Gibbs: stimulants and ADHD Flashcards
define stimulants
drugs that enhance CNS activity–> leading to alertness, awareness, wakefulness, decreased need for food/sleep, etc
uses for stimulants
counteract lethargy/fatigue, reduce sleepiness, decrease appetite, weight loss, improve focus
off label for depression
types of stimulants
-xanthines: caffeine, theobromine, theophylline
-nicotine
-amphetamines
-MDMA
-cocaine
-NRIs and NDRIs
-methylphenidate
-modafinil, adrafinil, armodafinil
-yohimbine
diagnostic criteria ADHD for children <17
at least 6 symptoms of inattention and/or at least 6 symptoms of hyperactivity-impulsivity for 6 months prior to assessment & inappropriate for developmental level
some symptoms present prior to 12 years of age
impairment in at least 2 settings
clinically significant impairment socially, academically, etc
symptoms not better accounted for by another mental disorder
neuroanatomical changes in ADHD
decreased activation in prefrontal cortex and medial prefrontal cortex
related to a decrease in dopamine function
pharmacotherapy options for ADHD
psychostimulants (methylphenidate & amphetamine)
non-stimulants: antidepressants (atomoxetine, bupropion, TCAs) or central alpha2 agonists (clonidine, guanfacine)
amphetamine & MPH are _____
phenethylamines
structurally similar to DA and NE
which drugs are amphetamines
amphetamine, methamphetamine, MDA, MDMA (ecstasy)
MDA & MDMA have a _______ moiety
methylenedioxy
mechanism of amphetamine and methamphetamine
enter the cell via DAT transporter– interfere with vesicular monoamine transporter– deplete synaptic vesicles of DA/NE– levels of DA/NE increase in the cytoplasm, causing release of neurotransmitter into synapse
what are the salts in adderall
4 salts:
dextroamphetamine saccharate
L-amphetamine aspartate monohydrate
dextroamphetamine sulfate
L-amphetamine sulfate
D-amphetamine is ___x as potent as L-amphetamine
3-4x
what is in vyvanse
lisdexamfetamine dimesylate (a prodrug of D-amphetamine)
symptoms of amphetamine toxicity
talkative, euphoric, agitated, confused, dilated pupils, teeth grinding
higher doses: tachycardia, dysrhythmias, vasoconstriction, hypertensive crisis
what is the mechanism of methylphenidate
increases DA/NE levels by blocking reuptake transporters
overall what is the difference in mechanism between amphetamine and methylphenidate
amphetamine enters via DAT & blocks DA uptake into vesicles, enters vesicles & releases DA into the cytoplasm
methylphenidate blocks DAT
what is the most prevalent prescription misused
stimulants
(eclipsed opioids)
what is cocaine
benzoylmethylecgonine
a stimulant, local anesthetic, hallucinogen, drug of abuse
chemistry of cocaine
it is a colorless amino ester
it has low water solubility
HCl salt is the most common water soluble derivative
how is cocaine absorbed
mucous membranes
onset/peak/duration of cocaine
onset 1 min
peak 5 min
duration 30 min
effects of cocaine in the peripheral versus central nervous system
peripheral: local anesthesia by blocking voltage-gated sodium channels
central: stimulation by blocking monoamine transporters or blocking reuptake of monoamines from synaptic cleft
what is brompton’s cocktail
alcoholic solution containing an opioid (morphine, heroin for analgesia), cocaine for euphoriant, antiemetics
can be used to alleviate terminal pain (cancer)
CNS effects of cocaine
euphoria, high energy, mental alertness
what causes the rewarding effect of cocaine
blockade of DAT results in increasing dopamine concentrations in the nucleus accumbens (reward center of brain) via mesolimbic pathway
symptoms of cocaine toxicity
diaphoresis
mydriasis (dilated pupils)
fever, tachycardia, tachypnea, confusion, xerostomia, hypertension
what are the 3 factors that promote cocaine abuse and addiction
euphoria
strong reinforcement properties
rapid onset
methods of cocaine abuse
smoking, crack cocaine, intranasal
cocaine abusers trying top maintain euphoria will take the drug how often
repeatedly every 30-40 minutes
what is the fatal dose of cocaine and how do you treat
1.2 grams
bring down BP, slow heart rate, maintain breathing (IV lorazepam and nitroprusside, mechanical respiration)
the alkaloid salt is _____
ionized amines
the alkaloid base is ____
unionized free amines
general steps as to how cocaine is made
coca leaves crushed–> then add H20 + Ca(OH)2 or CaCO3–> now it is crushed leaves in an aqueous weakly alkaline environment–> stir with gasoline or kerosine
the precipitate (B) can be smoked
the filtrate can be reacted with sulfuric acid to produce cocaine sulfate
