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Flashcards in Sleep Disorders Treatment Deck (36)
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1

Goals of therapy
3

1. Promote patient’s ability to fall asleep, maintain sleep, and awaken refreshed

2. Use med for as short a time as possible

3. Use minimal dose with least amount of side-effects

2

Benzodiazepines
7

1. Alprazolam (Xanax)
2. Estazolam (ProSom)
3. Flurazepam (Dalmane)
4. Lorazepam (Ativan)
5. Quazepam (Doral)
6. Temazepam (Restoril)
7. Triazolam (Halcion)

3

Benzodiazepines MOA?
3

MOA
1. Selectively acts on polysynaptic neuronal pathways throughout the CNS

2. Enhance the effects of GABA (an inhibitory neurotransmitter) in the CNS

3. Insomnia
--Facilitate the effects of GABA in the ascending reticular activating system

4

Benzos are divided into which three categories?

1. Short acting

2. Intermediate acting

3. Long acting

5

Which drugs are in each category:
1. Short acting 1

2. Intermediate acting 2

3. Long acting 2

1. Triazolam (Halcion)

2.
-Temazepam (Restoril)
-Estazolam (ProSom)

3.
-Flurazepam (Dalmane)
-Quazepam (Doral)

6

Benzo Adverse events
3

1. Drowsiness
2. Impaired motor function
3. Prolonged use
-Physical dependency

7

Benzos
1. Drug interactions? 2
2. Contraindications? 3

1. Interactions
-Caution with alcohol
-Low-dose contraceptives

2. Contraindications
-Acute narrow-angle glaucoma
-Preg X
-Lactation

8

Benzodiazepine Receptor Agonists (BRA)
1. Developed why?
2. Half life?
3. Has greater receptor specificity of the what?

1. to improve the safety profile of barbiturate-type compounds

2. Have short half-life
5 hours

3. GABAa BZ complex

9

Benzodiazepine Receptor Agonists (BRA): Drugs in this category?
3

Drugs
1. Eszopiclone (Lunesta)
2. Zolpidem (Ambien)
3. Zaleplon (Sonata)

10

Eszopiclone (Lunesta)
MOA?

Interacts with GABA receptors located near benzodiazepine receptors

11

BRAs: Dosage
1. Start with?
2. Can be started or increased to?

3. Elderly dosing?

1. Start at 2mg immediately before bed
2. Can be started or increased to 3mg to aid in sleep maintenance

3. Elderly
Start 1mg to help fall asleep
2mg for sleep maintenance

12

Eszopiclone (Lunesta)
1. Adverse affects? 3
2. Contraindications? 1
3. Preg cat?

1. Adverse events
-HA
-Dry mouth
-Dizziness

2. Contraindications
-Hypersensitivity

3. Preg C

13

Zolpidem (Ambien, Ambien CR)
1. MOA?
2. Dosage? 2

1. MOA
Modulates the GABA receptors to suppress neurons

2. Dosage
-5-10mg PO qhs
-Extended release
6.25-12.5mg PO qhs

14

Zolpidem
1. Adverse affects? 3
2. Contraindications? 1
3. Preg?

1. Adverse events
-Morning drowsiness
-Hangover
-HA

2. Contraindications
-Hypersensitivity

3. Preg C

15

Zaleplon (Sonata)
1. MOA?
2. Dosage?
-Start at?
-Range from?

1. MOA
Interacts with GABA-BZ omega 1 receptor

2. Dosage
Start: 10mg PO qhs
Range 5-20mg qhs

16

Zaleplon
1. Adverse affects? 3
2. Contraindications? 1
3. Preg?

1. Adverse Events
-Back or chest pain
-Migraine
-Constipation

2. Contraindications
-Hypersensitivity

3. Preg C

17

Most commonly used classes of OTC sleep-inducing agents?

Specific agent?

Antihistamines


Diphenhydramine (Benadryl)

18

Antihistamines:
Diphenhydramine (Benadryl)
1. MOA?
2. Dosage?
3. Adverse affects? 2

1. MOA
Unknown, but acts as a CNS depressant

2. Dosage
-25-50mg qhs

3. Adverse Events
-Excessive daytime drowsiness
-Impaired psychomotor function

19

Antidepressants
3

Newer agents? 2

1. Imipramine (Tofranil)
2. Amitriptyline hydrochloride (Elavil)
3. Nortriptyline (Pamelor)

Newer agents
1. Nefazodone hydrochloride (Serzone)
2. Venlafaxine (Effexor)

20

Doxepin (Silenor)
1. MOA?
2. Dosage?
3. Adverse effects? 4

1. MOA
Increases synaptic concentrations of serotonin and norepinephrine in the CNS

2. Dosage
-3-6mg within 30 min of bedtime

3. Adverse Events
-Drowsiness
-Dizziness
-Constipation
-Blurred vision

21

Doxepin (Silenor)
1. Contraindications? 2
2. BBW?
3. Preg cat?

1. Contraindications
-Glaucoma
-Urinary retention

2. Black Box Warning
-Suicide thinking/behavior

3. Preg C

22

Trazodone
MOA? 3

Dosage?

MOA
1. Inhibits reuptake of serotonin
2. Causes adrenoreceptor subsensitivity
3. Induces change in 5-HT presynaptic receptor adrenoreceptors

Dosage
50-100mg before bedtime

23

Trazodone
1. Adverse affects?
2. Contraindications? 2
3. Preg cat?
4. BBW?

1. Adverse Events
-Dizziness
-drowsiness

2. Contraindications
-Use of MAO inhibitors
-Patients receiving linezolid or IV methylene blue

3. Preg C

4. Black box warning
Suicidal thoughts

24

Amitriptyline (Elavil)
1. MOA?
2. Dosage?
3. Adverse affects? 3

MOA
1. Increases synaptic concentration of serotonin and/or norepinephrine in CNS

2. Dosage
25-50mg at bedtime

3. Adverse Events
-Sedation
-Dizziness
-HA

25

Amitriptyline
1. Contraindications? 2
2. Preg cat?
3. BBW?

1. Contraindications
-History of MI
-MAOIs

2. Preg C

3. Black box warning
Suicidal thoughts

26

Melatonin Agonist? 1

Ramelteon (Rozerem)

27

Ramelteon (Rozerem)
1. MOA?
2. Dosage?
3. Adverse effects? 3

4. Contraindications? 1
5. Preg cat?

1. MOA
Potent, selective agonist of melatonin receptors MT1 and MT2 within the suprachiasmic nucleus of the hypothalamus

2. Dosage
8mg daily within 30 min of bedtime

3. Adverse Events
-Somnolence
-HA
-Fatigue

4. Contraindications
Fluvoxamine (Luvox)

5. Preg C

28

Orexin Receptor Antagonist?

Suvorexant (Belsomra)

29

Suvorexant (Belsomra)
1. MOA?
2. Dosage?

1. MOA
Blocks binding of wake-promoting neuropeptides orexin A and orexin B to receptors OZ1R and OX2R

2. Dosage
10mg once daily within 30min of bedtime (max 20mg)

30

Suvorexant
1. Adverse effects? 3
2. Contraindications? 1
3. Preg cat?

1. Adverse Events
-Drowsiness
-HA
-Abnormal dreams

2. Contraindications
Narcolepsy

3. Preg C