Pharm: CNS Stimulants Flashcards
Which ADHD drugs are stimulants (amphetamine derivatives)?
Amphetamine
Dextroamphetamine
Lisdexamfetamine (pro-drug)
Methylphenidate
Dexmethylphenidate
Which ADHD drugs are non-stimulants?
Atomexetine
Guanfacine
Clonidine
What is the MOA of stimulants?
What does that mean in normal words?
Stimulants enhance NTM transmission by serving as direct and indirect non-catecholamine sympathomimetics
They block presynaptic reuptake, interfere with VMAT, increase NTM release
What is the main function of methyphenidate?
inhibits DA reuptake and inhibits NTM pre-synaptic reuptake
What are the side effects of stimulants?
GI distress
HA
decreased appetite
Neuropsychiatric sx (insomnia, anxiety, irritability)
elevated BP/HR
What are rare side effects of stimulants?
Priapism
Sz
Sudden cardiac death-ALWAYS assess for cardiac structure abnormalities
Stroke/MI
Chemical leukoderma with Daytrana Patch
Patients with these conditions should use stimulants with caution
anxiety/agitation
CV disease, intolderant of elevated BP
HTN
Glaucoma
Tourettes
Bipolar/psychoses
Szs (poorly controlled)
Drug abuse
How fast are the effects of stimulants seen after first dose?
24hrs
Are stimulants controlled substances?
Yes
Some states allow for 3 month refills, MO allows for future dating
Which form does each immediate release drug come in:
Dextroamphetamine (Adderall)
Dextroamphetamine sulfate
Amphetamine Sulfate
Dextroamphetamine (Zenzidi)
Tab
Liq
Cap
Tab
Every extended-release amphetamine-based stimulant comes in cap form except for what?
Amphetamine/Dyanavel XR (Liq)
What is Adzenys XR ODT?
It is a 3:1 ratio of d-amphetamine and l-amphetamine isomers
XR-ODT = 50% IR and 50% ER
No water necessary and approved for ages 6 and up with QD dosing
Which form does each methyphenidate-based IR drug come in?
Dexmethyphnidate
Methylphenidate/Methylin
Methyphenidate/Ritalin
All the sustained release methylphenidate drugs (Methylphenidate Ritalin and Methamphetamine) are in what form?
Tab
Liq
Tab
Tab
Which methylphenidate based stimulatantes XR come in cap form?
Methylphenidate
Dexmethylphenidate HCl
Methylphenidate HCl
Methylphenidate HCl ER
Which methylphenidate-based ER stimulants coem in tab form?
methylphenidate HCl
Methylphenidate ER
Which methylphenidate based ER stimulants come in patch, chewable, and liq?
Patch: methylphenidate transdermal (Daytrana)
Chewable: Methylphenidate HCl
Liq: Methylphenidate
What is the main effect of non-stimulants on ADHD?
Enhance NTM transmission via inhibition of the NE pre-synaptic reuptake (atomoxetine) or agonize CNS A2a adrenergic receptors (Guanfaceine/Clonidine)
What are the two effects of Guanfacine and Clonidine?
modulate noradrenergic tone in the Pre-frontal cortex by enhanced noradrenergic input from locus coeruleus
direct post-synaptic stimulation of a2A receptors located on the dendritic spines of cortical pyramidal cells, thereby directly promoting functional connectivity of the prefrontal networks
How long does it take for non-stimulants to take effect?
1-4 weeks
What is the benefit of non-stimulants over stimulants?
useful in pt’s intolerant to stimulants
non-scheduled
How is Atomoxetine metabolized?
via CYP2D6 (poor metabolizers/inhibitors)
Do NOT open capsules as it can irritate eyes
What are the side effects of Atomoxetine?
nervousness, GI distress, liver injury, suicidal ideation
What are the side effects of Clonidine and Guanfacine?
fatigue, drowsiness, low BP
Sudden withdrawal can lead to nervousness, anxiety, elevated BP
What are common dosing rules with Guanfacine and Clonidine?
Do not crush, chew or break tablets
approved for kids 6 and up
QD dosing (HS for clonidine)
Titrate down over 1+ weeks to D/C
