Chapter 37 - Sedative-Hypnotic Drugs Flashcards

1
Q

Sedative-hypnotics _________ CNS function

A

depress

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2
Q

What are sedative hypnotics used to treat?

A

anxiety and insomnia

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3
Q

How are antianxiety and hypnotic effects distinguished?

A

dosage

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4
Q

What is the most well known Benzodiazepine?

A

Diazepam (Valium)

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5
Q

What is the most prescribed benzodiazepine?

A

Lorazepam (Ativan)

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6
Q

Benefits of benzodiazepines over other CNS drugs:

A

-safer
-lower potential for abuse
-less tolerance and physical dependence
-fewer drug interactions

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7
Q

What are benzodiazepines used for?

A

-inducing general anesthesia
-seizure disorders
-muscle spasms
-alcohol withdrawal

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8
Q

How do Benzodiazepines act?

A

potentiate action of GABA

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9
Q

What do Benzodiazepines do to the CNS?

A

-reduce anxiety
-promote sleep

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10
Q

How do oral benzodiazepines affect the CV system?

A

they hardly do

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11
Q

How do IV benzodiazepines affect the CV system?

A

-hypotension
-possible cardiac arrest

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12
Q

How do benzodiazepines affect the respiratory system?

A

weak depression, even in toxic doses

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13
Q

Benzodiazepines (are/are not) lipid soluble

A

are

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14
Q

Most benzodiazepines undergo hepatic metabolism with active metabolites but which drugs have LESS extensive metabolism but NO METABOLITES…

A

Lorazepam
Oxazepam
Temazepam
Triazolam

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15
Q

Most benzodiazepines undergo hepatic metabolism with active metabolites but which drugs have extensive metabolism but NO METABOLITES…

A

Clonazepam

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16
Q

Diazepam, clonazepam, and flurazepam are _____ acting and have a half life of 3-100hrs

A

long

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17
Q

Triazolam, Lorazepam, and Alprazolam (Xanax) are ______ acting and have a half life of 2-20hrs

A

short

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18
Q

What are the adverse effects of Benzodiazepines?

A

-dizziness
-drowsiness
-confusion
-anterograde amnesia
-sleep depriving
-risk of falls (elderly)
-paradoxical effects (elderly)
-abuse
-withdrawal reaction
-respiratory depression (when injected or combined)

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19
Q

Are benzodiazepines safe during pregnancy?

A

no - risk category D and X

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20
Q

What do benzodiazepines interact with?

A

other CNS depressants

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21
Q

Does tolerance develop from Benzodiazepines?

A

to some effects but not others with prolonged use

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22
Q

What are the symptoms of an oral benzodiazepine overdose?

A

-drowsiness
-lethargy
-confusion

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23
Q

What are the symptoms of IV benzodiazepine overdose?

A

-life-threatening reactions
-hypotension
-respiratory and cardiac arrest

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24
Q

How is oral benzodiazepine overdose treated?

A

-gastric lavage
-saline cathartic
-dialysis

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25
Q

What is the reversal agent for acute benzodiazepine overdose?

A

flumazenil

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26
Q

What is flumazenil?

A

-competitive benzo receptor antagonist

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27
Q

What does flumazenil do?

A

reverse sedative effects but not respiratory depression

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28
Q

When does flumazenil work?

A

benzo OD and reversing effects after general anesthesia

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29
Q

How is flumazenil administered?

A

IV over 15s and repeated every min to a max dose of 3mg

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30
Q

Which benzodiazepines are available orally?

A

all of them

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31
Q

How is diazepam usually administered?

A

IV

32
Q

How is lorazepam usually administered?

A

IM

33
Q

What sedative class is zolpidem?

A

benzodiazepine-like drugs

34
Q

What is Zolpidem?

A

a hypnotic for short-term management of insomnia

35
Q

How does Zolpidem act?

