Gibbs: stimulants and ADHD

Question 1

define stimulants

Answer 1

drugs that enhance CNS activity–> leading to alertness, awareness, wakefulness, decreased need for food/sleep, etc

Question 2

uses for stimulants

Answer 2

counteract lethargy/fatigue, reduce sleepiness, decrease appetite, weight loss, improve focus
off label for depression

Question 3

types of stimulants

Answer 3

-xanthines: caffeine, theobromine, theophylline
-nicotine
-amphetamines
-MDMA
-cocaine
-NRIs and NDRIs
-methylphenidate
-modafinil, adrafinil, armodafinil
-yohimbine

Question 4

diagnostic criteria ADHD for children <17

Answer 4

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

Question 5

neuroanatomical changes in ADHD

Answer 5

decreased activation in prefrontal cortex and medial prefrontal cortex

related to a decrease in dopamine function

Question 6

pharmacotherapy options for ADHD

Answer 6

psychostimulants (methylphenidate & amphetamine)
non-stimulants: antidepressants (atomoxetine, bupropion, TCAs) or central alpha2 agonists (clonidine, guanfacine)

Question 7

amphetamine & MPH are _____

Answer 7

phenethylamines
structurally similar to DA and NE

Question 8

which drugs are amphetamines

Answer 8

amphetamine, methamphetamine, MDA, MDMA (ecstasy)

Question 9

MDA & MDMA have a _______ moiety

Answer 9

methylenedioxy

Question 10

mechanism of amphetamine and methamphetamine

Answer 10

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

Question 11

what are the salts in adderall

Answer 11

4 salts:
dextroamphetamine saccharate
L-amphetamine aspartate monohydrate
dextroamphetamine sulfate
L-amphetamine sulfate

Question 12

D-amphetamine is ___x as potent as L-amphetamine

Answer 12

3-4x

Question 13

what is in vyvanse

Answer 13

lisdexamfetamine dimesylate (a prodrug of D-amphetamine)

Question 14

symptoms of amphetamine toxicity

Answer 14

talkative, euphoric, agitated, confused, dilated pupils, teeth grinding
higher doses: tachycardia, dysrhythmias, vasoconstriction, hypertensive crisis

Question 15

what is the mechanism of methylphenidate

Answer 15

increases DA/NE levels by blocking reuptake transporters

Question 16

overall what is the difference in mechanism between amphetamine and methylphenidate

Answer 16

amphetamine enters via DAT & blocks DA uptake into vesicles, enters vesicles & releases DA into the cytoplasm

methylphenidate blocks DAT

Question 17

what is the most prevalent prescription misused

Answer 17

stimulants
(eclipsed opioids)

Question 18

what is cocaine

Answer 18

benzoylmethylecgonine
a stimulant, local anesthetic, hallucinogen, drug of abuse

Question 19

chemistry of cocaine

Answer 19

it is a colorless amino ester
it has low water solubility
HCl salt is the most common water soluble derivative

Question 20

how is cocaine absorbed

Answer 20

mucous membranes

Question 21

onset/peak/duration of cocaine

Answer 21

onset 1 min
peak 5 min
duration 30 min

Question 22

effects of cocaine in the peripheral versus central nervous system

Answer 22

peripheral: local anesthesia by blocking voltage-gated sodium channels

central: stimulation by blocking monoamine transporters or blocking reuptake of monoamines from synaptic cleft

Question 23

what is brompton’s cocktail

Answer 23

alcoholic solution containing an opioid (morphine, heroin for analgesia), cocaine for euphoriant, antiemetics
can be used to alleviate terminal pain (cancer)

Question 24

CNS effects of cocaine

Answer 24

euphoria, high energy, mental alertness

Question 25

what causes the rewarding effect of cocaine

Answer 25

blockade of DAT results in increasing dopamine concentrations in the nucleus accumbens (reward center of brain) via mesolimbic pathway

Question 26

symptoms of cocaine toxicity

Answer 26

diaphoresis
mydriasis (dilated pupils)
fever, tachycardia, tachypnea, confusion, xerostomia, hypertension

Question 27

what are the 3 factors that promote cocaine abuse and addiction

Answer 27

euphoria
strong reinforcement properties
rapid onset

Question 28

methods of cocaine abuse

Answer 28

smoking, crack cocaine, intranasal

Question 29

cocaine abusers trying top maintain euphoria will take the drug how often

Answer 29

repeatedly every 30-40 minutes

Question 30

what is the fatal dose of cocaine and how do you treat

Answer 30

1.2 grams
bring down BP, slow heart rate, maintain breathing (IV lorazepam and nitroprusside, mechanical respiration)

Question 31

the alkaloid salt is _____

Answer 31

ionized amines

Question 32

the alkaloid base is ____

Answer 32

unionized free amines

Question 33

general steps as to how cocaine is made

Answer 33

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