10. Pharmacology of CNS Stimulants Flashcards

1
Q

What are the 2 categories of ADHD medications?

A
  1. Stimulants (amphetamines)
  2. Non-stimulants
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2
Q

Types of amphetamines

A
  1. Amphetamine (d & l) and dextroamphetamine (methamphetamine)
  2. Lisdexamfetamine (pro-drug)
  3. Methylphenidate (d & l) and dexmethylphenidate
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3
Q

Types of non-stimulants

A
  1. Atomoxetine
  2. Guanfacine
  3. Clonidine
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4
Q

MOA of the stimulants used for ADHD?

A
  1. Block presynaptic reuptake of catecholamines and DA.
  2. Interfere with VMAT
  3. ↑ in NT release —> NE => DA => 5-HT, each at ↑ dose
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5
Q

Which isomers of AMP/MPH have more CNS activity?

A

D-isomers of AMP/MPH

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6
Q

What is methylphenidate’s main activity (MOA)?

A
  • Inhibition reuptake of DA and other NT pre-synaptic reuptake
  • Does NOT stimulate release of NT’s
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7
Q

What must you always assess for before prescribing stimulants for ADHD?

A

Structural cardiac abnormalities, to prevent sudden cardiac death, strokes and MI

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8
Q

Other RARE SE of stimulants

A
  1. Chemical Leukoderma (w/ Daytrana patch)
  2. Priapism
  3. Seizures
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9
Q

Describe what the following abbreviations mean:

  1. IR
  2. ER/XR
  3. LA
  4. CD
  5. ODT
A
  1. Immediate release
  2. Extended release
  3. Long-acting
  4. Controlled delivery
  5. Oral disintegrating tablet (ODT)
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10
Q

What cautions are there when using stimulants?

A
  1. ↑ anxiety/agitation
  2. Caution in pts with
    1. Ineffectively-treated bipolar (mania)/psychosis)
    2. CV disease and moderate-to-severe HTN
    3. Glaucoma
    4. Motor tics/Tourettes
    5. Poorly-controlled seizures
    6. Hx of drug abuse
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11
Q

What is the onset of activity for stimulants in most patients?

A

24 hours

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12
Q

How are stimulants administered?

A

Stimulants are controlled substances (1 month supply only, no refills, no samples); some states, like MO, allow 3 months of Rxs (future-dating)

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13
Q

What is the duration of action of the IR [amphetamine-based stimulants]?

A

4 - 6 hours

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14
Q

IR [Amphetamine Stimulants]

A
  1. Adderall (Dextroamphetamine/AMP)
  2. Zenzidi (Dextroamphetamine)
  3. ProCentra (Dextroamphetamine Sulfate)
  4. Evekeo (Amphetamine Sulfate)
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15
Q

Which IR amphetamine stimulant comes in a liquid form?

A

ProCentra (Dextroamphetamine Sulfate)

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16
Q

Which IR amphetamine stimulant comes in a capsule?

A

Evekeo (Amphetamine Sulfate)

17
Q

ER [Amphetamine Stimulants]

A
  1. Adderall XR (Dextroamphetamine)
  2. Dexedrine (Dextroamphetamine)
  3. Dyanavel XR (Amphetamine)
  4. Mydayis (Amphetamine/Mixed Salts)
  5. Vyvanse (Lisdexamfetamine)
18
Q

What is the ONLY liquid ER [amphetamine], while all of the other ones are capsules?

A

Dyanaval XR (Amphetamine)

19
Q

Which XR amphetamine stimulant comes in a capsule and has the longest duration (16 hrs)?

A

Mydayis (Amphetamine/Mixed Salts)

20
Q

What is the XR-ODT (oral disentegrating tablet) used for ADHD?

Who is it given to?

A
  • Adzenys XR- ODT (d,l- amphetamine)
    • 3:1 ratio of d-amphetamine:l-amphetamine.
    • 50% IR and 50% XR
    • Approved for: > 6YO without water q.d (once/day)
21
Q

3 IR Methylphenidates

A
  1. Focalin (Dexmethylphenidate)
  2. Methylin Oral Solution (Methylphenidate)
  3. Ritalin (Methylphenidate)
22
Q

IR Methylphenidates in tablet

A
  1. Focalin (Dexmethylphenidate)
  2. Ritalin (Methylphenidate)
23
Q

IR Methylphenidates in liquid

A
  1. Methylin oral solution (Methylphenidate)
24
Q

2 Sustained Release Methylphenidates

A
  1. Ritalin-SR (Methylphenidates)
  2. Desoxyn (Methamphetamine)

Both are tablets that last 4-8 hours.

25
Q

Which XR methylphenidate stimulant comes in a transdermal patch?

A

Daytrana (Methylphenidate Transdermal)

26
Q

Which XR methylphenidate stimulants comes in a liquid and has formulas that last 8, 10, and 12-hours?

A

Quillivant XR (Methylphenidate)

27
Q

Which ER/XR Methylphenidate comes in a chewable tablet?

A

QuilliChew (Methylphenidate HCl)

28
Q

Which 4 XR Methylphenidate stimulants come in a capsule; which has the longest duration of action?

A
  1. Aptensio XR (Methylphenidate): 12 hours
  2. Focalin XR (Dexmethyphenidate HCl)
  3. Metadate (Methylphenidate HCl)
  4. Ritalin LA (Methylphenidate HCl ER)
29
Q

What is the (MOA) of the non-stimulants used for ADHD: Atomoxetine, Guanfacine and Clonidine?

A

Enhance NT transmission by:

  1. Atomoxetine: inhibits pre-synaptic reuptake of NE.
  2. Guanefacine/Clonidine: α-2A-R AGO
30
Q

What is the onset of activity for the non-stimulants used for ADHD?

A

1 - 4+ weeks

31
Q

How are NON-stimulants administered and why?

A
  • Non-scheduled refills and samples that can be given up to 1 year.
  • Useful for patients intolerant/resistant to stimulants.
32
Q

Atomoxetine (Strattera)

  1. Form
  2. Duration of action
  3. How to use
  4. Warnings
A
  1. Capsule that lasts 24 hours
  2. Q.D for ppl > 6YO
  3. Warnings:
    1. Do not open the capsule => ocular irritant
    2. Metabolized by CYP2D6 (poor metabolizers/inhibitors)
33
Q

Which non-stimulants are ANTI-HYPERTENSIVES approved for ADHD?

Form? Duration of action?

A
  1. Kapvay ER (Clonidine)
  2. Intuniv ER (Guanfacine)

​Both are tablets and last 12-24 hours.

34
Q

What are common for both Guanfacine and Clonidine?

A
  1. Do not crush, chew or break tablets.
  2. Approved for > 6YO
  3. Take once/day (Q.D)
  4. When DQ, downwardly titrate over 1+ week, depending on dose due to risk of rebound HTN.