A

interacting with a GABA-BZ receptor complex that bind to BZ1 and some a1 receptors

36
Q

Does long-term Zolpidem use involve tolerance or increased AE?

A

generally no

37
Q

What are the side effects of Zolpidem?

A

-drowsiness
-dizziness
-headache
-confusion
-euphoria
-muscle aches

38
Q

How is Zolpidem administered?

A

sublingually

39
Q

What is the initial Zolpidem dose for women?

A

5mg

40
Q

What is the initial Zolpidem dose for men?

A

5-10mg

41
Q

When should Zolpidem be taken?

A

before bed with 7-8hrs before awakening

42
Q

Why does Zolpidem have a risk for morning driving impairment?

A

high blood levels after 10mg use overnight

43
Q

What sedative class is Zopiclone?

A

benzodiazepine-like drugs

44
Q

What is Zopiclone used for?

A

insomnia

45
Q

How does Zopiclone act?

A

binding to the GABA𝚊 A1 subunit in the brain

46
Q

What is the most common AE of Zopiclone?

A

bitter aftertaste

47
Q

What are other side effects of Zopiclone?

A

-headache
-somnolence
-dizziness
-dry mouth

48
Q

How is Zopiclone administered?

A

oral tabs

49
Q

What is the recommended starting dose for Zopiclone?

A

3.75mg at bedtime

50
Q

Zopiclone dose should not exceed ___ mg in old patients

A

5

51
Q

What should patients taking Zopiclone be advised about driving?

A

wait 12 hours after dosing before driving

52
Q

What is Lemborexant for?

A

insomnia

53
Q

How does Lemborexant act?

A

competitive antagonist at orexin receptors (OX1R and OX2R)

54
Q

What does the orexin neuropeptide system do?

A

promote wakefulness

55
Q

Lemborexant is contraindicated in patients with _____________

A

narcolepsy

56
Q

What are side effects of Lemborexant?

A

-somnolence
-headache
-nightmares
-depression
-suicidal ideation

57
Q

Does tolerance to Lemborexant develop?

A

no

58
Q

Lemborexant should not be taken with…

A

food or alcohol

59
Q

Lemborexant is contraindicated in…

A

pts with liver disease

60
Q

What are the side effects of melatonin?

A

-headache
-tachycardia
-pruritis
-nightmares

61
Q

What are the side effects of L-Tryptophan?

A

-GI upset
-dry mouth
-dizziness

62
Q

Chloral hydrate is fatal at doses more than ___ g

A

4

63
Q

What are the side effects of chloral hydrate?

A

-GI
-arrhythmia risk

64
Q

Chloral hydrate shouldn’t be taken with __________

A

alcohol

65
Q

What are negative takeaways of Barbiturates?

A

-tolerance and dependence
-abuse
-multiple DI’s
-respiratory depressants, fatal
-not used as often (Benzos used more)

66
Q

Thiopental is an __________-acting barbiturate

A

ultrashort

67
Q

Secobarbital is a ______ to ________-acting barbiturate

A

short to intermediate

68
Q

Phenobarbital is a _______-acting barbiturate

A

long

69
Q

How do barbiturates act?

A

bind to GABA receptor-chloride channel complex

70
Q

Barbiturates are lethal if mixed with _________

A

alcohol

71
Q

Barbiturates have a _______ onset and _______ duration

A

rapid; brief

72
Q

Barbiturates induce hepatic _________

A

enzymes

73
Q

What are barbiturates used for?

A

-seizure disorders
-**mainly induction of anesthesia
-insomnia

74
Q

What are the adverse effects of Barbiturates?

A

-respiratory depression
-suicide
-abuse

75
Q

What are the symptoms of acute barbiturate toxicity?

A

-respiratory depression
-coma
-pinpoint pupils

76
Q

How is barbiturate toxicity treated?

A

-removal of barbiturate (charcoal)
-maintain oxygen supply to brain

77
Q

How are barbiturates administered?

A

oral, IV, IM