Stimulants and ADHD Flashcards

1
Q

What are the uses of stimulants?

A
  • Counteract lethargy and fatigue
  • Reduce sleepiness/keep awake when necessary; treat narcolepsy
  • Decrease appetite and promote weight loss
  • Improve focus and concentrations at school/work
  • Used off-label to treat depression
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2
Q

What are some examples of stimulants?

A
  • Xanthines (purine derivative)
  • Nicotine
  • Amphetamines
  • MDMA
  • Cocaine
  • NRIs & NDRIs
  • Methylphenidate to treat ADHD
  • Modafinil, Adrafinil, & Armodoafinil (drugs for narcolepsy)
  • Yohimbine (alpha1, and alpha2 antagonist)
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3
Q

ADHD

A

People with ADHD show a persistent pattern of inattention with/or hyperactivity/impulsivity that interferes with functioning or development

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4
Q

What are some symptoms of inattention?

A
  • Often fails to close attention to details or makes careless mistakes
  • Often has trouble holding attention on tasks or play activities
  • Often does not seem to listen when spoken directly
  • Often does not follow through on instructions and fails to finish schoolwork
  • Often has trouble organizing tasks and activities
  • Often avoids, dislikes, or is reluctant to do tasks that require metnal effort over a long period of time
  • Often loses things necessary for tasks and activities
  • Is often easily distracted
  • Is often forgetful in daily activities
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5
Q

What are the symptoms of hyperactivity and impulsivity?

A
  • Often fidgets with or taps hands or feet, or squirms in seat
  • Often leaves sat in situations when remaining seated is expected
  • Often runs about or climbs in situations where it is not appropriate
  • Is often “on the go” activiting as if “driven by a motor”
  • Often talks excessively
  • Often blurts out an answer before a question has been completed
  • Often has trouble waiting his/her turn
  • Often interrupts or intrudes on others
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6
Q

What are the diagnostic criteria of ADHD for children less than 17 years of age?

A

> = 6 symptoms of inattention and/or >= 6 symptoms of hyperactivity-impulsivity, for 6 months prior to assessment and inappropriate for development level

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7
Q

What are the diagnostic criteria of ADHD for adults and adolescents age 17+?

A

> = 5 symptoms of inattention and/or >=5 symptoms of hyperactivity-impulsivity, for 6 months prior to assessment and inappropriate for developmental level

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8
Q

What does the MRI and PET studies show in regards to neuroanatomical changes in ADHD?

A

DECREASE activation in prefrontal cortex, especially right side, and parts of the corpus callosum and basal ganglia
and lower levels of dopamine function in striatum and prefrontal cortex

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9
Q

What does the functional neuroimaging show in regards to neuroanatomical changes in ADHD?

A

DECREASED activation of medial prefrontal cortex

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10
Q

What is the correlation between motivational deficits and dopamine function in the nucleus accumbens?

A

The more D2/D3 and DAT present, the better the motivation score

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11
Q

What are the psychostimulants?

A
  • Methylphenidate
  • Amphetamine
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12
Q

Which antidepressants treat ADHD?

A
  • Atomoxetine
  • Bupropion
  • Tricyclic antidepressants
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13
Q

What central alpha2-adrenergic agonists treat ADHD?

A
  • Clonidine
  • Guanfacine
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14
Q

What is the MOA of amphetamines?

A
  • Indirect-acting sympathmimetic drugs that promote of endogenous bioamines including dopamine (DA) & norepinephrine
  • Produce their effects by causing intracellular release from vesicles, thus reversing the action of biogenic amine transporters at the plasma membrane, resulting in transmitter release
  • Enter the cell via DAT transporter
  • Inside the cell amphetamine interferes with the vesicular monoamine transporter (vMAT)
  • This depletes synaptic vesicles of DA and NE
  • Levels of DA or NE increase in the cytoplasm causing reversal of the DAT direction and release of neurotransmitter into the synapse
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15
Q

Dextroamphetamine (Dexedrine, DextroStat)

A
  • DEA schedule II
  • Duration: about 5 hrs
  • Equally effective as methylphenidate
  • Used mostly for children intolerant to methylphenidate
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16
Q

What are the disadvantages of Amphetamine compound (Adderall)?

A
  • Potential for abuse
  • Appetite suppression
  • May exacerbate symptoms in psychotic children
  • May exacerbate hypertension
  • Growth suppressant
  • Insomnia
17
Q

What is the dosage of Amphetamines in children age 6 and older?

A
  • Start with 5 mg once or twice daily (adults may start at 10 mg)
  • May increase to 5 mg weekly intervals until optimal dose is obtained
  • Give first dose on awakening
  • Additional doses at interval of 4 or 6 hours
18
Q

What does the Adderall XR capsule contain?

A
  • Dextroamphetamine Saccharate: 2.5 mg
  • L-amphetamine aspartate monohydrate: 2.5 mg
  • Dextroamphetamine sulfate USP: 2.5 mg
  • L-amphetamine sulfate USP: 2.5 mg
19
Q

What is the PK of Adderall XR?

A
  • Half life: 9-14 hrs depending isomer
  • Well absorbed
  • 15-40% bound
  • Renal excretion
20
Q

Lisdexamfetamine dimesylate (Vvyanse)

A
  • Prodrug of D-amphetamine
  • Approved by the FDA for ADHD
  • Rapidly absorbed from GI tract and converted to D-amphetamine
21
Q

What are the doses of amphetamine toxicity?

A
  • Adults: 20-25 mg/kg
  • Children: as low as 1.5 mg/kg
22
Q

What are the symptoms of amphetamine toxicity?

A
  • Talkativeness
  • Euphoria
  • Agitation
  • Confusion
  • Pupillary dilation
  • Bruxism (teeth grinding)
23
Q

Methylphenidate

A
  • DEA schedule II
  • Increases dopamine and norepinephrine levels by blocking reuptake transporters
24
Q

What is the PK of methylphenidate?

A
  • Peak plasma concentrations at 1-3 hr after oral dose
  • Half life: 1.5-2.5 hrs (short half life)
25
Q

What are the common side effects of methylphenidate?

A
  • Nervousness
  • Insomnia
  • Loss of appetite
  • Headache
26
Q

What are the rare side effects of methylphenidate?

A
  • Irregular heartbeat
  • Seizures
  • Mood/behavior changes (agitation, aggression, depression)
  • Uncontrolled muscle movement, tics
27
Q

What percentage do young adults aged 18-25 report past-year stimulant misuse?

A

7.4%

28
Q

About how many college students have used stimulants non-medically?

A

1/3

29
Q

What is the 2nd line treatment for ADHD?

A

Antidepressants:
* Bupropion - DA/NE reuptake inhibitor
* Atomexetine - NE reuptake inhibitor

30
Q

What is the third line treatment for ADHD?

A
  • TCAs
31
Q

What other nonstimulants can be used to treat ADHD?

A
  • Antipsychotics
  • Alpha2 adrenoceptro agonist:
    • Clonidine
    • Guanfacine