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Neuro IV > Sleep Physiology and pharmacotherapy > Flashcards

Sleep Physiology and pharmacotherapy Flashcards

1
Q

Benzos and non-benzo receptor agonists’ mechanism of action

A

facilitate GABA at GABAa receptor-chloride channel complex –> membrane hyperpolarization

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2
Q

Triazolam pharmacokinetics

A

1.5-5h half-life, less daytime sedation (hangover). Rapid elimination –> rebound insomnia the next day. rapid absorption

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3
Q

Temazepam pharmacokinetics

A

9-13h half-life. slow absorption. peak effect at 2-3h

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4
Q

Flurazepam pharmacokinetics

A

75-90h half-life. little tolerance. Hepatic clearance (can accumulate in elderly –> daytime sedation, hangover, OD)

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5
Q

Zolpidem and zaleplon pharmacokinetics

A

6-8h duration. rapid oral absorption

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6
Q

Eszopiclone (Lunesta) pharmacokinetics

A

longer half-life than zolpidem and zapelon

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7
Q

First line in tx of insomnia

A

Z drugs. Little effect on sleep stages III and IV

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8
Q

Zolpidem role in insomnia tx

A

reduces sleep latency and nocturnal awakenings –> increased total sleep time and efficiency

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9
Q

Zaleplon role in insomnia tx

A

decreases time to sleep onset, no effect on awakening or total sleep time. Used for patients who fall asleep without sleep aid, but wake up in middle of night.

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10
Q

Eszopiclone role in insomnia tx

A

safest for long-term use

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11
Q

Benzo role in insomnia tx

A

declining use. cheaper than Z drugs. short-term tx of insomnia

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12
Q

trazodone side effects

A

oversedation and orthostasis (alpha adrenergic block)

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13
Q

TCAD side effects

A

antimuscarinic and antiadrenergic activity

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14
Q

Ramelteon

A

melatonin agonist –> induce sleepiness, regulates circadian rhythms

ADRs: dizziness, somnolence, fatigue, nausea

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15
Q

Antihistamines

A

H1 and muscarinic cholinergic antagonist

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16
Q

Black box warning for benzos and Z drugs

A

strange sleep-related behavior, anaphylaxis, facial swelling

17
Q

Benzo side effects

A

daytime sedation and performance impairment, anterograde amnesia, rebound insomnia, psych and physical dependence

18
Q

Zolpidem side effects

A

dorwsiness, amnesia, dizziness, headache, GI complaints

19
Q

Zaleplon side effects

A

dizziness, headache, sonolence

20
Q

Eszopiclone side effects

A

similar to zolpidem. increased incidence of psychomotor impairment with higher doses

21
Q

Sleep periods at birth

A

shorter. Consolidate with age

22
Q

Non-REM sleep

A

stage 1-3. high amplitude, slow brain waves. increased arousal threshold, decreased muscle activity, slow rolling eye movements, decreased heart rate, decreased respirations and metabolism

23
Q

REM sleep

A

every 90 minutes in adults. EEG similar to awake. Higher arousal threshold than slow-wave sleep. “Active brain in paralyzed body”. 85% of dreams

24
Q

sleep/wake switch

A

hypothalamus

25
Q

circadian clock. modulates core temp, alertness, cortisol and melatonin secretion

A

suprachiasmatic nucleus

26
Q

ascending cortical activation and REM/SWS switch

A

brainstem

27
Q

spindles, slow wave sleep

A

thalamus

28
Q

inhibit arousal systems during NREM sleep

A

neurons of ventrolateral preoptic area (GABA and galanin)

29
Q

Drive REM sleep

A

cholinergic pedunculopontine and laterodorsal tegmental (PPT/LDT) neurons. Inhibited by catecholamines during wake and NREM sleep

30
Q

Neurotransmitters active during wake

A

Ach in LDT/PPT, serotonin (raphe nucleus), NE (locus ceruleus), histamine (Tubomammillary nucleus), dopamine (VTA/SNc), adenosine (basal forebrain), hypocretin (lateral hypothalamus)

31
Q

Neurotransmitters active during NREM

A

GABA, galanine (ventrolateral preoptic nucleus), melatonin (pineal gland, SCN, hypothalamus)

32
Q

Neurotransmitters active during REM

A

Ach (LDT/PPT), DA (VTA/SNc)

33
Q

Homeostatic S drive

A

the longer we are awake, the sleepier we get. Mediated by adenosine. blocked by caffeine

34
Q

Circadian (C) alerting system

A

waxing/waning of sleepiness. resides in SCN, linked to core body temp

35
Q

Best sleep

A

descending curve of core body temp

36
Q

What happens when you stay up 72h?

A

sleepiness waxes and wanes due to C system

37
Q

Melatonin activity

A

Light –> SCN –> inhibits pineal gland production of melatonin

Dark –> reduced SCN firing –> disinhibition of pineal gland –> melatonin production

38
Q

Evolution of insomnia

A

3 Ps: Predisposed person (worrier), Precipitant (stress), Perpetuating factors (sleep worry)

39
Q

Two categories of insomnia

A

Learned and co-morbid

Neuro IV (21 decks)

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