Sleep Pharm

Question 1

Describe the 2 arousal pathways

Answer 1

1) Cholinergic neurons from the upper pons, PPT, and LDT activate the Thalamus
2) Monoaminergic: Dopaminergic (ventral tegmental nucleus), histaminergic (tuberomamilary), serotonergic (raphe nucleus), activate the cortex to process thalamic input followng cholinergic activation

Question 2

What the hell does orexin do?

Answer 2

Orein activates all of the wakeful state pathways listed above. Mediates the rapid transition between sleep and awake.

Question 3

Remember the safety issues with barbiturates:

Answer 3

They work by modulating GABA receptors to make GABA last longer. At very high doses can activate GABA itself. Remember the graph, the effects of larger doses just keep increasing. You’ll first feel sedated, then hypnotic, then completely out (anesthetized, then hit coma and it can kill you.

Question 4

How do you recognize a barbiturate drug by its name?

Answer 4

They all end in -barbital

Question 5

Benzos are much safer than barbiturates, remember their mech and how they shift the dose response curve to the left

Answer 5

ok

Question 6

All benzos are excreted how?

Answer 6

renally

Question 7

Al Benzos end in

Answer 7

-pam

Question 8

Benzo with the longest half life

Answer 8

Diazepam

Question 9

Short half life benzos? (will not accumulate)

Answer 9

Estazolam and Lorazepam

Question 10

All the benzos are contraindicated in

Answer 10

LIVER dz , COPD, Depression, Driving, other CNS drugs, Glaucoma, Category x

Question 11

All the benzodiazepines are metabolized via CYP3A4 except for

Answer 11

Quazepam which is CYP2B6

Question 12

Quaepam and Flurezepam accumulate

Answer 12

KNOW….along with Diazepam

Question 13

What the hell are the benzodiazepine receptor agonists?

Answer 13

• Important to note that they are all similar to benzo in their MOA. Include the same side effects like sedation, cognitive impairment, rebound insomnia with the short acting drugs

Question 14

Which can be used in pregnancy? Benzos or benzo receptor agonists?

Answer 14

Benzo receptor agonists- these are category c drugs

Benzos are category x

Question 15

Benzo receptor agonists we should know

Answer 15

Zolpidem
Zoleplon
Eszopiclone

Question 16

Zolpidem

Answer 16

most prescribed insominia drug on the market. comes in a sublingual form and a spray so that it can be used in the middle of the night and acts fast.

Question 17

Zaleplon

Answer 17

variability in asians

Question 18

FLUMAZENIL IS IMPORTANT WHY?

Answer 18

It is a benzo antagonist. reverses sedation from benzos quickly. IV agent.

Can cause abrupt awakening with agitation and potentially increase adverse effects.

Question 19

Ramelteon

Answer 19

Melatonin receptor agonist (MT-1 receptor)

Question 20

Antidepressants

Answer 20

Adverse effect of sedation comes in handy when you’re treating ppl who can;t sleep.

Question 21

AEs of antidepressants

Answer 21

• Cyps interactions
• Interaction with alcohol
• SUICIDE

Question 22

Doxepin

Answer 22

anti-H1 at low dose, muscarinic blocker

Question 23

Mirtazapine

Answer 23

significant alpha 2 antagonism

Question 24

Trazodone

Answer 24

anti-depressant

Question 25

1st gen antihistamines work how

Answer 25

Cross the BBB easily and produce rapid sedation through central H1 block

Question 26

WHat must you watch for with 1st gen antihistamines

Answer 26

blurred vision, INCREASED OCULAR PRESSURE therefore they are contraindicated in old ppl and glaucoma pts

Question 27

The two first gen anti-histamines

Answer 27

Diphenhydramine and doxylamine