Anxiolytics/Hypnotics Flashcards
what region of the brain is associated with anxiety?
amygdala
what are the two endings for benzodiazepines?
pam and lam
what is the one benzo that doesnt end in lam or pam?
chlordiazepoxide
what is the MoA of benzos?
they bind the GABA channel and help GABA enter through the channel to increase inhibition
what are the classic SEs of benzos?
drowsiness, dizziness, fatigue, memory loss, confusion
respiratory depression
what can happen with benzos with continued use over time?
tolerance
how does the body build tolerance to benzos?
increase glutamate presynaptice release and increase glutamate receptors on post synaptic
so what happens if you withdrawal benzos quickly?
the increased glutamate and receptors will lead to stimulation and you get anxiety/panic, insomnia, tachycardia
can benzos be addictive?
yes
why are benzos addictive?
they stimulate dopamine release into the nucleus accumbens
what is the nucleus accumbens also known as?
pleasure center/addictive center
how do benzos cause dopamine release in the nucleus accumbens?
they inhibit the release of GABA so more excitation in the area with loss of GABA
with chronic alcohol intake, what happens to glutamate?
glutamate amount and receptors increase to counterbalance the continued inhibitory effects of alcohol
what can you give for alcohol withdrawal to help with glutamate overload?
benzos
what are immediate symptoms of alcohol withdrawal?
anxiety, GI issues, tremors
what are long term results of alcohol withdrawal?
seizures 2-5 days out
delirium tremen 3-7 days out
what is the reversal agent for benzodiazepines?
Flumazenil
what is the MoA of Flumazenil?
competitively inhibits the binding of benzos to GABA receptors
what two drugs are benzos synergistic with that can lead to death?
alcohol and opiates
what is the issue with benzo metabolism?
can lead to sedation through active metabolites
which two benzos have significant active metabolites in breakdown?
chlordiazepoxide and diazepam
which three benzos do not have any metabolites in breakdown? what does this mean about them?
Lorazepam
Oxazepam
Temazepam
means they have no sedation side effect
what GABA receptor do benzos bind to be anxiolytics?
a2/5 GABA-R
what GABA receptor do benzo metabolites bind to be sedative?
a1 GABA-R
what is the MoA of Buspirone?
agonizes the inhibitory serotonin autoreceptor and decreases pre synaptic serotonin release
what are SEs of buspirone?
not really any
how do SSRI and SNRIs treat anxiety?
treat underlying depression
what class of drugs stimulates the a1 GABA-R receptor?
Z drugs
name the Z drugs
Zalepon
Zolpidem
Eszopiclone
what is the MoA and effect of Zalepon, Zolpidem and Eszopiclone?
they bind the a1-GABA receptor and induce sedation
what can Zalepon, Zolpidema and Eszopiclone cause?
sleep walking/eating/driving
what is the drug to give for inducing sleep that is similar to melatonin?
Ramelteon
when do you give ramelteon?
at night when sun goes down
