Yang Flashcards
what structure regulates sleep/wake cycles?
reticular formation
which sleep cycle resembles wakefulness on an EEG
REM
what time does melatonin start coming in
9 pm
neurotransmitter regulators of sleep
catecholamines (NE,E,dopamine)
serotonin
histamine
acetylcholine
adenosine
GABA
what is our main target for current medications
GABA
where do benzodiazepines bind the GABA A receptor/Cl channel
orthosteric site
alpha 1 / gamma 2
benzodiazepines increase _____ of channel opening
frequency
facilitate GABA action
Z hypnotics bind what
BZ 1 receptors of alpha 1
overdose treatment that is a benzo antagonist
flumazenil
barbiturates increase _____ of channel opening and have _____ on GABA A
duration
direct effects
1 position of benzos
alkylation that leads to source of active metabolites
annealating the 1-2 bond with an electron rich ring yeilds ____ and _____
high affinity and decreased half life
diazepam half life
LONG
how could we decrease half life of a benzo
annealate the 1-2 bond with an electron rich ring
diazepam (Valium used for)
seizures and accumulation of metabolites
clonazepam used for
anticonvulsant
clonazepam elimination rate
intermediate
midazolam elimination rate
fast
midazolam used for
rapid anesthesia
slow elimination benzos used for
active metabolites
benzos effect on REM and stage 3/4
decrease
short term insomnia drugs
zolpidem, zaleplon
long term insomnia drug
eszopiclone
which class has fewer negative effects on sleep patterns
z hypnotics
z hypnotics side effects
sleep-driving, sleep-cooking, sleep-eating, sleep-sex
long acting barbiturates
anticonvulsants: phenobarbital
short to intermediate acting barbiturates
sedative-hypnotics: pentobarbital
barbiturates can cause what
respiratory depression
barbiturtates bind what
all GABA A alpha 1-5
benzos bind what
all GABA A alpha 1-5
which drugs increase frequency of GABA opening
benzos and z hyps
Xyrem use
daytime sleepiness
increase wakeness
gamma-hydroxybutyric acid (GHB) names and use
liquid ecstacy
juice
scoops
causes CNS depression
concern with GHB
no antagonist
date rape drug
what produces melatonin
pineal gland
melatonin agonist drug for night shift workers
Ramelteon
Ramelteon benefit
no abuse, withdrawal, dependency
melatonin agonist used in blind individuals
Tasimelteon
(orphan drug registration)
orexin receptor antagonist drug
suvorexant
where are orxein receptors located
hypothalamus
suvorexant (Belsorma) moa
reduce rewarding stimuli
modulate projections between VTA and nucleus accumbens
antihistamines used in sleep
diphenhydramine
doxylamine
pyrilamine
hepatoxicity has been noted with which herbal
valerian
norepinephrine projects where
amygdala
in anxiety there is reduced ____ signaling
GABA
glutamate is converted to GABA by
glutamic acid decarboxylase
quick acting treatment of anxiety
benzos
buspirone is a _____ and has an _____ response
5HT1a partial agonist
adaptive
abuse potential of buspirone
low
is buspirone good for panic disorders?
no, benzos faster
beta blocker of choice and consideration
propranolol
need to test dose
decreased peripheral sx of anxiety