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neuro2 > drugs for insomnia > Flashcards

drugs for insomnia Flashcards

1
Q

flumazenil moa

A

BNZ and BzRA antagonist; reverses sedation or BNZ overdose, resulting in abrupt awakening

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2
Q

flumazenil side effects

A

dysphoria, agitation, seizures, and withdrawal in chronic BNZ patients

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3
Q

orexin neurons

A

located in the posterior-lateral hypothalamus; mediate the transition between sleep and awake states

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4
Q

benzodiazepines (drugs)

A

estazolam, flurazepam, quazepam, temazepam, triazolam

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5
Q

benzodiazepine receptor agonists (drugs)

A

zolpidem, zaleplon, eszopiclone

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6
Q

antidepressants for insomnia

A

doxepin, mirtazepine, trazodone

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7
Q

1st gen. antihistamines for insomnia

A

diphenhydramine, doxylamine

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8
Q

GABA receptor

A

chloride channel

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9
Q

benzodiazepine and benzodiazepine receptor agonist moa

A

allosteric modification of the GABA receptor, leading to a leftward shift in the dose-response curve

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10
Q

benzodiazepine and benzodiazepine receptor agonist adverse effects

A

sedation, cognitive impairment, rebound insomnia, withdrawal (anxiety, irritability, restlessness, obstructive sleep apnea, severe ventilatory impairment)

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11
Q

benzodiazepine receptor agonist target

A

BZ-1 receptor complex (at normal clinical doses)

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12
Q

benzo that does not cause excessive drowsiness

A

estazolam (due to short half-lives and direct metabolism to inactive glucuronides)

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13
Q

benzo without CYP interactions

A

temazepam

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14
Q

benzodiazepine contraindications

A

hepatic disease, depression, driving, CNS drugs, COPD, closed angle glaucoma, pregnancy (category X)

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15
Q

benzos with metabolic accumulation

A

flurazepam, quazepam

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16
Q

BzRAs contraindications

A

hepatic disease, COPD, depression, driving, CNS drugs, pregnancy category C

17
Q

BzRA with ethnic variability

A

zaleplon (asians)

18
Q

approved for middle of the night wakening

A

low dose sublingual zolpidem

19
Q

flumazenil pharm

A

given IV; short duration compared to some BNZs so redosing may be necessary

20
Q

MT1 receptor

A

melatonin binding attenuates suprachiasmatic nucleus activity and induces sleep

21
Q

MT2 receptor

A

binding maintains circadian rhythm

22
Q

ramelteon moa

A

melatonin receptor agonist

23
Q

ramelteon metabolism

A

hepatic: CYP 1A2> 2C9, 3A4; no accumulation with repeat dosing

24
Q

ramelteon adverse effects

A

headache, somnolence, nausea, insomnia, naso-pharyngitis, upper RTI with long-term use

25
Q

doxepin moa

A

NE reuptake block and 5-HT reuptake block (TCA); primarily H1 antagonism at low doses, little anticholinergic effect when used for insomnia

26
Q

mirtazapine moa

A

significant alpha-2 antagonism, reinforcing NE and 5-HT release

27
Q

trazodone moa

A

5-HT reuptake block (slight)

28
Q

antidepressant metabolism

A

CYP metabolism

29
Q

antidepressant adverse effects

A

suicidal ideation, may precipitate psychotic episode

30
Q

1st generation antihistamine contraindications

A

elderly and narrow-angle glaucoma

31
Q

1st generation antihistamine moa

A

cross BBB producing sedation (H1 antagonism) and to a varying degree, anticholinergic actions

32
Q

1st generation antihistamine adverse effects

A

xerostomia, blurred vision, urinary retention, increased intraocular pressure; rapid tolerance may develop

33
Q

cholinergic nuclei

A

PPT and LDT nuclei

34
Q

dompaminergic nuclei

A

ventral tegmental nucleus

35
Q

histaminergic nucleus

A

tuberomamillary nuclei

36
Q

serotoninergic nucleus

A

raphe nucleus

37
Q

orexinergic neurons are activated by….

A

suprachiasmiatic nucleus through the DM nucleus of the thalamus

38
Q

barbituate moa

A

modulate GABA receptors in the CNS, binding of the drug makes GABA action last longer; at very high doses, can act as GABA itself (tox)

neuro2 (9 decks)

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