Stimulants and ADHD - Watts Flashcards
The RAS contains what 4 types of neurons?
DA
Adrenergic
Serotonergic
Cholinergic
When do symptoms of ADHD appear?
ages 5-9
Before 12 for diagnosis
How many symptoms of ADHD must be present for diagnosis?
6 or more
Symptoms of ADHD?
Inattention
Hyperactivity
Impulsivity
Inattention examples
Difficulty organizing tasks/activities
Does not seem to listen
Easily distracted
Loses things for activities
Hyperactivity examples
Fidgets or squirms
Impulsivity examples
Leaves seat
Runs/climbs excessively
Interrupts
Methylxanthines are (direct/indirect) acting sympathomimetics
indirect
3 metabolites of caffeine?
Paraxanthine
Theobromine
Theophylline
What drug class are caffeine, paraxanthine, theobromine, and theophyllin?
Methylxanthines
MOA of methylxanthines
Antagonize adenosine receptor
Inhibit PDE: increase cAMP
Increase activity of ryanodine receptors (increase intracellular Ca)
Which adenosine receptors do methylxanthines antagonize?
A1, A2a, A2b, and A3
Linked to what receptor? location in synapse and brain, and what does it do?
A1 adenosine receptor
Gi/o linked
Pre and post synaptic
Located in cerebral cortex, hippocampus, cerebellum, thalamus, brain stem, and spinal cord
Inhibitory modulation of many neurotransmitters
CNS Activation of A1 adenosine receptors
Sedation, neuroprotection, anxiolysis, temperature reduction, anticonvulsant activity, and spinal analgesia
Peripheral activation of A1 adenosine receptors
Bronchoconstriction, decreased glomerular filtration, decreased HR, slowed atrioventricular conduction, adn decreased atrial myocardial contractility
Linked to what receptor? location in synapse and brain, and what does it do?
A2a adenosine receptor
Gs linked
pre and post synaptic
Located in cerebral vasculature and striatum: vasodilation
Inhibitory modulation of many neurotransmitters
Linked to what receptor? location in synapse and brain, and what does it do?
A2b adenosine receptor
Heterodimerize with A1 and D2 dopamine receptors
Gs-linked
Mostly on glial cells
Function unknown
Linked to what receptor? location in synapse and brain, and what does it do?
A3 adenosine receptor
Heterodimerize with A1 and D2 dopamine receptors
Gq-linked, hippocampus and thalamus
Only activated in state of excessive catabolism
NOT antagonized by methylxanthines
Effects of methylxanthines
Mild cortical arousal Increased alertness Decreased fatigue Nervousness/insomnia Ionotropic/chronotropic effects Vasoconstriction (cerebral vessels) Smooth muscle relaxation Diuretic action (think about what caffeine does!!!)
Stimulants are (direct/indirect) acting sympathomimetics
indirect
Cocaine is a ____
stimulant
Cocaine is an _____ from the leaves of _____
alkaloid
erythroxoylon coca
Cocaine inhibits monoamine transporters which affects the concentration of what neurotransmitters?
NE
5-HT
DA
Cocaine can be used as what type of anesthetic and is highly ____ and ____
local
Rewarding and addictive
Cocaine is (a direct/an indirect) acting sympathomimetics
an indirect
Amphetamines are (direct/indirect) acting sympathomimetics
indirect
Amphetamines are (selective/non-selective) activators of monoamines?
non-selective
Except MDMA which is more selective for 5-HT!
What effects do amphetamines have on a user?
Wakefulness, alertness, increased ability to concentrate
High doses of amphetamines can elicit what type of behavior?
Psychotic
Clinical uses for amphetamines?
Narcolepsy
Anorexiant
ADHD
Examples of pharmacologic amphetamines
Dextroamphetamine Lisdexamfetamine Methylphenidate Dexmethylphenidate Adderall Mydayis
Which penetrates the CNS better?
Amphetamine vs Methamphetamine
Methamphetamine
Non-stimulants used for ADHD
Atomoxetine TCAs Bupropion Clonidine Modafinil
Modafinil is approved for ____ but not ____
narcolepsy
ADHD
Alternative therapies for ADHD?
Elimination of artificial food additives, colors and/or preservatives EEG biofeedback Essential fatty acid supplementation Yoga/massage Green outdoor spaces
Physical/cognitive aspects of narcolepsy
Excessive daytime sleepiness Cataplexy/Weakening of muscles Poor sleep quality Sleep paralysis Hypnogogic hallucinations
Treatment for narcolepsy
Stimulants for sleepines Solriamfetol Modafinil Antidepressants Xyrem Pitolisant
Pitolisant is a (pre/post synaptic) ____ antagonist
presynaptic
H3 antagonist
Solriamfetol blocks ___ and ____
NET and DAT
Modafinil blocks ____
DAT