drugs for insomnia

Question 1

flumazenil moa

Answer 1

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

Question 2

flumazenil side effects

Answer 2

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

Question 3

orexin neurons

Answer 3

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

Question 4

benzodiazepines (drugs)

Answer 4

estazolam, flurazepam, quazepam, temazepam, triazolam

Question 5

benzodiazepine receptor agonists (drugs)

Answer 5

zolpidem, zaleplon, eszopiclone

Question 6

antidepressants for insomnia

Answer 6

doxepin, mirtazepine, trazodone

Question 7

1st gen. antihistamines for insomnia

Answer 7

diphenhydramine, doxylamine

Question 8

GABA receptor

Answer 8

chloride channel

Question 9

benzodiazepine and benzodiazepine receptor agonist moa

Answer 9

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

Question 10

benzodiazepine and benzodiazepine receptor agonist adverse effects

Answer 10

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

Question 11

benzodiazepine receptor agonist target

Answer 11

BZ-1 receptor complex (at normal clinical doses)

Question 12

benzo that does not cause excessive drowsiness

Answer 12

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

Question 13

benzo without CYP interactions

Answer 13

temazepam

Question 14

benzodiazepine contraindications

Answer 14

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

Question 15

benzos with metabolic accumulation

Answer 15

flurazepam, quazepam

Question 16

BzRAs contraindications

Answer 16

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

Question 17

BzRA with ethnic variability

Answer 17

zaleplon (asians)

Question 18

approved for middle of the night wakening

Answer 18

low dose sublingual zolpidem

Question 19

flumazenil pharm

Answer 19

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

Question 20

MT1 receptor

Answer 20

melatonin binding attenuates suprachiasmatic nucleus activity and induces sleep

Question 21

MT2 receptor

Answer 21

binding maintains circadian rhythm

Question 22

ramelteon moa

Answer 22

melatonin receptor agonist

Question 23

ramelteon metabolism

Answer 23

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

Question 24

ramelteon adverse effects

Answer 24

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

Question 25

doxepin moa

Answer 25

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

Question 26

mirtazapine moa

Answer 26

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

Question 27

trazodone moa

Answer 27

5-HT reuptake block (slight)

Question 28

antidepressant metabolism

Answer 28

CYP metabolism

Question 29

antidepressant adverse effects

Answer 29

suicidal ideation, may precipitate psychotic episode

Question 30

1st generation antihistamine contraindications

Answer 30

elderly and narrow-angle glaucoma

Question 31

1st generation antihistamine moa

Answer 31

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

Question 32

1st generation antihistamine adverse effects

Answer 32

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

Question 33

cholinergic nuclei

Answer 33

PPT and LDT nuclei

Question 34

dompaminergic nuclei

Answer 34

ventral tegmental nucleus

Question 35

histaminergic nucleus

Answer 35

tuberomamillary nuclei

Question 36

serotoninergic nucleus

Answer 36

raphe nucleus

Question 37

orexinergic neurons are activated by....

Answer 37

suprachiasmiatic nucleus through the DM nucleus of the thalamus

Question 38

barbituate moa

Answer 38

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)