Pharmacology: Sleep

Question 1

Main receptor associated with Pharmacology of Sleep

Answer 1

GABA receptor

Question 2

MOA of Benzodiazepines

Answer 2

Facilitate GABAA action by increasing the FREQUENCY of Cl- Channel Opening.

Question 3

Used for Short term Insomnia (7-10 days)

Answer 3

Benzodiazepines and Non-benzodiazepines

Question 4

Benzodiazepine Drug Names

Answer 4

Temazepam and Triazolam

Question 5

Drug that has adverse effect of rebound insomnia with abrupt discontinuation

Answer 5

Benzodiazepines - Temazepam and Triazolam

Question 6

Non-benzodiazepines drug names and main adverse effect

Answer 6

• Zolpidem (and Zaleplon as well as Escopiclone)

- A/E: Sleep Walking, Sleep Driving, etc.

Question 7

MOA of Zolpidem (and Zaleplon as well as Escopiclone)

Answer 7

• Facilitate GABAa action by binding specifically to site of alpha 1 subunit of benzodiazepine site (BZ1) => Very specific, less risk for rebound insomnia compared to Benzos)

Question 8

Drug used specifically for onset of sleep in insomnia

Answer 8

Ramelteon

Question 9

MOA of Ramelteon

Answer 9

Agonist at Melatonin Receptors => Circardian Rhythms

Question 10

MOA of 5-HT Receptor Modulator + Drug name

Answer 10

Trazodone - Selective inhibitor of SERT + major metabolite (m-cpp) that is a potent 5-HT2 antagonist (antidepressant effect)

• Therapeutic Indication of Insomnia + Major Depression (more via metabolite?)

Question 11

Concept of Narcolepsy: Main component of “pathology”

Answer 11

Orexin Neurons: thought to regulate awake and sleep state
- patients with narcolepsy (excessive sleepiness, tiredness, and cataplexy) usually have significant decrease of orexin neurons)

Question 12

Drug used for narcolepsy and to reduce excessive sleepiness

Answer 12

Modafinil