Sedatives & hypnotics Flashcards Preview

Pharm II Exam 4 > Sedatives & hypnotics > Flashcards

Flashcards in Sedatives & hypnotics Deck (49):
1

An effective sedative agent should reduce _____ & exert a _______

anxiety

a calming effect

2

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

drowsiness

state of sleep

3

Describe the absorption & distribution of sedative-hypnotic drugs

lipid soluble

Good distribution to the brain

4

Describe the metabolism & excretion of sedative-hypnotic drugs

Metabolized by hepatic enzymes

Active & inactive metabolites

5

What is the MOA of benzos?

Facilitates the inhibitory actions of GABA

6

Receptors for benzodiazepines are located in what 3 brain regions?

Thalamus
Limbic structures
Cerebral cortex

7

What are benzos used for?

Anxiety
Panic attacks
Insomnia
Skeletal muscle relaxation
Seizures

8

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

Extension of CNS depressant actions

Dependence (barbiturates > benzos)

9

What should you remember about diazepam?

Active metabolites

Erratic bioavailability from IM injection

10

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

Flurazepam

11

Which drugs have no active metabolites? (3)

Lorazepam

Oxazepam

Zolpidem

12

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

daytime sedation

psychomotor incoordination

cognitive deficits

13

What are ADEs of benzos?

anterograde amenesia

rebound insomnia

*Start at lowest effective dose to avoid these

14

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

anaphylaxis

facial angioedema

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

15

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

Additive CNS depression effects

16

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

Alcohol
Antihistamines
Antipsychiotic
Opioids
TCAs

17

Overdosage of sedative-hypnotics can result in...

respiratory & CV depression

18

What drug may reverse CNS depressant effects?

Flumazenil

19

What is the MOA of flumazenil?

Antagonist at benzo sites on GABA receptor

Antagonist to benzos & the newer hyponotic drugs only

20

What are ADEs of flumazenil?

Agitation, confusion

Withdrawal syndrome

21

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

Zolpidem
Zaleplon
Eszopiclone

22

What is the MOA of the newer hypnotics?

Bind to GABA receptor sites

Facilitate Cl channel opening

23

What is the MOA of barbiturates ("tal") ?

Prolongs the inhibitory effects of GABA & glycine

24

What are barbiturates ("tal") used for?

anesthesia

insomnia & sedation

seizures

25

Which 2 drug classes induce liver enzymes?

What does this cause?

Barbiturates & carbamates

Drug interactions

26

Which 2 antihistamines are more sedating than pyrilamine?

Diphenhydramine & doxylamine

27

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

Doxepin

28

Which antidepressant may promote sleep?

Mirtazapine

29

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

Trazodone

30

What are ADEs of trazadone?

Carryover sedation

Alpha-adrenergic blockade - orthostasis

Priapism

31

What are 2 ADEs of mirtazapine?

Daytime sedation

Wt gain

32

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

Ramelteon

33

Ramelteon forms active metabolite via...

CYP1A2

34

What are the MC ADEs of ramelteon?

HA, dizziness, somnolence

35

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

COPD & sleep apnea

36

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

Smells like old gym socks

37

What is the MOA of buspirone?

Selective anxiolytic

Partial agonist at 5-HT receptors & D2 receptors

Interacts w/ 5-HT1A subclass of serotonin receptors

38

What effects does buspirone express?

Minimal CNS depressant effects

39

Describe the onset of action of buspirone

Slow (> 1 week)

40

Does buspirone form active metabolite?

What does buspirone interact w/?

Yes

CYP3A4 inducers & inhibitors

41

What are the ADEs of buspirone?

GI distress, tachy

Paresthesia

Tolerance is minimal w/ chronic use

Little rebound anxiety or withdrawal sx upon discontinuance

42

Is buspirone safe in pregnancy?

yes appears to be

43

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

SSRIs, SNRI
Benzos
TCA
MOI

44

Which SSRI can cause QT prolongation?

Citalopram

45

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

SSRIs, SNRI
Benzos

46

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

Avoid blue spectrum light from TV, phones, tablets

Schedule worry time during the day; do not take troubles to bed

47

What is another sleep hygiene recommendation?

Avoid illuminated clocks the bedroom

48

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

Relief of anxiety

Insomnia

Control of withdrawal states

49

What 2 drugs have the potential to lead to coma?

Barbiturates & alcohol