ADHD Meds: Stimulants And Non-stimulants Flashcards
Describe MOA of stimulants for ADHD
Stimulants enhance neurotransmitter transmission by serving as direct and indirect non-catecholamine sympathomimetics
Block presynaptic reuptake, interference with vesicular monoamine transporter (VMAT), and increase in neurotransmitter release (NE, then DA, then 5HT each at increasing doses)
D-isomers of AMP/MPH have more CNS activity than mixed or Ltype
Methylphenidate’s main activity: inhibition of DA reuptake and inhibition of neurotransmitter presynaptic reuptake (doesn’t stimulate release of neurotransmitters)
**Describe onset and prescription of stimulants
Onset usually 24 hrs in most pts
Controlled substances, so 1 month supply only, no refills, no samples
Some states allow 3 months. MO allows future dating
Describe Adzenys XR-ODT (d,l-amphetamine)
3:1 ratio of d-amphetamine and l-amphetamine isomers XR-ODT = 50% IR and 50% XR No water necessary Approved for ages 6 and older QD dosing
Describe Dyanavel XR liquid (d,l-amphetamine)
3.2:1 ratio of d- and l-amphetamine
LiquiXR tech
Approved for ages 6 and older
QD
Dexedrine Spansules (dextroamphetamine)
Can sprinkle on food
6 years and older
Also narcolepsy in adults
QD
Vyvanse (lisdexamfetamine; prodrug of dextroamphetamine)
Converted to dextroamphetamine by hydrolytic activity of RBCs. Not metabolized by cytochrome P450 enzymes
May empty contents into glass of water, juice, pudding, yogurt
Shire for chewable tablets
ADHD in 6 years and older
Moderate-to-severe binge eating disorder in adults
QD
Adderall XR (d,l-amphetaminedextroamphetamine)
1/4 total dose each of 2 salt forms, each of amphetamine and dextroamphetamine 3:1 ratio of d to l XR = 50% IR and 50% XR beads Can sprinkle on food Ages 3 and older Narcolepsy in adults QD
Concerts (d,l-methylphenidate)
Phase 1: 22% IR and Phase 2: 78% ER
OROS (Osmotic Release Oral System) delivery system with biphasic release property
6 years and older
QD
Ritalin LA (d,l-methylphenidate)
LA = 50% IR beads and 50% LA beads (enteric-coated, delayed-release)
SODAS (spheroidal oral drug absorption system)
Can sprinkle
6 years and older
QD
Metadata CD (d,l-methylphenidate)
CD = 30% IR and 70% CD (release-control polymer)
May empty CD capsule-contents onto food
Approved for 6 years and older
QD
Aptensio XR (d,l-methylphenidate)
XR = 40% IR and 60% XR (multilayer bead-releasing system)
6 years and older
May empty capsule contents onto food
QD
Daytrana (patch) (d,l-methylphenidate)
MPH in acrylic adhesive dispersed in silicone adhesive (DOT MATRIX tech)
Wear time individualize-able (wear 9 hrs = 10-12 hr DOA)
Not re applicable to skin (changes from clear to opaque)
Sweat/water not factor in adhesion
Low abuse potential (silicone dispersion tech)
6 years and older
QD
QuilliChew ER (d-methylphenidate)
Only extended-release chewable methylphenidate tablet
OralXR release tech (cherry)
XR = 30% IR and 70% XR
XR-methylphenidate ironically-bound to sulfonate groups of sodium polystyrene sulfonate particles
6 years and older
QD
Quillivant XR (d-methylphenidate)
Only extended-release oral methylphenidate suspension
LiquiXR release tech
Distributed as powder requiring reconstitution prior to dispensing
No need to refrigerate. Do need to shake well
XR = 20% IR and 80% XR
6 years and older
QD
Focalin XR (dexmethylphenidate)
XR = 50% IR beads and 50% XR (enteric-coated, delayed-release beads) SODAS Can sprinkle on food 6 years and older QD
What are side effects of stimulants?
Dyspepsia/GI distress (N/V/Ab pain)
Headache
Decreased appetite (weight loss, reduced growth progression)
Insomnia
Anxiety/jitteriness
Irritability/aggression/agitation (motor/vocal tics, psychoses, mania)
Elevated BP/HR (usually mild; dose dependent)
What are rare side effects of stimulants?
Priapism
Seizure (may lower convulsive threshold)
Sudden cardiac death (rare)
Structural cardiac abnormalities/other serious heart
Stroke and MI (adults)
Chemical leukoderma (with Daytrana patch)
Describe caution with using stimulants
Marked anxiety and agitation
Symptomatic CV disease (intolerant of increased BP)
Moderate-to-severe HTN
Glaucoma
Motor tics or family history/diagnosis of Tourette’s syndrome
Ineffectively-treated bipolar (mania)/psychoses
Poorly-controlled seizures
History of drug abuse
Describe non-stimulants for ADHD
Main effect of non-stimulants is to enhance neurotransmitter transmission via
Inhibition of NE pre-synaptic reuptake (atomoxetine)
Agonists of CNS alpha2A adrenergic receptors (guanfacine/clonidine)
-modulates noradrenergic tone in PFC by enhanced noradrenergic input from locus ceruleus
Direct postsynaptic stimulation of alpha2a receptors located on dendritic spines of cortical pyramidal cells, thereby directly promoting functional connectivity of PFC networks
**Describe onset, indications, prescription of non-stimulants
Onset 1-4+ weeks
Useful for pts intolerant of stimulant effects or parents/pts resistant to using stimulant-class
Effect size not as large as seen with stimulants
Non-scheduled, refills and samples permitted up to 1 year
Atomoxetine
Do not open capsules (ocular irritant)
Metabolized by CYP2D6 (poor metabolizes/inhibitors)
6 years and older
QD
Side effects and caution of atomoxetine
Similar to stimulants except
NO motor/vocal tics, NO seizures, NO marked anxiety/agitation, NO motor tics or history of Tourette’s, NO poorly controlled seizures, NO history of drug abuse
Different: **Suicidal ideation Severe liver injury/jaundice Narrow-angle glaucoma MAO inhibitors CYP2D6 inhibitors
Describe guanfacine and clonidine
Alpha2 agonists, extended-release products
Do not crush, chew, or break tablets
6 years and older
QD (HS for clonidine)
Downward dose titration over 1+ weeks (depending on dose) recommended upon discontinuation
Risk for rebound hypertension (both anti-hypertensives)
Describe side effects of alpha2 agonists
Dyspepsia/GI distress (N/V)
Somnolence/sedation/fatigue
**Hypotension/bradycardia
Orthostatic hypotension
Rare side effects of alpha2 agonists
Exacerbation of cardiac conduction abnormalities
QT prolongation
AV block
Caution using alpha2 agonists
Symptomatic CV disease (intolerant of decrease BP)
Hypotension/bradycardia
Cardiac conduction abnormalities
