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Psych Week 2 > ICL 8.6: Psychopharmacology of Sleep > Flashcards

ICL 8.6: Psychopharmacology of Sleep Flashcards

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1
Q

what is primary insomnia?

A
  1. too much arousal during the night and day
  2. not feeling sleepy despite not sleeping at night
  3. most of the medications are studies with primary insomnia –> most medications are tested in people who have primary insomnia, not secondary insomnia from a psychiatric disorder
  4. studies with depression and anxiety show better remission rates
  5. treat chronic insomnia chronically- long term treatment
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2
Q

which FDA drugs are used for insomnia?

A
  1. benzodiazepines (flurazepam, temazepam, triazolam)
  2. nonbenzodiazepine (zolpidem, eszopiclone, zaleplon) = 3Zs of sleep
  3. orexin-receptor antagonist (suvorexant)
  4. melatonin receptor agonists (ramelteon)
  5. antidepressants (doxepin)
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3
Q

what are H1 receptors?

A

G protein coupled- phosphatidyl inositol and transcription cFOS

responsible for wakefulness, alertness and precognition

blockage of H1 receptors causes drowsiness, sedation or sleep

this is why antihistaminergics are sedatives

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4
Q

what are H2 receptors?

A

action on gastric acid secretion

G protein coupled- phospholipase A and transcription CREB

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5
Q

what are H3 receptors?

A

presynaptic, auto receptors-inhibition of histamine release

no known drug-clinical developmental stage

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6
Q

what is the main nucleus that releases histamine?

A

tuberomammillary nucleus in the hypothalamus

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7
Q

which drug types of histamine H1 antagonists?

A
  1. popular over the counter drugs, diphenhydramine

2. tricyclic antidepressants

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8
Q

what are the side effects of TCAs?

A

anticholinergic side effects = blurred vision, constipation, memory, dry mouth, hangover

it causes histamine blockage –> difficult to separate antihistamine actions from antimuscarinic, and or alpha blockage

ex. amitriptyline (elavil)

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9
Q

what is doxepin?

A

doxepin at low doses is a potent H1 blocker (1-6 mg) –> if you up the doge to 150-300 mg it can have antidepressant action

so it causes rapid sleep induction with all-night sleep maintenance without hangover

no tolerance or withdrawal; no weight gain –> H1 blockers usually only cause weight gain if they’re also paired with something that blocks serotonin

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10
Q

which drugs are benzodiazepine receptor agonists?

A
  1. zolpidem
  2. zaleplon
  3. eszopiclone

3Zs of sleep

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11
Q

what are the benefits of using benzodiazepine receptor agonists?

A
  1. fewer hangover symptoms than benzodiazepines
  2. fewer problems with dependency, though still an issue
  3. do not show deleterious effects to the sleep cycle
  4. generally a longer half-life than benzodiazepines so help with sleep maintenance

one is approved for long-term use: Eszopiclone (but the others have open label studies)

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12
Q

which subunits of the GABA(A) receptor do benzodiazepines interact with?

A

BZDs interact at the α 1, 2, 3 and 5 subunit

zolpidem, zaleplon and eszopiclone are positive allosteric modulator (PAM) of GABAA receptor, at the alpha 1 subunit –> this selectivity may be why there is a lower risk of dependence

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13
Q

what is the function of the α1 subunit in the GABA(A) receptor?

A

α1 is critical for sedation

also linked to daytime sedation, anticonvulsant and amnesia

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14
Q

what is the function of the α2 and α3 subunit in the GABA(A) receptor?

A
  1. anxiolytic
  2. muscle relaxant
  3. alcohol potentiating
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15
Q

what is the function of the α5 subunit in the GABA(A) receptor?

A

hippocampus- cognition and other function

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16
Q

what are melatonergic hypnotics?

A

melatonin is neurotransmitter secreted by pineal glad that acts on SCN

they help restore circadian rhythm and help with phase delay

can be used in depressed patients, teenagers and people with jet lag

melatonergic hypnotics work at the M1, M2 and M3 receptors

17
Q

which drugs are melatonergic hypnotics?

