Lecture 4 Sedative/Hypotics Flashcards
a ____ calms anxiety, decreases excitement ;
a ____ induces sleep (refreshing)
sedative,
hypnotic
the _____ ____ regulates sleep-wake transitions and synchronization of the EEG
reticular formation
stage N3/4 of sleep:
___ waves occur that have ____ frequency and ____ amplitde. it is the ____ non-REM sleep
delta,
low, high;
deepest
REM sleep and awake:
both have ____ waves
beta
the GABAa receptor acts as a ____ channel when bound
Cl
pentameric
GABAa receptor:
the orthersteric site (Where GABA binds) is ___ and ___;
Benzos bind the ortho or allosteric site?
location of this site?
alpha 1, beta 2;
allosteric–alpha 1, gamma 2
benzo’s increase the ____ of Cl- channel opening.
what drug binds the same location as benzo’s but is an antagonist?
FREQUENCY;
flumazenil
____ and ____ bind to different allosteric sites of the GABAa receptor
barbituates, alcohol
barbituates increase the _____ of GABAa channel opening
duration
name a GABA channel blocker?
picrotoxin
benzo structure things:
alkylation at the ____ position is the source of active metabolites;
an OH at the ___ position causes rapid excretion;
1;
3
name the 4 short acting benzo’s
do these have higher or lower addictive potential?
ATOM =
alprazolam, triazolam, oxazepam, midazolam;
higher
benzo’s generally end in ___ or ____
olam, epam
oxazepam is the active metabolite of ____, which is a long lasting benzo
diazepam
most of the benzo’s have ____ half lives and form ____ metabolites. they are ____ by the liver and eventually excreted _____
long;
active;
conjugated;
renally
____, _____, and ____ are metabolized Outside The Liver
oxazepam, temazepam, lorazepam
long acting vs intermediate/rapid eliminated benzos:
which are preferred in patietns with liver problems?
preferred in elderly?
can accumulate?
rapid tolerance?
intermediate/rapid;
rapid;
long acting;
rapid
benzo effect on sleep: \_\_\_\_ REM sleep. \_\_\_\_ stage 3 and 4 (Deep sleep); \_\_\_\_\_ total sleep; \_\_\_\_\_ sleep latency
decrease,
decrease;
increase (increase stage 2);
reduce
benzo’s:
can be used for ____ withdrawl (ie ____);
cause ____ amnesia, which can be useful for chill surgery’s;
muscle _____
alcohol (DTs);
anterograde;
relaxant
also treat anxiety, spasticity, epilepsy etc
benzo side effects:
more or less severe than barbituates?
cause central ____, somnolence, and confusion, especially in ___ patients.
tolerance and physical addiction
less;
ataxia;
elderly
_____ is used to treat benzo overdoses;
2 bad side effects (starred in notes)
flumazenil;
panic attack, withdrawl seizure
name the 3 non-benzo hypnotics;
do these bind at the same or different site from benzos?
zolpidem, zaleplon, eszopiclone (3 zzzs);
same (but have higher specificity)
zolpidem, zalepolon, eszopiclone:
which are used to help fall asleep ie ____ acting?;
which has a longer half-life?
which can be used for sleep maintenance and onset?
zolpidem, zaleplon = short acting;
eszopliclone;
eszopliclone
the Z-hypnotics: metabolized by \_\_\_\_; treat overdose with \_\_\_\_\_; ataxia, headaches, confusion... addiction risk?
liver enzymes (p450’s);
flumazenil;
pretty low
