Lecture 13 - CNS stimulants Flashcards
as a group, stimulants belong to what drug class?
they increase ____ in the synaptic cleft, particularly ___ and _____
indirect sympathomimetics;
catecholamines;
dopamine, NE
stimulant effects:
____ bp, ____ HR;
can cause euophoria –> _____ at high doses;
increase, increased (Risk of stroke);
psychosis
nicotine is a _____ and was initially advertised to treat asthma (lol);
amphetamines were used for ______, _____, _____
bronchodilator;
bronchodilation, obesity, narcolepsy
amphetamines are currently used for _____, ____, and _____
narcolepsy (plus other sleepiness disorders), obesity, ADHD
amphs include amphetamine, methylphenidate
_____ is a weaker psycho stimulant used for narclopsy and is _____ selective, vs amphetamine which acts on NE and Dopa transporters
modafinil (also armodafinil);
DAT
______ is a NET selective drug used to treat ADHD. guanfacine is a _____ _____ also used to treat
atomoxetine;
alpha 2 agonist
______ is a pro-drug that is metabolized in the stomach into amphetamine and lysine. it has a _____ Duration of action
lisdexamfetamine (vyvanse);
long
stimulants mainly reduce appetite/lose weight via increased levels of _____. ______ is a cathinone that is NET selective
NE;
amfepramone
benzphetmaine/phentermine are amphetamine related, used to treat hyperphagia
psychostimulants/Eating disorder probs:
weight _____ occurs with drug discontinuation. ____ can develop leading to abuse potential. chronic use is associated with ______
gain;
tolerance;
hypertension
nicotine is a weak ____ and is easily absorbed . unlike Ach, it is not degraded by _____ and has a _____ half life
base;
AchEsterase; longer
nicotine binds receptors in the _______, leading to increased dopamine release to the ______
VTA;
nucleus accumbens
nictone binds to NAchR, which is a pentameric _____ channel.
ion
binding of NAchR allows ____ to enter the cell, some ____ to exit the cell, and overall a _____ to occur
Na, K; action potential
NAchR and interneurons:
the alpha7 receptor is found presynaptically on gluataminergic neurons in the _____. binding increases glutamine release –> activating _____ releasing neurons in the ____ _____
VTA;
dopamine, Nucleus accumbens
NAchR and interneurons:
the alpha4beta2 receptor is found on _____ interneurons, binding indirectly inhibits ____ release –> causing an increase in dopamine release
GABA;
GABA
varenicline is a _______ used for smoking cessation. ____ inhibits NET and dopamine reuptake and is also used for smoking cessation
NAchR partial agonist;
bupropion
cocaine is mainly a ______ antagonist
DAT (dopamine transporter);
also inhibits SERT, NET to a lesser extent
meth/amphetamines:
mimics endogenous _____
dopamine
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
reuptake;
VMAT;
reverse (ie out into synapse)
MDMA/XTC has more effects on _____ and ____ relative to meth
SERT, NET
MDMA/XTC also activates _______ which _____ DAT –>induces _____ _____ function
trace amine-associated receptor (TAAR1);
phosphorylates;
reverse transport
of cocaine vs amphetamines:
which is taken up by dopamine transporter?
which blocks?
amphetamines; cocaine blocks (its bigger)
ephedrine:
used for what, medically?
nasal decongestion
also bronchodilates
why are amphetamines contraindicated in patients that also are on anti-depressants?
MAO inhibitor –> can cause serotonin syndrome
synthetic _____ are derivatives from the Khat plant (catha edulis) that cause euphoria.
cathinones;
name 2 synthetic cathinones (common names): ____ and _____ ; in general these, all inhibit NET, DAT, or SERT to varying degrees
molly, bath salts
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
hyperthermia;
paranoid delusions
