
  • insomnia
  • sedation
  • agitation
  • Blurry vision
  • Tremor
  • greater potential for causing seizures (dose-dependent)
71
Q

Bupropion Sympathetic Side effects

A
  • excessive sweating
  • increased heart rate
72
Q

Bupropion neuropsychiatric Side effects

6 listed

A
  • confusion
  • delusions
  • hallucinations
  • psychotic episodes (psychosis)
  • paranoia
  • suicidal thoughts
73
Q

Clonidine and Guanfacine MOA

A

Centrally acting α2 adrenoreceptor agonists

74
Q

Clonidine and Guanfacine Clinical uses

A
  • used primarily for the treatment of systemic hypertension
  • ADHD
75
Q

Clonidine and Guanfacine Halflife

A

16 hrs

76
Q

Clonidine and Guanfacine maximum concentration

A

3 hrs

77
Q

Clonidine and Guanfacine​ metabolism

A

Guanfacine is a substrate of CYP3A4/5 and exposure is affected by CYP3A4/5 inducers/inhibitors

78
Q

Clonidine and Guanfacine caution

A

caution in patients taking Ketoconazole and other strong CYP3A4/5 inhibitors

79
Q

Clonidine and Guanfacine general Side effects

A
  • dry mouth
  • sedation
  • weakness
  • dizziness
  • constipation
  • impotence
  • urinary incontinence
  • conjunctivitis
  • paresthesia
  • dermatitis
80
Q

Clonidine and Guanfacine Cardiovascular side effects

A
  • risk of rebound hypertension is low but it can occur
  • hypotension
  • bradycardia
  • syncope
  • palpitations
  • substernal pain
81
Q

Clonidine and Guanfacine selectivity

A
  • Sedation and somnolence is associated with 2b and 2C activity of clonidine
  • Guanfacine is more specific to 2A only
82
Q

Question

A
83
Q

What should I know?

A
84
Q

ADHD risk of developing dementia

A

3X higher

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