Insomnia Drugs

Question 1

Benzos used for insomnia

Answer 1

estazolam, flurazepam, quazepam, temazepam, triazolam

Question 2

MOA of benzos

Answer 2

benzo receptor site on the alpha subunit of the Cl- channel complex @ BZ-1, BZ-2 & BZ-3. Upon binding to alpha subunit of Cl- channel, the receptor allosterically amplifies GABA action (inhibitory)

Question 3

action of BZ-1, BZ-2, BZ-3

Answer 3

BZ-1 = sedation, amnesia
BZ-2 = anxiolysis
BZ-3 = myorelaxation, anticonvulsant

Question 4

AE of benzos

Answer 4

sedation, cognitive impairment, rebound insomnia, hepatic disease

Question 5

complications of benzo withdrawal

Answer 5

Withdrawal = anxiety, irritability, restlessness, OSA, ventilator impairment

Question 6

CI of benzos

Answer 6

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

Question 7

pregnancy category of benzos

Answer 7

category X

Question 8

which benzo has no cyp interactions

Answer 8

temazepam

Question 9

schedule of benzos

Answer 9

schedule IV

Question 10

benzo receptor agonists

Answer 10

zolpidem, zaleplon, eszopiclone

Question 11

moa of benzo receptor agonists

Answer 11

capable only of sedative and amnesic actions via the BZ-1 receptor complex at nml clinical doses

Question 12

contraindications of BRAs

Answer 12

CI: COPD, depression, driving, other CNS Rx

Question 13

pregnancy category of BRAs

Answer 13

category C

Question 14

which BRA is cautioned in asian population

Answer 14

zaleplon due to interaction with aldehyde dehydrogenase

Question 15

which BRA has short acting and oral spray available

Answer 15

zolpidem (ambien)

Question 16

BRA DDI ?

Answer 16

CYP enzymes

Question 17

melatonin receptor agonist

Answer 17

ramelteon

Question 18

MOA of ramelteon

Answer 18

binds to MT1 & MT2 GPCR – widely in CNS. Action in suprachiasmatic nucleus impact on sleep-wake switch

Question 19

action of MT1 and MT2

Answer 19

MT1 = ↓SCN activity & ↑sleep
MT2 = maintains circadian rhythm

Question 20

AE of ramelteon

Answer 20

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

Question 21

metabolism of ramelteon

Answer 21

CYPs (possible DDI)

Question 22

issues with ramelteon elimination with repeated doses

Answer 22

no

Question 23

antidepressants used for insomnia

Answer 23

doxepin, mirtazapine, trazodone

Question 24

MOA doxepin

Answer 24

primarily anti-histaminergic @ low doses @ ↓anti-Ach at this dose

Also have potential for M-block, NE reuptake block and 5-HT reuptake block

Question 25

MOA mirtazapine

Answer 25

significant alpha-2 antagnoism, reinforcing NE, 5-HT release

Question 26

MOA trazodone

Answer 26

achieves sedation and mild 5-HT reuptake block

Question 27

AE with antidepressants

Answer 27

interaction with other CNS depressants (EtOH), suicidal ideation & worsening of suicidal thoughts Caution in patients with psychosis disorders

Question 28

metabolism of antidepressants

Answer 28

CYP metabolism (possible DDI)

Question 29

which antidepressant is approved for insomnia

Answer 29

doxepin

Question 30

where is antihistaminergic sedation regulated

Answer 30

tuberomamillary nucleus

Question 31

which 1st gen antihistamines are used for insomnia

Answer 31

diphehydramine, doxylamine

Question 32

moa of 1st gen anti-H

Answer 32

cross BBB, producing sedation and some anti-ach action

Question 33

AE of antihistamines

Answer 33

xerostomia, blurred vision, urinary retention, increase interocular pressure

Question 34

caution in antihistamines

Answer 34

elderly and narrow angle glaucoma

Question 35

which benzos have risk of accumulation

Answer 35

flurazepam, quazepam

Question 36

which benzos have no risk of accumulation

Answer 36

estazolam, temazepam, triazolam