Sedatives & hypnotics

Question 1

An effective sedative agent should reduce _____ & exert a _______

Answer 1

anxiety

a calming effect

Question 2

Hypnotic drugs should produce _______ & encourage the onset & maintenance of a ______

Answer 2

drowsiness

state of sleep

Question 3

Describe the absorption & distribution of sedative-hypnotic drugs

Answer 3

lipid soluble

Good distribution to the brain

Question 4

Describe the metabolism & excretion of sedative-hypnotic drugs

Answer 4

Metabolized by hepatic enzymes

Active & inactive metabolites

Question 5

What is the MOA of benzos?

Answer 5

Facilitates the inhibitory actions of GABA

Question 6

Receptors for benzodiazepines are located in what 3 brain regions?

Answer 6

Thalamus
Limbic structures
Cerebral cortex

Question 7

What are benzos used for?

Answer 7

Anxiety 
Panic attacks 
Insomnia 
Skeletal muscle relaxation
Seizures

Question 8

Toxicity of sedative-hypnotics (benzos, newer hypnotic drugs, barbiturates) can lead to what?

Answer 8

Extension of CNS depressant actions

Dependence (barbiturates > benzos)

Question 9

What should you remember about diazepam?

Answer 9

Active metabolites

Erratic bioavailability from IM injection

Question 10

Which drug has active metabolites w/ long half-lives?

Answer 10

Flurazepam

Question 11

Which drugs have no active metabolites? (3)

Answer 11

Lorazepam

Oxazepam

Zolpidem

Question 12

High doses of benzos w/ long or intermediate half-lives have a greater potential to produce…

Answer 12

daytime sedation

psychomotor incoordination

cognitive deficits

Question 13

What are ADEs of benzos?

Answer 13

anterograde amenesia

rebound insomnia

*Start at lowest effective dose to avoid these

Question 14

The FDA requires labeling for benzos & barbiturates to include a caution regarding… (3)

Answer 14

anaphylaxis

facial angioedema

complex sleep behaviors (sleep driving or eating, phone calls)

Question 15

What is the MC type of drug interaction w/ sedative-hypnotics?

Answer 15

Additive CNS depression effects

Question 16

What are examples of substances that interact w/ sedative-hypnotics?

Answer 16

Alcohol 
Antihistamines 
Antipsychiotic
Opioids
TCAs

Question 17

Overdosage of sedative-hypnotics can result in…

Answer 17

respiratory & CV depression

Question 18

What drug may reverse CNS depressant effects?

Answer 18

Flumazenil

Question 19

What is the MOA of flumazenil?

Answer 19

Antagonist at benzo sites on GABA receptor

Antagonist to benzos & the newer hyponotic drugs only

Question 20

What are ADEs of flumazenil?

Answer 20

Agitation, confusion

Withdrawal syndrome

Question 21

What are 3 newer hypnotic drugs (not among the benzo class)?

Answer 21

Zolpidem
Zaleplon
Eszopiclone

Question 22

What is the MOA of the newer hypnotics?

Answer 22

Bind to GABA receptor sites

Facilitate Cl channel opening

Question 23

What is the MOA of barbiturates (“tal”) ?

Answer 23

Prolongs the inhibitory effects of GABA & glycine

Question 24

What are barbiturates (“tal”) used for?

Answer 24

anesthesia

insomnia & sedation

seizures

Question 25

Which 2 drug classes induce liver enzymes? What does this cause?

Answer 25

Barbiturates & carbamates Drug interactions

Question 26

Which 2 antihistamines are more sedating than pyrilamine?

Answer 26

Diphenhydramine & doxylamine

Question 27

Which antidepressant has FDA approval for the tx of sleep maintenance insomnia?

Answer 27

Doxepin

Question 28

Which antidepressant may promote sleep?

Answer 28

Mirtazapine

Question 29

Which antidepressant can be given at bedtime to improve sleep continuity?

Answer 29

Trazodone

Question 30

What are ADEs of trazadone?

Answer 30

Carryover sedation Alpha-adrenergic blockade - orthostasis Priapism

Question 31

What are 2 ADEs of mirtazapine?

Answer 31

Daytime sedation Wt gain

Question 32

Which melatonin-receptor agonist is approved for the tx of sleep-onset insomnia?

Answer 32

Ramelteon

Question 33

Ramelteon forms active metabolite via...

Answer 33

CYP1A2

Question 34

What are the MC ADEs of ramelteon?

Answer 34

HA, dizziness, somnolence

Question 35

Ramelton is helpful for sleep- onset difficulties in what 2 conditions?

Answer 35

COPD & sleep apnea

Question 36

What is the main complaint regarding valerian (an herbal sleep remedy)?

Answer 36

Smells like old gym socks

Question 37

What is the MOA of buspirone?

Answer 37

Selective anxiolytic Partial agonist at 5-HT receptors & D2 receptors Interacts w/ 5-HT1A subclass of serotonin receptors

Question 38

What effects does buspirone express?

Answer 38

Minimal CNS depressant effects

Question 39

Describe the onset of action of buspirone

Answer 39

Slow (> 1 week)

Question 40

Does buspirone form active metabolite? What does buspirone interact w/?

Answer 40

Yes CYP3A4 inducers & inhibitors

Question 41

What are the ADEs of buspirone?

Answer 41

GI distress, tachy Paresthesia Tolerance is minimal w/ chronic use Little rebound anxiety or withdrawal sx upon discontinuance

Question 42

Is buspirone safe in pregnancy?

Answer 42

yes appears to be

Question 43

Which classes of drugs are used for tx of panic d/o?

Answer 43

SSRIs, SNRI Benzos TCA MOI

Question 44

Which SSRI can cause QT prolongation?

Answer 44

Citalopram

Question 45

What classes of drugs are used for tx of social anxiety d/o?

Answer 45

SSRIs, SNRI | Benzos

Question 46

What are examples of stimulus control procedures used for sleep hygiene?

Answer 46

Avoid blue spectrum light from TV, phones, tablets Schedule worry time during the day; do not take troubles to bed

Question 47

What is another sleep hygiene recommendation?

Answer 47

Avoid illuminated clocks the bedroom

Question 48

What are some of the clinical uses of sedative-hypnotics?

Answer 48

Relief of anxiety Insomnia Control of withdrawal states

Question 49

What 2 drugs have the potential to lead to coma?

Answer 49

Barbiturates & alcohol