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Advanced Pharmacology > Sedative-Hypnotics Agents > Flashcards

Sedative-Hypnotics Agents Flashcards

1
Q

What are the clinical uses of sedative-hypnotics?

A

-Treatment of insomnia (main)
-Anxiolytic
-Adjunctive sedation and anterograde amnesia before medical and surgical procedures
-Anticonvulsant (treatment of epilepsy and seizures states)
-Control of alcohol withdrawal

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2
Q

What are examples of sleep disorders?

A

-Primary insomnia (difficult initiating or maintaining sleep)
-Dysomnia (affects amount, quality, or timing of sleep)
-Primary hyperinsomnia
-Narcolepsy
-Circadian rhythm disorders (i.e jet lag)
-Parasomnias (related to abnormal/pathologic events)

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3
Q

What can be done for those with sleep disorders before initiating medication?

A

-Cognitive behavioral therapy
-Good sleep hygiene (regular sleep/wake schedule)
-Evaluate administration times of current medications

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4
Q

What can help someone have a regular sleep/wake schedule?

A

-Bedroom-> dark, quiet, comfortable
-Avoid daytime naps
-Exercise early in the day
-Avoid heavy meals, alcohol, stimulants (caffeine)
-Establish pre-bedtime ritual and/or regular schedule of activities

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5
Q

What are examples of pharmacological treatments for sleep disorders?

A

-FDA-approved “hypnotics”
-Benzodiazepines
-Zolpidem (Ambien)
-Zaleplon (Sonata)
-Eszopiclone (Lunesta)
-Ramelteon (Rozerem)

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6
Q

What are examples of Benzodiazepines that are prescribed for treatment of sleep disorders?

A

-Estazolam (ProSom)
-Quazepam (Doral)
-Temezepam (Restoril)
-Triazolam (Halcion)

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7
Q

Additional treatment considerations for sleep disorders:

A

-Screen for underlying physical psychiatric illness
-Treatment of underlying illnesses may help to alleviate sleep difficulties
-Ensure pain control is adequate for those with chronic pain

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8
Q

Zolpidem (Ambien) binds to ____ receptors, similar to benzodiazepines

A

GABA-A

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9
Q

Zolpidem (Ambien) is good for ___-__ treatment of insomnia, about 7-10 days

A

Short-term

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10
Q

Zolpidem (Ambien) has a rapid onset of action of ___ minues

A

30

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11
Q

The duration of action of Zolpidem (Ambien) is ___-___ hours

A

7-8

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12
Q

Zolpidem (Ambien) is a schedule ____ controlled substance

A

IV

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13
Q

Zolpidem (Ambien) is helpful for disturbances that affect ____ portions of sleep

A

All

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14
Q

Zolpidem (Ambien) has less ____ residual effects than other sleep medications

A

Daytime

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15
Q

Zolpidem (Ambien) has no ____ metabolites

A

Active

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16
Q

Ambien ___ mg is given before bedtime

A

10

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17
Q

Ambien ___ mg can be given to the elderly or those with hepatic dysfunction

A

5

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18
Q

Ambien ___ is a non-narcotic and non-benzodiazepine formulated to offer a new indication for sleep maintenance, in addition to sleep induction

A

CR

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19
Q

Ambien CR is a bi-layered tablet; the first layer dissolved quickly to ____ sleep and the second layer is released more gradually into the body to help provide more continuous sleep

A

Induce

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20
Q

____ is a sublingual dosage form of Zolpidem; it absorbs much faster than the oral form so it requires a smaller dose (dose is also smaller for women than men because men absorb it even faster)

A

Intermezzo

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21
Q

What is the dose of Intermezzo for women?

A

1.75 mg

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22
Q

What is the dose of Intermezzo for men?

A

3.5 mg

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23
Q

What are some common side effects of Zolpidem (Ambien)?

A

-Nausea
-Dizziness
-Headache
-Dry mouth

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24
Q

A ____ mg dose of Zolpidem (Ambien) can be used for the treatment of Major Depressive Disorder

A

10

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25
Q

The FDA has requested that all manufacturers of sedative-hypnotic drugs products strengthen their product labeling to include stronger language concerning potential ____ such as severe allergic reactions and complex sleep-related behaviors

A

Risks

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26
Q

Zaleplon (Sonata) binds to ____ receptors similar to benzodiazepines

A

GABA-A

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27
Q

Zaleplon (Sonata) is used for ___-___ treatment of insomnia (7-10 days)

A

Short-term

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28
Q

Zaleplon (Sonata) is a schedule ____ drug (controlled substance)

A

IV

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29
Q

Zaleplon (Sonata) has a rapid onset of action of ___-___ minutes

A

30-60

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30
Q

The duration of action of Zaleplon (Sonata) is less than ____ hours, which reduces the risk of a “hang-over” effect

A

4

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31
Q

Zaleplon (Sonata) is very similar to ____

A

Ambien

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32
Q

Zaleplon (Sonata) has no ____ metabolites

A

Active

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33
Q

A ___-___ mg dose of Zaleplon (Sonata) is given before bedtime

A

5-20

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34
Q

Sonata ___ mg should be given to elderly patients/those with hepatic dysfunction

A

5

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35
Q

Eszopiclone (Lunesta) interacts with GABA-RC near the ____ binding site

A

Benzodiazepine

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36
Q

Eszopiclone (Lunesta) is used for ___-___ treatment of insomnia (6 months)

A

Long-term

37
Q

Eszopiclone (Lunesta) has a rapid onset of action of ___-___ minutes

A

10-30

38
Q

The duration of action for Eszopiclone (Lunesta) is ____ hours

A

6

39
Q

Eszopiclone (Lunesta) is helpful for disturbances that affect ____ portions of sleep

