Anti Sedatives/ Hypnotics

Front 1

Inhibitory Neurotransmitter is?
Excitatory Neurotransmitter is?
Which one causes depolarization/ hyperpolarization?
What are the ionotropic receptors & metabotropic receptors for each?

Back 1

GABA-inhibitory-hyperpolarization
Ionotropic- GABAa and GABAc
Metabotropic-GABAb

Glutamate- Excitatory-depolorization
Ionotropic-NMDA, AMPA, kainase
metabotropic- Mglur

Front 2

alpha 1 receptor is linked to...
alpha 2 GABAa, alpha3 GABAa is linked to...

Back 2

alpha1- sedation, hypnosis
alpha 2,alpha 3- anxiety

Front 3

BDZs work as positive allosteric modulators and do/ do not activate GABA receptors in the absence of GABA

Back 3

DO NOT!

Front 4

BDZs are used for all of these EXCEPT:
a) Anxiety
b)alcohol withdrawal syndrome
c) epilepsy
d) status epilepticus
e)muscle relaxants

Back 4

c) Epilepsy

Front 5

Midazoloam (Versed) is a short acting/ intermediate acting/ long acting BDZ and is used as...

Back 5

Short acting! used for pre-anesthesia, pre-op- fast onset of effect used IV, IM

Front 6

Triazolam (Halcion) has a very __ onset of effect and is used orally to decrease time of sleep but what is one of the problems?

Back 6

fast onset of effect- causes rebound insominia- short duration of action- doesn't prolong sleep

Front 7

What is rebound insominia?

Back 7

When using BDZs chronically, GABA becomes dysfunctional- (downregulation of GABA)when you stop drug, insominia will come back

Front 8

Alprazoloam(Xanax) is used orally, is therapeutically used for and tolerance only develops with..

Back 8

used for anxiety disorders phobias,tolerance only develops with sedation
also, it is intermediate acting

Front 9

Estazoloam (Prosom) is used orally and is used for...

Back 9

insomnia

Front 10

Lorazapem(Ativan) can be used orally, IV, or IM and what is different about this drug?

Back 10

It is intermediate acting and used for status epilepticus

Front 11

Oxazepam(Serax) has a ___ onset of action because it is more hydrophillic

Back 11

delayed

Front 12

Temazapem (Restorial), Oxazepam (Serax), and Lorazapem (Ativan) are all metabolized in the

Back 12

kidneys- directly glucuronidated- good for drug-drug interactions with CYP 450, geriatric pts, and hepatatic dysfunction

Front 13

Which drug is FDA approved for alcohol withdrawal management?
a) Clonazapem (Klonopin)
b)Oxazepam (Serax)
c) Diazepam (Valium)
d) Chlordiazepoxide (Librium))
e) Alprazolam (Xanax)

Back 13

d) Chlordiazepoxide (Librium)

Front 14

Clorazepate (Tranxene) is a prodrug so it has ___ onset of action

Back 14

delayed

Front 15

All of these have active metabolites EXCEPT:
a) Chlorodiazpeoxide
b)Diazepam
c)Flurazepam
d)Alprazolam
e)Estazolam

Back 15

e)Estazolam

Front 16

Which one of these BDZs has the fastest onset of action?
a) Flurazepam
b) Quazepam
c)Alprazolam
d)Diazepam
e)Midazolam

Back 16

d) Diazepam- favored for status epilepticus

Front 17

CYP 3A4 inhibitors may ___the duration of effect of BDZs and CYP 3A4 inducers may ___ BDZ's effectiveness.

Back 17

prolong, reduce

Front 18

With chronic use, BDZs have pharmacodynamic tolerance because of:

Back 18

GABAa receptor desenitization
Evidence of downregulation of GABAa receptor subunit expression

Front 19

Which drug would have more a dependence effect, Diazepam or Oxazepam?

Back 19

Diazapem because its onset of action is faster and Oxazepam is a polar compound and has a slow onset of effect

Front 20

How would abrupt discontinuation of BDZs lead to seizures?

Back 20

Because GABA is inhibitory- if GABA is dysfuntional, there is an imbalance of excitatory and inhibitory, and you would see more excitatory effects leading to seizures

Front 21

BDZs with short half produces ___ withdrawal symptoms compared to agents with longer half life.

Back 21

more pronounced.

Front 22

To treat BDZ withdrawal symptom, you should

Back 22

substitute with a BDZ with longer half life (e.g. diazepam) or adjunctive treatment with propanolol

Front 23

Anterograde amnesia is a side effect of BDZs..what is it?

Back 23

Short term memory loss after drug is taken

Front 24

What is the date rape drug?

Back 24

Fluinitrazepam (Rophynl)

Front 25

What will alcohol do with BDZs?

Back 25

augment GABA- increased drowsiness can lead to CNS depression

Front 26

When you take Alprazolam(Xanax), you might experience ___ at first, but it will be gone soon.

Back 26

drowsiness

Front 27

BDZs related drugs are selective for alpha1 GABAa and therefore only treat _____.

Back 27

insomnia

Front 28

Eszoplicone (Lunesta) is approved for

Back 28

long term treatment of insomnia.

Front 29

To reverse BDZ sedation, this drug can be used:
a) Lunesta
b)Fluintrazepam
c)Flumazenil
d)Diazepam
e)Phenobarbital

Back 29

c)Flumazenil(Romazicon)
It is a BDZ antagonist- binds with high affinity to GABA

Front 30

Barbiturates are:
a)Positive allosteric modulators
b) Increase Cl- current
c) Weak agonists at GABAa
d)have a higher efficacy than BDZs
e) All of the above

Back 30

e) All of the above

Front 31

Barbiturates are non competitve antagonists at ____ glutamate receptor by preventing opening of channels, preventing depolarization.

Back 31

AMPA

Front 32

Which one of these barbiturates is used to treat increased intracranial pressure?
a) Amobarbital
b)Phenobarbital
c)Thiopental
d)Methohexital
e)Secobarbital

Back 32

c) Thiopental (Pentothal)

Front 33

Which barbiturate indcues medical coma?
a) Amobarbital
b)Pentobarbital
c)Thiopental
d)Methohexital
e)Secobarbital

Back 33

b)Pentobarbital

Front 34

Phenobarbital(Luminal) is a ___acting barbiturate and is an anticonvulsant, used for status epilepticus, and pre-op sedation.

Back 34

long acting

Front 35

Barbiturates have both pharmacodynamic and pharmacokinetic tolerance. Pharmokinetic tolerance- is the upregulation of CYP450 enzymes. What does this mean?

Back 35

Auto induction- drug induces its own metabolism as well have drug interction with metabolism of CYP3A4, CYP3A5, and CYP3A7

Front 36

Ramelton (Rozarerem) is a:

Back 36

Mt1 and Mt2 receptor agonsit
Mt1- induces sleep
MT2- regulates circadian rhythm
Ramelton more selective for MT1

-No tolerance of withdrawal development
Less residual hypnotic side effect

Front 37

Buspirone(Buspar) has partial agonist effect at the___ receptor and is an adjunctive treatment for anxiety of mild to moderate intensity.

Back 37

5HT1A-Serotonin- anxiolytic effect- not that effective because partial agonist