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Pharm II Exam 4 > Sedatives & hypnotics > Flashcards

Sedatives & hypnotics Flashcards

1
Q

An effective sedative agent should reduce _____ & exert a _______

A

anxiety

a calming effect

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2
Q

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

A

drowsiness

state of sleep

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3
Q

Describe the absorption & distribution of sedative-hypnotic drugs

A

lipid soluble

Good distribution to the brain

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4
Q

Describe the metabolism & excretion of sedative-hypnotic drugs

A

Metabolized by hepatic enzymes

Active & inactive metabolites

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5
Q

What is the MOA of benzos?

A

Facilitates the inhibitory actions of GABA

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6
Q

Receptors for benzodiazepines are located in what 3 brain regions?

A

Thalamus
Limbic structures
Cerebral cortex

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7
Q

What are benzos used for?

A 
Anxiety 
Panic attacks 
Insomnia 
Skeletal muscle relaxation
Seizures
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8
Q

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

A

Extension of CNS depressant actions

Dependence (barbiturates > benzos)

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9
Q

What should you remember about diazepam?

A

Active metabolites

Erratic bioavailability from IM injection

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10
Q

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

A

Flurazepam

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11
Q

Which drugs have no active metabolites? (3)

A

Lorazepam

Oxazepam

Zolpidem

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12
Q

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

A

daytime sedation

psychomotor incoordination

cognitive deficits

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13
Q

What are ADEs of benzos?

A

anterograde amenesia

rebound insomnia

*Start at lowest effective dose to avoid these

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14
Q

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

A

anaphylaxis

facial angioedema

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

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15
Q

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

A

Additive CNS depression effects

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16
Q

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

A 
Alcohol 
Antihistamines 
Antipsychiotic
Opioids
TCAs
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17
Q

Overdosage of sedative-hypnotics can result in…

A

respiratory & CV depression

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18
Q

What drug may reverse CNS depressant effects?

A

Flumazenil

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19
Q

What is the MOA of flumazenil?

A

Antagonist at benzo sites on GABA receptor

Antagonist to benzos & the newer hyponotic drugs only

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20
Q

What are ADEs of flumazenil?

A

Agitation, confusion

Withdrawal syndrome

21
Q

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

A

Zolpidem
Zaleplon
Eszopiclone

22
Q

What is the MOA of the newer hypnotics?

A

Bind to GABA receptor sites

Facilitate Cl channel opening

23
Q

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

A

Prolongs the inhibitory effects of GABA & glycine

24
Q

What are barbiturates (“tal”) used for?

A

anesthesia

insomnia & sedation

seizures

25
Q

Which 2 drug classes induce liver enzymes?

What does this cause?

A

Barbiturates & carbamates

Drug interactions

26
Q

Which 2 antihistamines are more sedating than pyrilamine?

A

Diphenhydramine & doxylamine

27
Q

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

A

Doxepin

28
Q

Which antidepressant may promote sleep?

A

Mirtazapine

29
Q

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

A

Trazodone

30
Q

What are ADEs of trazadone?

A

Carryover sedation

Alpha-adrenergic blockade - orthostasis

Priapism

31
Q

What are 2 ADEs of mirtazapine?

A

Daytime sedation

Wt gain

32
Q

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

A

Ramelteon

33
Q

Ramelteon forms active metabolite via…

A

CYP1A2

34
Q

What are the MC ADEs of ramelteon?

A

HA, dizziness, somnolence

35
Q

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

A

COPD & sleep apnea

36
Q

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

A

Smells like old gym socks

37
Q

What is the MOA of buspirone?

A

Selective anxiolytic

Partial agonist at 5-HT receptors & D2 receptors

Interacts w/ 5-HT1A subclass of serotonin receptors

38
Q

What effects does buspirone express?

A

Minimal CNS depressant effects

39
Q

Describe the onset of action of buspirone

A

Slow (> 1 week)

40
Q

Does buspirone form active metabolite?

What does buspirone interact w/?

A

Yes

CYP3A4 inducers & inhibitors

41
Q

What are the ADEs of buspirone?

A

GI distress, tachy

Paresthesia

Tolerance is minimal w/ chronic use

Little rebound anxiety or withdrawal sx upon discontinuance

42
Q

Is buspirone safe in pregnancy?

A

yes appears to be

43
Q

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

A

SSRIs, SNRI
Benzos
TCA
MOI

44
Q

Which SSRI can cause QT prolongation?

A

Citalopram

45
Q

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

A

SSRIs, SNRI

Benzos

46
Q

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

A

Avoid blue spectrum light from TV, phones, tablets

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

47
Q

What is another sleep hygiene recommendation?

A

Avoid illuminated clocks the bedroom

48
Q

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

A

Relief of anxiety

Insomnia

Control of withdrawal states

49
Q

What 2 drugs have the potential to lead to coma?

A

Barbiturates & alcohol

Pharm II Exam 4 (14 decks)

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