A
  1. agomelatonin (antidepressant) (M1, M2 and 5HT2B, 5HT2C)
  2. melatonin (M1, M2, M3)
  3. Ramelton (M1/M2 agonist)
  4. tasimelteon (M1/M2)

they shift circadian rhythm and help with phase delay

18
Q

what’s the different between M1 and M2 melatonin receptors?

A

M1 mediated inhibition of neurons at SCN promotes sleep-lowering alerting signals of SCN

found in brain / pituitary / supra-chiasmatic nuclei of hypothalamus; Associated with circadian rhythm and reproductive functioning

M2: phase shifting and circadian rhythm-SCN

found in the retina

19
Q

what is the MOA of ramelteon?

A

rozerem selectively binds both MT1 and MT2 and is an agonist

helps with sleep initiation insomnia

20
Q

what is trazodone?

A

a serotonergic hypnotic but it’s used as a sleep medication!

to work as antidepressant high doses are needed to recruit 5HT2A and serotonin reuptake blocking properties

sedating action is due to H1 antihistamine and α antagonism

by giving it at night and lowering dose H1 antihistamine and α blocking and 5HT2A are retained.

21
Q

which antidepressants are commonly used as sedatives?

A
  1. amitriptyline (used with pts. who also have pain)
  2. trazodone (used with pts. who also have MDD or hypotension)
  3. doxepin/silenor (sleep maintenance insomnia)
  4. mirtazepine
22
Q

what is mirtazepine?

A

an antidepressant used for sleep that works on noradrenergic and serotonergic receptor

smaller doses used for depression

significant weight gain**

23
Q

what are orexin antagonists?

A

orexin neurons are located on lateral hypothalamus, perifornical area and posterior hypothalamus

orexin A and orexin B keep you awake –> orexin 2 activates TMN histaminergic neurons

lack of orexin causes narcolepsy!

24
Q

what are DORAs?

A

DORA = dual orexin receptor antagonists

DORAs are orexin receptor antagonists at orexin 1 and 2 receptors

can also be used for drug abuse and weight loss

helps with initiation and maintenance of sleep without the benzodiazepines side effects; but in theory it could cause narcolepsy since you’re blocking orexin but it doesn’t actually happen in practice oddly enough

ex. Almorexant, Suvorexant (Belsomra)

25
Q

what are SORAs?

A

SORA 1 is an orexin 1 receptor antagonist –> SORA 1 not robust for treating insomnia

SORA 2 is an orexin 2 receptor antagonist

26
Q

what is suvorexant?

A

belsomra is a DORA = dual orexin receptor antagonist

helps with sleep onset and sleep maintenance

take within 30 minutes of going to bed, time to peak about 2 hours; eliminated after 12 hours –> metabolized by 3A4; no dose adjustment needed for mild to moderate hepatic or renal dysfunction

contraindicated in narcolepsy

27
Q

what is prazosin?

A

Prazosin is an alpha-1 adrenergic receptor antagonist

it’s recommended as a first-line therapy for nighttime PTSD symptoms (nightmares or sleep disturbances)

nightmares can interfere with PTSD recovery, by disrupting sleep-dependent processing of emotional experiences and causing repeated re-sensitization to trauma cues and increasing neuro-cognitive deficits

also used in opiod use disorders!

28
Q

how does alcohol effect sleep?

A

Helps you fall asleep faster, but does NOT improve quality of sleep; will wake you up early!

1 drink can affect sleep for up to 3 nights

it briefly increases alpha and delta sleep; it interrupts REM sleep and circadian rhythm

29
Q

what are the principles you need to follow when prescribing medications for insomnia?

A
  1. use lowest effective dose
  2. use agents with short or intermediate half-lives
  3. use intermittent dosing
  4. use no more than for 3-4 weeks
  5. discontinue medication gradually
  6. be alert for rebound insomnia
  7. be alert for drug-drug interactions
  8. caution patients about interaction with alcohol
  9. review daytime sleepiness** especially with heavy machinery
  10. consider consultation with a sleep specialist before starting continuous, long-term therapy with hypnotic medication
  11. start with a GABA agonist for acute or short-term insomnia

Psych Week 2 (18 decks)

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