Exam 2: Hypnotics Flashcards

1
Q

BZD MOA

A

bind to GABAa receptors, allosteric site

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2
Q

BZD AE overview (4)

A
  1. daytime sedation
  2. psychomotor impairment
  3. cognitive deficits
  4. anterograde amnesia
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3
Q

BZD cautions (10)

A
  1. older adults
  2. tolerance and dependence within 4-6 weeks of use
  3. withdrawal
  4. rebound insomnia
  5. AVOID IN HX OF DRUG USE
  6. AVOID W/ ALCOHOL USE OR OPIOD USE
  7. BOXED WARNING W OPIODS
  8. AVOID IN SLEEP APNEA
  9. AVOID IN PREGNANCY
  10. can worsen depression, PTSD, suicidal ideation
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4
Q

BZD drugs (2)

A
  1. tamezepam
    - 7.5-50mg dose
    - sleep onset/maintenance
    - slow onset
  2. Triazolam
    - 0.125-0.25 mg
    - rapid onset
    - sleep onset use
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5
Q

BZE Adverse Effects (7)

A
  1. CNS depression
    - sedation
    - respiratory depression
  2. psychomotor impairment
    - ataxia
    - falls in elderly
  3. Confusion
  4. Agression
  5. Disinhibition
  6. Amnesia
    - anterograde
    - retrograde
  7. Dependence and abuse
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6
Q

Non-BZD Receptor Agonist

Z-Drugs

MOA

A

Bind to GABAa receptor, allosteric site

-more selective subunits

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7
Q

Z-drugs

Adverse effects (4)

A
  1. Daytime sedation
  2. cognitive deficits
  3. amnesia
  4. complex sleep behaviors
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8
Q

Z-drugs

Cautions (6)

A
  1. older adults
  2. tolerance and rebound insomnia < BZDs
  3. rx for significant withdrawal
  4. AVOID concomitant CNS depressants, including alcohol and opioids
  5. can worsen depression, suicidal ideation
  6. BOXED WARNING:
    April 2019
    -serious injuries or death in 66 patients, caused by parasomnias
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9
Q

Z-Drug pearls (1)

A

Rapid onset; food delays by 1-2 hours

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10
Q

Melatonin Agonist

MOA (1)

A
  1. melatonin analogue; binds melatonin 1 & 2 receptors (hypothalamus)
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11
Q

Melatonin Agonist Sleep Benefits (3)

A
  1. Regulates circadian rhythms (phase shifting)
  2. direct effect on decreasing sleep latency
  3. no effect on sleep maintenance
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12
Q

Melatonin Agonist AE (4)

A
  1. HA
  2. Dizziness
  3. daytime somnolence
  4. GI upset
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13
Q

Melatonin Agonist Caution (2)

A
  1. may increase prolactin level in men & women

2. decreased testosterone levels in men

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14
Q

Melatonin Agonist Pearls (5)

A
  1. SAFE in sleep apnea, COPD, hx of substance use disorder
  2. may require 3 weeks of nightly use for maximum effect on sleep onset
  3. high-fat meal decreased effectiveness
  4. affected by CYP1A2 and CYP3A4 inhibition/induction
  5. brand-only $$$
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15
Q

Orexin Agonist MOA

A

Antagonism or orexin receptor 1 and 2 in the hypothalamus

-when activated they promote waking

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16
Q

Orexin Agonist Adverse Effects (7)

A
  1. daytime solomnce
  2. sleep paralysis
  3. cataplexy
  4. abnormal thinking
  5. hallucination
  6. CNS depression
  7. sleep-related activities
17
Q

Cautions Orexin Agonist (4)

A
  1. potential to worse depression/suicidal ideation
  2. CONTRAINDICATED IN NARCOLEPSY
  3. Potential for abuse,
    AVOID USE IN ALCOHOL
  4. AVOID USE WITH STRONG CYP3A 4 inhibitors
18
Q

Orexin Agonist Pearls

A
  1. onset delayed with food
  2. plan for 7 hours of sleep time
  3. brand-only $$$
19
Q

Antidepressants MOA (3)

A
  1. Histamine H antagonism, “selective” at low doses
  2. serotonin 5HT2c antagonism
  3. Alpha-1 blockade (trazodone)
20
Q

Antidepressants benefits/effect on sleep (3)

A
  1. primarily sleep maintenance
  2. not dependence, minimal tolerance
  3. not well studied in patients without depression
21
Q

Antidepressants cautions (4)

A
  1. side effects vary widely between medications
  2. daytime somnolence/sedation is a possible side effect of each of the agents commonly used for sleep
  3. sedative effect within 1-2 weeks
  4. insomnia doses generally not effective for treatment of depression
22
Q

Antihistamines MOA

A
  1. histamine H1 antagonism
23
Q

Antihistamines benefits

A

may be effective for transient insomnia; latency and maintenance

24
Q

Cautions Antihistamines (4)

A
  1. Tolerance to hypnotic effect; after 10 days
  2. increased dose does not equal increased response
  3. anticholinergic; CNS depression, next-day residual effects
  4. AVOID: narrow-angle glaucoma, acute asthma, urinary obstruction
25
Q

Pearls Antihistamines (2)

A
  1. in a variety OTC products

2. some combo products contain antihistamines

26
Q

Melatonin OTC MOA

A
  1. M1, M2, M3 receptors
27
Q

Melatonin OTC Side effects

A

minimal, some daytime somnolence

28
Q

Valerian OTC MOA

A

increases GABA

29
Q

Valerican OTC SE

A

minimal, some diarrhea

30
Q

Kava/chamomile/wuling MOA

A

*possible effects on GABA, 5HT, or glutamate

31
Q

Kava/chamomile/wuline AE

A

hapatotoxicity (KAVA)

-rest similar to placebo

32
Q

Gabapentin Role/ Risks

A
  • not recommended
    1. role: insomnia with consistent alcohol use disorder
  1. Rx: Dizziness, N/V
    - mortality rx with opioids
    - Rx dependency and abuse
33
Q

Atypical Antipsychotics

role/rx

A
  • NOT recommended
    1. quetiapine, olanzapine
    2. Role: insomnia with schizophrenia, Bipolar, or depressive d/o
  1. rx:
    - metabolic effects
    - movement d/o
    - anticholingeric
    - QTc prolongation
    - orthostatic hypotension
    - increased mortality in elderly patients with dementia-related psychosis