A

All

40
Q

Eszopiclone (Lunesta) is a schedule ____ controlled substance

A

IV

41
Q

Eszopiclone (Lunesta) has very limited daytime ____ effects

A

Residual

42
Q

Eszopiclone (Lunesta) is similar to ____ and ____

A

Sonata and ambien

43
Q

Eszopiclone (Lunesta) is used for sleep ____ and ____

A

Inhibition and maintenance

44
Q

The initial dose of Lunesta is ___ mg before bedtime

A

2 mg

45
Q

Someone with chronic insomnia should get ____ mg of Lunesta before bedtime

A

3

46
Q

An elderly person should get ___ mg of Lunesta before bedtime, and it may be increased to ___ mg if needed for chronic insomnia

A

1; 2

47
Q

Common side effects of Lunesta include…

A

-Headache (15-21%)
-Unpleasant taste (8-34%)
-Dry mouth (3-7%)

48
Q

____ is an endogenous hormone made in the pineal gland in the evening in response to low light

A

Melatonin

49
Q

Melatonin has roles in…

A

-GI function
-Reproductive function
-Immune function

50
Q

Melatonin supplements may be taken for…

A

-Jet lag
-Shift workers
-Insomnia

51
Q

Over-the-counter melatonin supplements can be found in doses from ___-___ mg, most commonly 1.5-3 mg

A

1-20

52
Q

Melatonin is considered very safe, but it may have drug interactions with ____ and ____

A

-Warfarin (increases effects)
-Nifedipine->antihypertension (decrease effects)

53
Q

Melatonin used to be made from ground up ox pineal gland, but is usually ____ now

A

Synthetic

54
Q

Melatonin is not regulated by the ____

A

FDA

55
Q

Ramelteon (Rozerem) is a potent ____ ____ ____ _____

A

Selective melatonin receptor agonist

56
Q

Ramelteon (Rozerem) has a negligible affinity for ____ receptor

A

GABA-A

57
Q

Ramelteon (Rozerem) is indicated for the treatment of ____ characterized by difficult sleep onset

A

Insomnia

58
Q

Ramelteon (Rozeram) can be used for ___-___

A

Long-term

59
Q

Ramelteon (Rozerem) is similar to ____ and ____

A

Sonata, Ambien

60
Q

Rozeram ____ mg should be taken 30 minutes before bedtime

A

8

61
Q

The same 8 mg dose of Rozerem can be used for…

A

-Elderly
-Those with sleep apnea or COPD

62
Q

What are some common side effects of Ramelteon (Rozeram)?

A

-Somnolence
-Dizziness
-Fatigue

63
Q

With Rozeram, there are ____ next-day residual effects, rebound or withdrawal effects, abuse liability, and tolerance

A

Limited

64
Q

Suvorexant (Belsomra) is an ____ antagonist

A

Orexin

65
Q

Orexin regulates…

A

-Arousal
-Wakefulness
-Appetite

66
Q

Orexin ____ selectively blocks orexin receptors

A

Antagonists

67
Q

Suvorexant (Belsomra) is indicated for ____

A

Insomnia

68
Q

Suvorexant (Belsomra) should be administered ____ minutes before bedtime

A

30

69
Q

If taking Suvorexant (Belsomra), people should get at least ___ hours of sleep

A

7

70
Q

What are some adverse effects of Suvorexant (Belsomra)?

A

-Daytime sleepiness
-Sleepwalking
-Confusion

71
Q

Suvorexant (Belsomra) should not be administered to a patient with ____

A

Nacolepsy

72
Q

____ ____ is a non-barbiturate hypnotic used for inducing sleep and promoting pre-op sedation

A

Chloral hydrate

73
Q

Chloral hydrate may also be given as an adjunct for ____ and ____

A

Opiates or analgesics

74
Q

At therapeutic levels, chloral hydrate has little effect on…

A

-Respiration
-Blood pressure
-Reflexes

75
Q

Tolerance to chloral hydrate builds after about ___ ___ of therapy

A

2 weeks

76
Q

What are some adverse effects of chloral hydrate?

A

-Disorientation
-Paranoia
-Delirium
-Nightmares

77
Q

Sudden withdrawal of chloral hydrate may be severe enough to be ____

A

Fatal

78
Q

What are symptoms of withdrawal from chloral hydrate?

A

-CNS excitation
-Seizures
-Hallucinations

79
Q

What are three examples of barbiturates?

A

-Phenobarbitol (Bellatal)
-Secobarbital (Seconal)
-Pentobarbital (Nembutal)

80
Q

Barbiturates have mostly been replaced by ____

A

Benzodiazepines

81
Q

Barbiturates are effective for only short-term treatment of insomnia because…

A

-They are highly habit forming
-Tolerance builds over time

82
Q

There are many severe CNS, respiratory, and cardiovascular ___ ___ of barbiturates

A

Side effects

83
Q

Overdose of barbiturates cause ____ and ____ depression

A

CNS and respiratory

84
Q

We can use sedating antidepressants such as…

A

-Trazadone (50-150 mg)
-Doxepin (25-50 mg)
-Nortriptyline (10-50 mg)

85
Q

Chloral hydrate is not recommended for us in ____ due to safety concerns (it is easy to overdose, can cause arrhythmias)

A

Pediatrics

86
Q

There may be an antidepressant effect from Trazedone at doses of ___-___ mg

A

300-600

87
Q

Antihistamines can also have sedative effects; some examples include…

A

-Hydroxyzine pamoate (Vistaril)
-Diphenhydramine
-Doxylamine

88
Q

Antihistamines can sometimes cause a _____ effect in the morning; can also cause paradoxical effects in pediatrics and geriatrics

A

Hangover

Advanced Pharmacology (10 decks)

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