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

Neuroscience Week 7: ADHD and Stimulant Drugs Flashcards

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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
Amphetamine-like CNS actions
26
Amphetamine-like drugs side effects 6 listed
* decreased sense of fatigue * increase in motor activity and mental alertness * mild euphoria * brighter spirits * mild anorexic effect * insomnia
27
Dextroamphetamine structure
is the d-isomer of amphetamine and is twice as potent a CNS stimulator on a weight basis than racemic amphetamine
28
Dextroamphetamine compared to other catecholamines
has a greater CNS-stimulating activity than epinephrine or other catecholamines
29
Dextroamphetamine clinical uses
* Narcolepsy * ADD * ADHD
30
Methylphenidate MOA
Blocks DAT and NET leading to increased DA and NE
31
Methylphenidate structure and properties
* chemically similar to amphetamine * peripheral pharmacologic actions are milder than those of the amphetamines
32
Methylphenidate clinical uses
* 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
33
Modafinil MOA
Increases DA and NE by blocking transporters but may also increase excitatory glutaminergic transmission
34
Modafinil addictive potential
* lower addictive potential * can mitigate cocaine dependence
35
Modafinil side effects
* 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
Can mitigate cocaine dependence
Modafinil
37
Stimulant-like drugs Pharmacokinetics 4 listed
38
Question
39
Amphetamine (stimulant) like agents Side effects and contraindications
40
Amphetamine (stimulant) like agents Somatic Side effects
* 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
Amphetamine (stimulant) like agents Neurologic Side effects 5 listed
* Hallucinations * Psychosis * Tics * Tourette's Syndrome * Seizure
42
Amphetamine (stimulant) like agents Cardiovascular Side effects
* 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
Amphetamine (stimulant) like agents and MAOI
can be a risk of serotonin syndrome and avoid in patients on MAOI
44
Amphetamine (stimulant) like agents Cardiovascular
recommend all children with ADHD have a thorough cardiovascular assessment prior to initiation of drug therapy
45
Atomoxetine structure and description
a SNRI and the first-nonstimulant drug approved for attention-deficit hyperactivity disorder
46
Atomoxetine is strucutrally similar to?
Fluoxetine
47
Atomoxetine promiscuity
minimal affinity for other neurotransmitter's transporters or receptor sites
48
Atomoxetine abuse potential
no potential for abuse and is not classified as a controlled substance
49
Atomoxetine cardiovascular concerns
* safe in adolescents and children * Little effect on CV
50
Atomoxetine clinical use
considered an alternate ADHD therapy in patients where psychostimulants are not an option
51
Question
B.
52
Atomoxetine Pharmacokinetics
* rapidly absorbed from the GI tract * Cmax 1-2 hours
53
Atomoxetine side effects: Children
* Nausea/Vomiting * anorexia or a decrease in appetite * Dizziness and growth suppression
54
Atomoxetine Side effects: Adults 8 listed
* Headache * sleepiness * dizziness * irritability * change in libido * erectile and ejaculatory dysfunction * menstrual changes * urinary dysfunction
55
Atomoxetine GI Side effects
* dry mouth * Nausea * abdominal pain * Vomiting * serious liver problems (increased hepatic enzymes and bilirubin
56
Atomoxetine serious risks
increased risk of suicidal ideation (children and adolescents)
57
Atomoxetine Cardiovascular
* 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
Atomoxetine avoid in patients with?
Narrow angle Glaucoma
59
Bupropion AKA
* -Zyban * Wellbutrin
60
Bupropion description
* Antidepressant drug of the aminoketone class * NOT a tricyclic antidepressant and is unrelated to other known antidepressants
61
Bupropion MOA
* 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
Bupropion structurally similar to
Amphetamine
63
Bupropion avoid in patients with?
Taking MAOIs
64
Bupropion Off-label use
Neuropathic pain
65
Bupropion orthostatic hypotension
well tolerated in patients experiencing orthostatic hypotension with TCAs Does not inhibit MAO
66
Bupropion other effects
moderate anticholinergic effects and produces a mild local anesthesia on the oral mucosa
67
Bupropion clinical uses
* smoking cessation * off-label addiction to smokeless tobacco * off-label multiple neurological/psychological uses * off-label neuropathic pain
68
Bupropion Pharmokinetics
69
Bupropion GI Side effects
* Dry mouth * constipation * Nausea * Vomiting * Weight loss * Weight gain * Anorexia
70
Bupropion Neurologic Side effects
* headache * insomnia * sedation * agitation * Blurry vision * Tremor * greater potential for causing seizures (dose-dependent)
71
Bupropion Sympathetic Side effects
* excessive sweating * increased heart rate
72
Bupropion neuropsychiatric Side effects 6 listed
* confusion * delusions * hallucinations * psychotic episodes (psychosis) * paranoia * suicidal thoughts
73
Clonidine and Guanfacine MOA
Centrally acting α2 adrenoreceptor agonists
74
Clonidine and Guanfacine Clinical uses
* used primarily for the treatment of systemic hypertension * ADHD
75
Clonidine and Guanfacine Halflife
16 hrs
76
Clonidine and Guanfacine maximum concentration
3 hrs
77
Clonidine and Guanfacine​ metabolism
Guanfacine is a substrate of CYP3A4/5 and exposure is affected by CYP3A4/5 inducers/inhibitors
78
Clonidine and Guanfacine caution
caution in patients taking Ketoconazole and other strong CYP3A4/5 inhibitors
79
Clonidine and Guanfacine general Side effects
* dry mouth * sedation * weakness * dizziness * constipation * impotence * urinary incontinence * conjunctivitis * paresthesia * dermatitis
80
Clonidine and Guanfacine Cardiovascular side effects
* risk of rebound hypertension is low but it can occur * hypotension * bradycardia * syncope * palpitations * substernal pain
81
Clonidine and Guanfacine selectivity
* Sedation and somnolence is associated with 2b and 2C activity of clonidine * Guanfacine is more specific to 2A only
82
Question
83
What should I know?
84
ADHD risk of developing dementia
3X higher

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