Drugs for Insomnia

Question 1

What are some of the general concerns in regards to the development of drugs for insomnia?

Answer 1

Daytime somnolence, unconscious nighttime activity, and suicidal ideation.

Question 2

Most of the benzodiazepines, benzo receptor agonists, and barbituates act on what receptors in the CNS?

Answer 2

GABA

Question 3

Which of the benzo-structure related drugs does not work on the GABA receptors?

Answer 3

Ramelteon (melatonin receptor)

Question 4

T/F: These drugs work in place of endogenous GABA.

Answer 4

F: modifies response pattern of GABA to ligand

Question 5

T/F: Binding of benzodiazepines and their receptor antagonists produces only allosteric modification.

Answer 5

True

Question 6

ADE of Benzos and their receptor agonists

Answer 6

Sedation, cognitive impairment rebound insomnia, and withdrawal.

Question 7

What are the 3 distinct structural subgroups in the GABA receptor?

Answer 7

BZ-1, BZ-2, BZ-3

Question 8

Benzos work on what receptor subgroups?

Answer 8

All three

Question 9

Benzodiazepine receptor agonists work on what receptor subgroups?

Answer 9

BZ-1

Question 10

Benzos with long half lives usually cause what type of effects?

Answer 10

Cumulative through multiple dosings

Question 11

Which benzodiazepine works on CYP 2B6?

Answer 11

Quazepam

Question 12

Which two benzodiazepines has miniman metabolism accumulation?

Answer 12

Estazolam and Temazepam

Question 13

What preggo category are benzos?

Answer 13

Category X

Question 14

Benzos are contraindicated in what dxs?

Answer 14

COPD, Depression, hepatic diseases, closed angle glaucoma

Question 15

Preggo category of benzo receptor agonists.

Answer 15

C

Question 16

Shared characteristics of benzo receptor agonists?

Answer 16

CYP-mediators, hepatic dx, cautioned with COPD, depression and driving

Question 17

Which benzo receptor agonist can be available in both sublingual and oral spray prep?

Answer 17

Zolpidem

Question 18

Which Benzo receptor agonist can be taken in the middle of the night?

Answer 18

Zolpidem

Question 19

Special ADE of Zolpidem?

Answer 19

Different dosing recommendations for women due to diminished elimination rate (next day impairment).

Question 20

Benzo and Benzo receptor antagonist

Answer 20

Flumazenil

Question 21

Flumazenil causes what?

Answer 21

Abrupt awakening (does NOT reverse barbituates, opiate agonists and TCAs)

Question 22

Melatonin works on receptors located where?

Answer 22

Suprachiasmatic nucleus

Question 23

MT1 attenuates what?

Answer 23

SCN activity and induces sleep

Question 24

MT2 binds and dmaintains what?

Answer 24

Circadian rhythm

Question 25

Melatonin receptor agonist?

Answer 25

Ramelteon

Question 26

Special characteristics of Ramelton

Answer 26

No residual effects and no abuse

Question 27

What CYP does ramelton work on?

Answer 27

CYP1A2

Question 28

ADE of ramelton

Answer 28

Headache, somnolence, nausea, insomnia, naso-pharyngitis, upper RTI

Question 29

Antidepressants used in insomnia?

Answer 29

Doxepin, mirtazapine, trazodone

Question 30

Clinical utility in insomnia of antidepressants involves what?

Answer 30

Histaminergic signaling (tuberomammillary nucleus)

Question 31

Which antidepressant works on sedation, and bloacks M, NE, and 5-HT receptors?

Answer 31

Doxepin

Question 32

ADE of antidepressants?

Answer 32

Suicidal ideation, interactions with alcohol, and CYP metab

Question 33

2 1st gen antihistamines used in antihistamines

Answer 33

Diphenhydramine and Doxylamine

Question 34

ADE of 1st Gen antihistamines

Answer 34

Rapid tolerance and anticholinergic actions

Question 35

What population do you avoid with first gen antihistamines

Answer 35

Elderly and those with narrow-angle glaucoma

Question 36

What should you do if someone is being fucked by drug-induced insomnia?

Answer 36

Change the drug or reduce the dose before starting polydrugs for the problem

Question 37

Home remedies for insomnia

Answer 37

Melatonin, meditation, yoga and music

Question 38

Home remedies that dont work for insomnia

Answer 38

Chamomile and valerian

Question 39

MOA of suvorexant

Answer 39

Targets orexin receptors