Lecture 13 - CNS stimulants

Question 1

as a group, stimulants belong to what drug class?

they increase ____ in the synaptic cleft, particularly ___ and _____

Answer 1

indirect sympathomimetics;
catecholamines;
dopamine, NE

Question 2

stimulant effects:
____ bp, ____ HR;
can cause euophoria –> _____ at high doses;

Answer 2

increase, increased (Risk of stroke);

psychosis

Question 3

nicotine is a _____ and was initially advertised to treat asthma (lol);

amphetamines were used for ______, _____, _____

Answer 3

bronchodilator;

bronchodilation, obesity, narcolepsy

Question 4

amphetamines are currently used for _____, ____, and _____

Answer 4

narcolepsy (plus other sleepiness disorders), obesity, ADHD

amphs include amphetamine, methylphenidate

Question 5

_____ is a weaker psycho stimulant used for narclopsy and is _____ selective, vs amphetamine which acts on NE and Dopa transporters

Answer 5

modafinil (also armodafinil);

DAT

Question 6

______ is a NET selective drug used to treat ADHD. guanfacine is a _____ _____ also used to treat

Answer 6

atomoxetine;

alpha 2 agonist

Question 7

______ is a pro-drug that is metabolized in the stomach into amphetamine and lysine. it has a _____ Duration of action

Answer 7

lisdexamfetamine (vyvanse);

long

Question 8

stimulants mainly reduce appetite/lose weight via increased levels of _____. ______ is a cathinone that is NET selective

Answer 8

NE;
amfepramone

benzphetmaine/phentermine are amphetamine related, used to treat hyperphagia

Question 9

psychostimulants/Eating disorder probs:
weight _____ occurs with drug discontinuation. ____ can develop leading to abuse potential. chronic use is associated with ______

Answer 9

gain;
tolerance;
hypertension

Question 10

nicotine is a weak ____ and is easily absorbed . unlike Ach, it is not degraded by _____ and has a _____ half life

Answer 10

base;

AchEsterase; longer

Question 11

nicotine binds receptors in the _______, leading to increased dopamine release to the ______

Answer 11

VTA;

nucleus accumbens

Question 12

nictone binds to NAchR, which is a pentameric _____ channel.

Answer 12

ion

Question 13

binding of NAchR allows ____ to enter the cell, some ____ to exit the cell, and overall a _____ to occur

Answer 13

Na, K; action potential

Question 14

NAchR and interneurons:
the alpha7 receptor is found presynaptically on gluataminergic neurons in the _____. binding increases glutamine release –> activating _____ releasing neurons in the ____ _____

Answer 14

VTA;

dopamine, Nucleus accumbens

Question 15

NAchR and interneurons:
the alpha4beta2 receptor is found on _____ interneurons, binding indirectly inhibits ____ release –> causing an increase in dopamine release

Answer 15

GABA;

GABA

Question 16

varenicline is a _______ used for smoking cessation. ____ inhibits NET and dopamine reuptake and is also used for smoking cessation

Answer 16

NAchR partial agonist;

bupropion

Question 17

cocaine is mainly a ______ antagonist

Answer 17

DAT (dopamine transporter);

also inhibits SERT, NET to a lesser extent

Question 18

meth/amphetamines:

mimics endogenous _____

Answer 18

dopamine

Question 19

meth:
blocks dopamine _____. acts on ____ and also pushes dopmaine from vesicles = increased extravesicular amt. higher concentration of dopamine within the neuron causes _____ transport to occur

Answer 19

reuptake;
VMAT;
reverse (ie out into synapse)

Question 20

MDMA/XTC has more effects on _____ and ____ relative to meth

Answer 20

SERT, NET

Question 21

MDMA/XTC also activates _______ which _____ DAT –>induces _____ _____ function

Answer 21

trace amine-associated receptor (TAAR1);
phosphorylates;
reverse transport

Question 22

of cocaine vs amphetamines:
which is taken up by dopamine transporter?
which blocks?

Answer 22

amphetamines;
cocaine blocks (its bigger)

Question 23

ephedrine:

used for what, medically?

Answer 23

nasal decongestion

also bronchodilates

Question 24

why are amphetamines contraindicated in patients that also are on anti-depressants?

Answer 24

MAO inhibitor –> can cause serotonin syndrome

Question 25

synthetic _____ are derivatives from the Khat plant (catha edulis) that cause euphoria.

Answer 25

cathinones;

Question 26

name 2 synthetic cathinones (common names): ____ and _____ ; in general these, all inhibit NET, DAT, or SERT to varying degrees

Answer 26

molly, bath salts

Question 27

cathinones can cause _____ which is significant due to their use at raves –> dehydration. also can cause heart palpitatations, cardiac arrest, _____ that can last for days

Answer 27

hyperthermia;

paranoid delusions