28b - Drugs for Insomnia Flashcards

1
Q

MOA of estazolam

A

benzodiazepine

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2
Q

MOA of flurazepam

A

benzodiazepine

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3
Q

MOA of quazepam

A

benzodiazepine

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4
Q

MOA of temazepam

A

benzodiazepine

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5
Q

MOA of triazolam

A

benzodiazepine

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6
Q

MOA of doxepin

A

antidepressant

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7
Q

MOA of mirtazapine

A

antidepressant

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8
Q

MOA of trazodone

A

antidepressant

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9
Q

MOA of zolpidem

A

benzodizepine receptor agonist

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10
Q

MOA of zaleplon

A

benzodizepine receptor agonist

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11
Q

MOA of eszopiclone

A

benzodizepine receptor agonist

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12
Q

MOA of ramelteon

A

melatonin receptor agonist

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13
Q

MOA of diphenhydramine

A

1st gen antihistamine

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14
Q

MOA of doxylamine

A

1st gen antihistamine

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15
Q

What are the 2 arousal pathways?

A
  1. Ach cells from upper pons, PPT and LDT activate thalamus
  2. activation of cerebral cortex so it can receive thalamic inputs.
    - histamine from TMN
    - dopamine from A10 cell group
    - serotonin from dorsal and median raphe
    - noradrenaline from locus coeruleus
    - orexin and melanin-concentrating hormone from lateral hypothalamus (LHA)
    - GABA or Ach from Basal forebrain
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16
Q

What drugs are approved for insomnia?

A

benzodiazepines, benzo receptor agonists (BRA), and melatonin receptor agonists

17
Q

Which insomnia drug does NOT work on GABA receptors?

A

Ramelteon

18
Q

What is only insomnia drug that can open GABA-A channels completely by themselves?

A

barbiturates at high doses

19
Q

What are the subgroups of BNZ receptors and what do they each do?

A
BZ-1 = sedation/amnesia
BZ-2 = anioxlysis
BZ-3 = myorelaxation and anticonvulsant
20
Q

Which BNZ subgroups do benzodiazepines act on?

A

all three, BZ1-3

21
Q

which BNZ subgroups do BRAs act on?

A

only on BZ1 at normal doses

22
Q

What is the longest acting BNZ?

A

diazepam

23
Q

What is the shortest acting BNZ?

A

midazolam

24
Q

Which BNZ has CYP 2B6 activity?

A

Quazepam

25
Q

Which BNZ has no CYP interactions?

A

Temazepam

26
Q

Which BNZ is the only one approved for middle of the night awakening and why?

A

Zolpidem because of its short period of activity

27
Q

What do you give for BNZ overdose?

A

flumazenil, and BNZ antagonist and BzRA antagonist.

can reverse overdose, cause withdrawals

28
Q

ADE of flumazenil?

A

withdrawals, seizures, does NOT work on barbiturates, opiates or TCAs

29
Q

What are the subgroups of melatonin receptors and what do they do?

A
MT1 = SCN activity to induce sleep
MT2 = maintains circadian rhythm
MT3 = NOT involved in sleep
30
Q

ADE of ramelteon?

A

not many. No abuse or respiratory depression

31
Q

What is the only antidepressant approved for insomnia?

A

doxepin

32
Q

Why do antidepressants work for insomnia?

A

seem to work thorugh H1 antagonism in tuberomamillary nucleus

33
Q

ADE of antidepressants for insomnia?

A

suicidal ideation

CYP interactions

34
Q

What are the 1st gen antihistamines? and how do they work?

A

diphenhydramine and doxylamine.

cross BBB to inhibit H1 and some Ach.

35
Q

ADE of 1st gen antihistamines?

A

xerostomia, blurred vision, urine reten, high intraoc press, rapid tolerance
caution in elderly and narrow-angle gluacoma

36
Q

Patient experiences anxiety, irritability, restlessness, sleep apnea, respiratory depression. What is happening?

A

benzodiazepene withdrawals

37
Q

ADE of BNZs?

A

sedation, cognitive impairment, rebound insomnia