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NEUROLOGY > drugs for insomnia > Flashcards

drugs for insomnia Flashcards

1
Q

what are the 2 main goals of treating insomnia?

A

improvement in nighttime and daytime symptoms

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2
Q

most drugs used to treat insomnia are considered __________ __________

A

off label

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3
Q

which drugs are approved for insomnia?

A

benzodiabepines, BNZ receptors agonists (zolipidem), Melatnonin receptor agonists (e.g. remelteon)

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4
Q

how do each of the drug classes used to treat insomnia affect the response pattern of the GABA receptors?

A

the different drug classes modifies the response pattern of the GABA receptor to endogenous ligand

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5
Q

at very high doses, which drug class is capable of activating and opening the GABA-A channel?

A

barbituates

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6
Q

at normal clinical doses, do any of the drug classes used to treat insomnia cause opening of the endogenous GABA channel?

A

no

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7
Q

how are benzodiazepines or benzodiazepine receptor agonists different in respect to endogenous GABA action?

A

the benzodiazepines or benzodiazepine receptor agonist produces only an allosteric modification, leading to leftward shift in the dose response curve to endogenous GABA action (they have ceiling effect)

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8
Q

benzodiazepines are only lethal when consumed with quantities of what?

A

alcohol

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9
Q

what are some of the adverse effects of BNZs the morning after?

A

sedation, cognitive impairment, rebound insomnia

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10
Q

what are some of the adverse effects of BNZ withdrawal?

A

anxiety, irritability, restlessness, OSA, severe ventilatory impairment, tapered withdrawal

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11
Q

what are 2 attributes that you would like to have in a drug used to treat insomnia?

A
  1. drug with a rapid onset time

2. drug that has durability of action that pts don’t wake up in the middle of the night

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12
Q

Benzodiazepine receptor agonists seem capable only of sedative and amnesic actions via ________ receptor complex at normal clinical doses

A

BZ-1

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13
Q

Cumulative and residual effects like excessive drowsiness are less of a problem with benzodiazepines like what 3 drugs?

A

estazolam, oxazepam, lorazepam, have short half-lives and are metabolized directly to inactive glucuronides

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14
Q

what pregnancy category are benzodiazepines?

A

category X

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15
Q

what are some of the contraindications for the benzodiazepines?

A

COPD, closed angle glaucoma, CNS drugs, driving, and depression

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16
Q

which BNZ is rapidly inactivated?

A

triazolam

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17
Q

which 2 BNZs have metabolites that accumulate?

A

Flurazepam, Quazepam

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18
Q

which BNZ has CYP2B6 > 3A4 interactions?

A

quazepam

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19
Q

which BNZ doesn’t have CYP interactions bc it is conjugated metabolically?

A

temazepam

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20
Q

3 of the BNZs have interactions with CYP3A4, what are they?

A

estazolam, flurazepam, triazolam

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21
Q

the benzodiazepine receptor agonists are considered what pregnancy category?

A

Pregnancy Category C

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22
Q

which benzodiazepine receptor agonist has interactions with aldehyde dehydrogenase?

A

zaleplon

23
Q

name the 3 Benzodiazepine receptor agonists?

A

Zolpidem
Zaleplon
Eszopiclone

24
Q

what is the only drug approved for middle of the night awakening?

A

zolpidem (administered solely as a short acting product)

25
Q

Which Benzodiazepine receptor agonist is available in both sublingual and oral spray preps for increased onset of action?

A

zolpidem

26
Q

what is the most widely prescribed hypnotic in the US?

A

zolpidem

27
Q

why can’t you chew the oral benzodiazepine receptor agonists?

A

the action is reliant on the tablet integrity

28
Q

which drug has new dosing recommendations for women due to diminished elimination rate compared to women?

A

zolpidem (dose reduced)

29
Q

which population of pts are more likely to experience residual effects of zolpidem the next day?

A

women, b/c women eliminate the drug more slowly than men do

30
Q

how are the benzodiazepine receptor agonists metabolized?

A

hepatically with various CYP interactions

31
Q

what is the mechanisms of action of flumazenil?

A

BNZ & benzodiazepine receptor agonist— antagonist, given IV

32
Q

what is the result of melatonin binding to MT1 receptors?

A

attenuates SCN activity & induces sleep

33
Q

what is the result of melatonin binding to MT2 receptors?

A

maintains circadian rhythm

34
Q

which melatonin receptor is not involved in sleep regulation?

A

MT3

35
Q

what type of receptors are MT1 and MT2, and where can they be found?

A

G -protein coupled receptors found in the CNS

36
Q

MOA of Ramelteon

A

melatonin receptor agonist

37
Q

what are the benefits of ramelteon?

A

not associated with residual effects, no abuse potential or respiratory depression

38
Q

how is ramelteon metabolized?

A

CYP1A2> 2C9, 3A4

39
Q

what are some of the adverse effects of ramelteon?

A

headache, somnolence, nausea, insomnia, naso-pharyngitis, URTI w/ long term use

40
Q

what is the only FDA approved antidepressant used to treat insomnia?

A

doxepin

41
Q

name the drug: antidepressant with primarily an anti-histaminergic action at low doses

A

doxepin

42
Q

what is an adverse effect of using doxepin to treat insomnia?

A

has residual effects the next day

43
Q

which antidepressant used to treat insomnia has significant alpha-2 antagonism, reinforcing NE, 5-HT release?

A

mirtazapine

44
Q

what are 2 antidepresants used to treat insomnia that have a strong effect of sedation but very little effect on muscarinic block, NE, reuptake block, or 5-HT reuptake block?

A

mirtazapine & trazodone

45
Q

antidepressants used to treat insomnia have a BBW for what?

A

suicidal ideation

46
Q

name the 3 antidepressants used to treat insomnia?

A

doxepin
mirtazapine
trazodone

47
Q

you should be cautious of prescribing antidepressants to pts with a history of what?

A

psychotic disorders

48
Q

what are some of the antimuscarinic adverse effects of the first generation antihistamines?

A

xerostomia, blurred vision, urinary retention, increased intraocular pressure

49
Q

what is a major downside to using 1st gen. antihistamines for insomnia?

A

rapid tolerance may develop to sedative action

50
Q

what are the two 1st. gen. antihistamines used for insomnia?

A

diphenhydramine & doxylamine

51
Q

why do you try to avoid using 1st gen. antihistamines in the elderly?

A

because of excessive sedation, urinary retention (anticholinergic effect) and falls producing injury

note also caution w/ Narrow-angle glaucoma

52
Q

name some drugs that can produce insomnia?

A

TCAs, MAOis, SSRIs, Venlafaxine, Buproprion, Levodopa, Felbamate, beta-blockers, decongestants, antibiotics, asthma meds, stimulants

53
Q

what is the most commonly used alternative medicine for insomnia?

A

chamomile

NEUROLOGY (9 decks)

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