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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
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
Risks
26
Zaleplon (Sonata) binds to ____ receptors similar to benzodiazepines
GABA-A
27
Zaleplon (Sonata) is used for ___-___ treatment of insomnia (7-10 days)
Short-term
28
Zaleplon (Sonata) is a schedule ____ drug (controlled substance)
IV
29
Zaleplon (Sonata) has a rapid onset of action of ___-___ minutes
30-60
30
The duration of action of Zaleplon (Sonata) is less than ____ hours, which reduces the risk of a "hang-over" effect
4
31
Zaleplon (Sonata) is very similar to ____
Ambien
32
Zaleplon (Sonata) has no ____ metabolites
Active
33
A ___-___ mg dose of Zaleplon (Sonata) is given before bedtime
5-20
34
Sonata ___ mg should be given to elderly patients/those with hepatic dysfunction
5
35
Eszopiclone (Lunesta) interacts with GABA-RC near the ____ binding site
Benzodiazepine
36
Eszopiclone (Lunesta) is used for ___-___ treatment of insomnia (6 months)
Long-term
37
Eszopiclone (Lunesta) has a rapid onset of action of ___-___ minutes
10-30
38
The duration of action for Eszopiclone (Lunesta) is ____ hours
6
39
Eszopiclone (Lunesta) is helpful for disturbances that affect ____ portions of sleep
All
40
Eszopiclone (Lunesta) is a schedule ____ controlled substance
IV
41
Eszopiclone (Lunesta) has very limited daytime ____ effects
Residual
42
Eszopiclone (Lunesta) is similar to ____ and ____
Sonata and ambien
43
Eszopiclone (Lunesta) is used for sleep ____ and ____
Inhibition and maintenance
44
The initial dose of Lunesta is ___ mg before bedtime
2 mg
45
Someone with chronic insomnia should get ____ mg of Lunesta before bedtime
3
46
An elderly person should get ___ mg of Lunesta before bedtime, and it may be increased to ___ mg if needed for chronic insomnia
1; 2
47
Common side effects of Lunesta include...
-Headache (15-21%) -Unpleasant taste (8-34%) -Dry mouth (3-7%)
48
____ is an endogenous hormone made in the pineal gland in the evening in response to low light
Melatonin
49
Melatonin has roles in...
-GI function -Reproductive function -Immune function
50
Melatonin supplements may be taken for...
-Jet lag -Shift workers -Insomnia
51
Over-the-counter melatonin supplements can be found in doses from ___-___ mg, most commonly 1.5-3 mg
1-20
52
Melatonin is considered very safe, but it may have drug interactions with ____ and ____
-Warfarin (increases effects) -Nifedipine->antihypertension (decrease effects)
53
Melatonin used to be made from ground up ox pineal gland, but is usually ____ now
Synthetic
54
Melatonin is not regulated by the ____
FDA
55
Ramelteon (Rozerem) is a potent ____ ____ ____ _____
Selective melatonin receptor agonist
56
Ramelteon (Rozerem) has a negligible affinity for ____ receptor
GABA-A
57
Ramelteon (Rozerem) is indicated for the treatment of ____ characterized by difficult sleep onset
Insomnia
58
Ramelteon (Rozeram) can be used for ___-___
Long-term
59
Ramelteon (Rozerem) is similar to ____ and ____
Sonata, Ambien
60
Rozeram ____ mg should be taken 30 minutes before bedtime
8
61
The same 8 mg dose of Rozerem can be used for...
-Elderly -Those with sleep apnea or COPD
62
What are some common side effects of Ramelteon (Rozeram)?
-Somnolence -Dizziness -Fatigue
63
With Rozeram, there are ____ next-day residual effects, rebound or withdrawal effects, abuse liability, and tolerance
Limited
64
Suvorexant (Belsomra) is an ____ antagonist
Orexin
65
Orexin regulates...
-Arousal -Wakefulness -Appetite
66
Orexin ____ selectively blocks orexin receptors
Antagonists
67
Suvorexant (Belsomra) is indicated for ____
Insomnia
68
Suvorexant (Belsomra) should be administered ____ minutes before bedtime
30
69
If taking Suvorexant (Belsomra), people should get at least ___ hours of sleep
7
70
What are some adverse effects of Suvorexant (Belsomra)?
-Daytime sleepiness -Sleepwalking -Confusion
71
Suvorexant (Belsomra) should not be administered to a patient with ____
Nacolepsy
72
____ ____ is a non-barbiturate hypnotic used for inducing sleep and promoting pre-op sedation
Chloral hydrate
73
Chloral hydrate may also be given as an adjunct for ____ and ____
Opiates or analgesics
74
At therapeutic levels, chloral hydrate has little effect on...
-Respiration -Blood pressure -Reflexes
75
Tolerance to chloral hydrate builds after about ___ ___ of therapy
2 weeks
76
What are some adverse effects of chloral hydrate?
-Disorientation -Paranoia -Delirium -Nightmares
77
Sudden withdrawal of chloral hydrate may be severe enough to be ____
Fatal
78
What are symptoms of withdrawal from chloral hydrate?
-CNS excitation -Seizures -Hallucinations
79
What are three examples of barbiturates?
-Phenobarbitol (Bellatal) -Secobarbital (Seconal) -Pentobarbital (Nembutal)
80
Barbiturates have mostly been replaced by ____
Benzodiazepines
81
Barbiturates are effective for only short-term treatment of insomnia because...
-They are highly habit forming -Tolerance builds over time
82
There are many severe CNS, respiratory, and cardiovascular ___ ___ of barbiturates
Side effects
83
Overdose of barbiturates cause ____ and ____ depression
CNS and respiratory
84
We can use sedating antidepressants such as...
-Trazadone (50-150 mg) -Doxepin (25-50 mg) -Nortriptyline (10-50 mg)
85
Chloral hydrate is not recommended for us in ____ due to safety concerns (it is easy to overdose, can cause arrhythmias)
Pediatrics
86
There may be an antidepressant effect from Trazedone at doses of ___-___ mg
300-600
87
Antihistamines can also have sedative effects; some examples include...
-Hydroxyzine pamoate (Vistaril) -Diphenhydramine -Doxylamine
88
Antihistamines can sometimes cause a _____ effect in the morning; can also cause paradoxical effects in pediatrics and geriatrics
Hangover

Advanced Pharmacology (10 decks)

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