Sedative hypnotics DSA (Kruse)

Question 1

MOA of ramelteon?

Answer 1

agonist at MT1 and MT2 receptors of suprachiasmatic nuclei

Question 2

CYP metabolism of ramelteon?

Answer 2

CYP1A2 –> caution if hepatic impairment

Question 3

Avoid coadministration of ramelteon with?

Answer 3

Fluvoxamine (SSRI) b/c it is CYP1A2 inhibitor

Question 4

adverse effects of Ramelteon?

Answer 4

dizziness, somnolence, fatigue, decreased T, increased prolactin

Question 5

__ approved for tx of GAD (anxilytic effects may take >1 wk), does not cause sedation, hypnotic, euphoric, anticonvulsant, or muscle relaxant effects

Answer 5

Buspirone

Question 6

Buspirone extensively metabolized by __

Answer 6

CYP3A4

Question 7

adverse effects of Buspirone?

Answer 7

tachycardia, palpitations, nervousness, GI distress, paresthesias, dose-dependent papillary constriction

Question 8

__ approved for short-term relief of anxiety. Effective pre-operative agent to relieve anxiety and provide sedation, effective in promoting sleep in anxious and tense pt.

Answer 8

Meprobomate

Question 9

Meprobomate is an active metabolite of the drug ___

Answer 9

carisoprodol (centrally-acting muscle relaxant)

Question 10

MOA of eszopiclone, zaleplon, and zolpidem?

Answer 10

Bind GABA-A receptor sites–> a1-subunit

Question 11

clinical applications for eszopiclon, zaleplon, and zolpidem?

Answer 11

sleep disorders, esp when sleep onset is delayed

Question 12

eszopiclone, zolpidem, and zaleplon metabolized by CYP __

Answer 12

CYP3A4