Sleep-Wake Disorders

Question 1

What is sedation?

Answer 1

reduces anxiety and evokes a calming effect/anxiolytic

-CNS depression

Question 2

What is hypnotic?

Answer 2

evokes drowsiness and sleep maintenance

-higher degree of CNS depression than sedation

Question 3

Explain dose-response curve?

Answer 3

Drug A: Barbiturates and alcohol, increase dose has additive effect
Drug B: Benzodiazepines, plateau’s

Question 4

Explain absorption and distribution of sedative-hypnotic drugs? (3)

Answer 4

• lipid soluble
• good distribution to brain
• absorb well from GI tract

Question 5

What is metabolism and excretion of sedative hypnotic drugs?

Answer 5

• active and inactive metabolites
• metabolized before excretion
• mainly by liver enzymes

Question 6

What is tx for insomnia?

Answer 6

Benzodiazepines

Question 7

Name the benzos for insomnia? (8)

Answer 7

Estazolam
Eszopiclone 
Flurazepam
Quazepam
Temazepam 
Triazolam 
Zaleplon
Zolpidem

Question 8

T/F New nonbenzos Gaba agonist only have sedative effects?

Answer 8

True

Question 9

What is MOA of benzondiazepines?

Answer 9

bind to benzo receptors in cerebral cortex, thalamus,
and limbic structures
-facilitate inhibitory action of GABA

Question 10

What are clinical uses of benzos? (5)

Answer 10

insomnia
muscle relaxant
GAD
panic attacks 
seizures

Question 11

What is 1/2 life of benzos?

Answer 11

2-4 hrs

Question 12

Where are benzos metabolized?

Answer 12

liver

Question 13

Which benzos do not have active metabolites? (3)

Answer 13

lorazepam
oxazepam
zolpidem

Question 14

Which benzo is rapid onset and short duration?

Answer 14

Alpralozam

Triazolam

Question 15

Which benzo has a long half life and and active metabolite?

Answer 15

Flurazepam

Question 16

Which benzo is a prodrug?

Answer 16

Clorazepate

Question 17

Which benzo is absorbed slowly?

Answer 17

Temazepam

Question 18

What are ADE of benzos?

Answer 18

daytime sedation
tolerance 
cognitive impairment
anterograde amnesia  
rebound insomnia
anaphylaxis angioedema

Question 19

name drug interactions with benzos?

Answer 19

alcohol
opiods
anti-psychotic
tricyclic anti depressant

Question 20

Which drug reverses the CNS depressive effects of benzos, eszopiclone, zolpidem, and zaplenon?

Answer 20

Flumazenil

Question 21

What is MOA of Flumazenil?

Answer 21

antagonist, binds benzo receptors

Question 22

What is PK of flumazenil?

Answer 22

short acting IV

Question 23

ADE of flumazenil?

Answer 23

agitation, confusion

Question 24

Name the three newer hypnotics, not benzos?

Answer 24

• zolpidem
• eszoplicone
• zaleplon

Question 25

What is MOA of newer hypnotics?

Answer 25

- more selective | - bind to GABA receptor isoforms BZ1 and W1

Question 26

What is MOA of barbituates?

Answer 26

- bind at other sites on benzo receptor to facilitate action of GABA - not antagonized by flumazenil - blocks glutamate and sodium channels

Question 27

what are uses of barbs?

Answer 27

anesthesia | insomnia

Question 28

PK of barbs?

Answer 28

oral | liver metabolism

Question 29

toxicities of barbs?

Answer 29

tolerance and dependence

Question 30

what is tx for mild insomina?

Answer 30

anti-histamines | diphenyhydramine and doxylamine best

Question 31

what is tx for sleep maintenance insomnia?

Answer 31

anti-depressants | low dose doxepin

Question 32

If patient has abuse issues which med is given for sleep maintenance?

Answer 32

Trazadone

Question 33

what is MOA of surovexant?

Answer 33

orexin a and b antagonits | turns off wake signal

Question 34

what type of insomnia does surovexant tx?

Answer 34

helps with falling asleep and staying asleep

Question 35

What is MOA of Ramelton?

Answer 35

melatonin antagonist

Question 36

ADE of Ramelton?

Answer 36

dizziness, headaches, somnolence

Question 37

what does Ramelton tx?

Answer 37

sleep onset insomnia | helps in pt with COPD and sleep apnea

Question 38

Which herb has sedative-hypnotic properties?

Answer 38

Valerian root

Question 39

What are the four characteristics of Narcolepsy?

Answer 39

1. EDS 2. Cataplexy: sudden loss of bilateral muscle tone 3. hallucinations 4. sleep paralysis

Question 40

What is pathology in Narcolepsy?

Answer 40

dysfunction with hypocretin/orexin system

Question 41

What is used to tx excessive daytime sleepyness in Narcolepsy

Answer 41

modafinil ,armodafinil

Question 42

T/F Methylphenidate can cause dependence issues?

Answer 42

TRUE

Question 43

What is MOA for Cataplexy?

Answer 43

block re uptake of 5'HT and norepi at locus cerelus and raphe and supress REM sleep

Question 44

which meds are used to tx cataplexy

Answer 44

imipramine fluoxetine nortriptyline clomipramine

Question 45

what is used to tx EDS and cataplexy?

Answer 45

Selegiline

Question 46

What is used to tx EDS, catalpexy, hallucinations?

Answer 46

Sodium oxybate

Question 47

What is MOA of sodium oxybate?

Answer 47

changes sleep architecture to resemble normal potent not to be used by any other increases slow wave sleep, decrease night timee awakenings and increases REM sleep