Lecture 4 Sedative/Hypotics

Question 1

a ____ calms anxiety, decreases excitement ;

a ____ induces sleep (refreshing)

Answer 1

sedative,

hypnotic

Question 2

the _____ ____ regulates sleep-wake transitions and synchronization of the EEG

Answer 2

reticular formation

Question 3

stage N3/4 of sleep:

___ waves occur that have ____ frequency and ____ amplitde. it is the ____ non-REM sleep

Answer 3

delta,
low, high;
deepest

Question 4

REM sleep and awake:

both have ____ waves

Answer 4

beta

Question 5

the GABAa receptor acts as a ____ channel when bound

Answer 5

Cl

pentameric

Question 6

GABAa receptor:
the orthersteric site (Where GABA binds) is ___ and ___;
Benzos bind the ortho or allosteric site?
location of this site?

Answer 6

alpha 1, beta 2;

allosteric–alpha 1, gamma 2

Question 7

benzo’s increase the ____ of Cl- channel opening.

what drug binds the same location as benzo’s but is an antagonist?

Answer 7

FREQUENCY;

flumazenil

Question 8

____ and ____ bind to different allosteric sites of the GABAa receptor

Answer 8

barbituates, alcohol

Question 9

barbituates increase the _____ of GABAa channel opening

Answer 9

duration

Question 10

name a GABA channel blocker?

Answer 10

picrotoxin

Question 11

benzo structure things:
alkylation at the ____ position is the source of active metabolites;
an OH at the ___ position causes rapid excretion;

Answer 11

1;

3

Question 12

name the 4 short acting benzo’s

do these have higher or lower addictive potential?

Answer 12

ATOM =
alprazolam, triazolam, oxazepam, midazolam;

higher

Question 13

benzo’s generally end in ___ or ____

Answer 13

olam, epam

Question 14

oxazepam is the active metabolite of ____, which is a long lasting benzo

Answer 14

diazepam

Question 15

most of the benzo’s have ____ half lives and form ____ metabolites. they are ____ by the liver and eventually excreted _____

Answer 15

long;
active;
conjugated;
renally

Question 16

____, _____, and ____ are metabolized Outside The Liver

Answer 16

oxazepam, temazepam, lorazepam

Question 17

long acting vs intermediate/rapid eliminated benzos:
which are preferred in patietns with liver problems?
preferred in elderly?
can accumulate?
rapid tolerance?

Answer 17

intermediate/rapid;
rapid;
long acting;
rapid

Question 18

benzo effect on sleep:
\_\_\_\_ REM sleep.
\_\_\_\_ stage 3 and 4 (Deep sleep);
\_\_\_\_\_ total sleep;
\_\_\_\_\_ sleep latency

Answer 18

decrease,
decrease;
increase (increase stage 2);
reduce

Question 19

benzo’s:
can be used for ____ withdrawl (ie ____);
cause ____ amnesia, which can be useful for chill surgery’s;
muscle _____

Answer 19

alcohol (DTs);
anterograde;
relaxant

also treat anxiety, spasticity, epilepsy etc

Question 20

benzo side effects:
more or less severe than barbituates?
cause central ____, somnolence, and confusion, especially in ___ patients.
tolerance and physical addiction

Answer 20

less;
ataxia;
elderly

Question 21

_____ is used to treat benzo overdoses;

2 bad side effects (starred in notes)

Answer 21

flumazenil;

panic attack, withdrawl seizure

Question 22

name the 3 non-benzo hypnotics;

do these bind at the same or different site from benzos?

Answer 22

zolpidem, zaleplon, eszopiclone (3 zzzs);

same (but have higher specificity)

Question 23

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?

Answer 23

zolpidem, zaleplon = short acting;
eszopliclone;
eszopliclone

Question 24

the Z-hypnotics:
metabolized by \_\_\_\_;
treat overdose with \_\_\_\_\_;
ataxia, headaches, confusion...
addiction risk?

Answer 24

liver enzymes (p450’s);
flumazenil;
pretty low

Question 25

3 of the barbituates end in “___”

Answer 25

barbital ie

phenobarbital, pentobarbital, secobarbital

Question 26

thiopental is a _____ acting barb and is used for ____

Answer 26

ultra short; IV anesthesia

Question 27

phenobarbital is a ____ acting barb and is used primarily for ____

Answer 27

long;
anticonvulsant

similar to mephobarbital

Question 28

2 bad effects that barbs have at high doses:

Answer 28

cardiac depression, respiratory depression

both can lead to death

Question 29

barbs are cytochrome P450 ____

Answer 29

inducers

Question 30

thiopental has ____ lipid solubility. why does it have such short action?

Answer 30

high;

rapid redistribution to peripheral tissues

Question 31

GABAb receptor:
presynaptically, it \_\_\_\_\_ Ca conductance;
post-synaptically, it \_\_\_\_ K conduction;
overall = \_\_\_\_ effect;
it is coupled to what?

Answer 31

decreases;
increases;
inhibit;
a Gi protein

Question 32

____ is a GABAb receptor activator at the _____ level. it does what?

Answer 32

baclofen;
spinal cord;
induces skeletal muscle relaxation

phaclofen, saclofen are antagonists

Question 33

sodium oxybate is also called ____. it binds ___ and ____ receptors

Answer 33

GHB (gamma hydroxybutyric acid);

GABAa, GABAb, (maybe GHB receptor)

Question 34

GHB is used for what clinically?

Answer 34

narcolepsy

used illicitly for date-rape, raving