CNS stimulants

psychomotor stimulants therapeutic indications:

ADHD, narcolepsy

People with ADHD are thought to have lower areas of —- in certain areas of the brain - Giving them amphetamines (and other drugs obviously) will give them this —- that they lack 

dopamine

all CNS stimulants produce a——- (a drug will have different effects based on baseline behavior)

rate dependent effect

stimulant medications used to treat ADHD: 

amphetamine, lisdexamfetamine, methylphenidate, bupropion 

selective norepinephrine reuptake inhibitor med that is used to treat ADHD:

atomoxetine

sudden loss of motor movement, Might freeze up or collapse, Pts with narcolepsy can appear with this as well

catalepsy

Due to loss of orexin-producing hypothalamic neurons (wake-promoting neurons), No therapeutics to directly address this

narcolepsy 

most common drugs used for narcolepsy that do not produce tolerance

modafinil, armodafinil

is structurally similar to norepi and epi

dopamine

synthesized presynaptically, stored in vesicles, released upon neuron activation, and bind to both postsynaptic and presynaptic receptors

norepinephrine, dopamine

Dopamine and norepinephrine are eliminated from the synapse primarily by ——Can be either recycled into synaptic vesicles or metabolized into inactive metabolites

reuptake 

reverse reuptake transporters and increase dopamine/norepinephrine release, indirect acting sympathomimetics

amphetamine like sympathomimetics

stimulates release of norepi and dopamine even without an action potential, used to treat ADHD, narcolepsy, obesity, ex: adderall

amphetamine

prodrug of amphetamine; slow release of amphetamine during the day (~ 12 h), just has a longer duration of action (half-life) because it’s a prodrug that gets broken down to amphetamine so that extra step makes it last longer, Vyvanse 

lisdexamfetamine 

amphetamine =

a-methyl phenethylamine

stimulates release of dopamine and norepinephrine from presynaptic nerves, widely abused stimulant, therapeutic indication for ADHD and obesity

methamphetamine

block reuptake transporters and inhibit dopamine/norepinephrine reuptake from synapse (MDP)

methylphenidate like sympathomimetics 

dopamine reuptake inhibitor, ADD/ADHD (preferred for adolescents), Ritalin

methylphenidate

selective norepinephrine reuptake inhibitor, marketed as non-stimulant ADHD treatment, only blocks norepinephrine reuptake, Does not block dopamine transporter, As good as methylphenidate and amphetamine in fixing impulsivity

atomoxetine

dopamine and norepinephrine reuptake inhibitor, does not have FDA approval for ADHD - But is used for that off label, used to treat depression and smoking cessation as well, Wellbutrin 

bupropion 

Low affinity dopamine reuptake transporter inhibitors, Little euphoria, lower addiction potential, fewer side effects than other psychostimulants, used for narcolepsy, obstructive sleep apnea, also used by military to keep soldiers awake - alerting effect, Provigil

modafinil

Effects of stimulants are

dose dependent

adverse effects of psychomotor stimulants 

psychotic effects, reduced appetite, increased BP and HR, xerostomia

(dry mouth), Combination of vasoconstriction and lack of salivation, Risk of tooth decay

xerostomia 

you can’t give theses meds if you are taking a psychomotor stimulant

MAOIs

what does MAOIs stand for

monoamine oxidase inhibitors

psychomotor stimulants are ——-substances and can be highly addictive and have bad cravings

schedule II

“Non-psychomotor” stimulants: distinct stimulant effects while having unique pharmacology to psychomotor stimulants

methylxanthenes 

Overall, leads to CNS stimulation and smooth muscle relaxation, Inhibits enzyme phosphodiesterase, Adenosine (A1, A2, and A3) receptor antagonist

methylxanthene

methylxanthene drugs:

theophylline, caffeine

Long acting, found in tea, Oral, I.V., these are all off-label / non-preferred uses, Airflow obstruction (COPD/asthma), Bradycardia following heart transplant, Acute cardiac decompensation

theophylline

Used recreationally for stimulant effects, Used therapeutically for headache, migraine relief, hypotension (very rare), intermediate acting 

caffeine 

lethargy, irritability, headache, for caffeine, this can occur 1-3 days no consumption

methylxanthene withdrawal

nicotinic acetylcholine receptor agonist, Produces stimulant effects when used, Short duration of action, Marked tolerance, physical dependence, and behavioral dependence

nicotine

indicated for cravings associated with cessation, Sustained release formulation; modest effects, Increased risk of seizures, Zyban (other use for this drug) 

bupropion 

partial agonist of nicotinic acetylcholine receptors, smoking cessation, Produces less euphoric effects and more effective nicotine replacement

varenicline