28b - Drugs for Insomnia

Question 1

MOA of estazolam

Answer 1

benzodiazepine

Question 2

MOA of flurazepam

Answer 2

benzodiazepine

Question 3

MOA of quazepam

Answer 3

benzodiazepine

Question 4

MOA of temazepam

Answer 4

benzodiazepine

Question 5

MOA of triazolam

Answer 5

benzodiazepine

Question 6

MOA of doxepin

Answer 6

antidepressant

Question 7

MOA of mirtazapine

Answer 7

antidepressant

Question 8

MOA of trazodone

Answer 8

antidepressant

Question 9

MOA of zolpidem

Answer 9

benzodizepine receptor agonist

Question 10

MOA of zaleplon

Answer 10

benzodizepine receptor agonist

Question 11

MOA of eszopiclone

Answer 11

benzodizepine receptor agonist

Question 12

MOA of ramelteon

Answer 12

melatonin receptor agonist

Question 13

MOA of diphenhydramine

Answer 13

1st gen antihistamine

Question 14

MOA of doxylamine

Answer 14

1st gen antihistamine

Question 15

What are the 2 arousal pathways?

Answer 15

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

Question 16

What drugs are approved for insomnia?

Answer 16

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

Question 17

Which insomnia drug does NOT work on GABA receptors?

Answer 17

Ramelteon

Question 18

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

Answer 18

barbiturates at high doses

Question 19

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

Answer 19

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

Question 20

Which BNZ subgroups do benzodiazepines act on?

Answer 20

all three, BZ1-3

Question 21

which BNZ subgroups do BRAs act on?

Answer 21

only on BZ1 at normal doses

Question 22

What is the longest acting BNZ?

Answer 22

diazepam

Question 23

What is the shortest acting BNZ?

Answer 23

midazolam

Question 24

Which BNZ has CYP 2B6 activity?

Answer 24

Quazepam

Question 25

Which BNZ has no CYP interactions?

Answer 25

Temazepam

Question 26

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

Answer 26

Zolpidem because of its short period of activity

Question 27

What do you give for BNZ overdose?

Answer 27

flumazenil, and BNZ antagonist and BzRA antagonist. | can reverse overdose, cause withdrawals

Question 28

ADE of flumazenil?

Answer 28

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

Question 29

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

Answer 29

``` MT1 = SCN activity to induce sleep MT2 = maintains circadian rhythm MT3 = NOT involved in sleep ```

Question 30

ADE of ramelteon?

Answer 30

not many. No abuse or respiratory depression

Question 31

What is the only antidepressant approved for insomnia?

Answer 31

doxepin

Question 32

Why do antidepressants work for insomnia?

Answer 32

seem to work thorugh H1 antagonism in tuberomamillary nucleus

Question 33

ADE of antidepressants for insomnia?

Answer 33

suicidal ideation | CYP interactions

Question 34

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

Answer 34

diphenhydramine and doxylamine. | cross BBB to inhibit H1 and some Ach.

Question 35

ADE of 1st gen antihistamines?

Answer 35

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

Question 36

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

Answer 36

benzodiazepene withdrawals

Question 37

ADE of BNZs?

Answer 37

sedation, cognitive impairment, rebound insomnia