Sedative Hypnotics, Anxiolytics, and Hypnotics

Question 1

Flumazenil MOA, Use, and Tox

Answer 1

MOA: Antagonist at BDZ binding site at GABA receptor
Use: blocks actions of BDZ and “zz” drugs but not for other sedative-hypnotic drugs. IV increases recovery following BDZ administration in anesthetic procedures.
Tox: agitation,confusion,and withdrawal symptoms in those who are chronic BDZ users.

Question 2

zolpidem (ambien)
eszopiclone
zaleplon
“non-BDZ zz drugs”

MOA, Use, and Tox

Answer 2

MOA: BDZ-like action on Cl- channels

Use: minor effect on REM sleep, shorter duration of action, less hangover effect and daytime sedation, target specific GABAa subunit.

Toxicity: anterograde amnesia, hallucinations, delusions, impaired judgment, sleepwalking.

Question 3

Ramelton MOA, Use, and Tox

Answer 3

MOA: MT-1, MT-2 melatonin receptor agonist
Use: not addictive (not a controlled substance)
Tox: none

Question 4

Suvorexant MOA

Answer 4

MOA: Orexin antagonist

Question 5

Amphetamine Dextroamphetamine

Answer 5

MOA: CNS stimulation, inhibits reuptake of NE and DA, increases release of catecholamines from nerve terminals

Use: narcolepsy

Tox: sympathomimetic effects (cardiostimulation, insomnia, weight loss)

Question 6

Methylphenidate modafanil MOA, Use, and Tox

Answer 6

MOA: inhibits DA reuptake

Use: Narcolepsy

Tox: Less anxiety and anorexia than amphetamines

Question 7

Propranolol MOA, Use, Tox

Answer 7

MOA: beta-1, beta-2 antagonist

Use: blocks SANS contribution to anxiety “situational anxiety”

Tox: CNS depression, fatigue, bradycardia, asthma, hypoglycemia because of B2 blockade

Question 8

Buspirone (Buspar) MOA, Use, Tox.

Answer 8

MOA: 5HT1 agonist

Use: generalized anxiety; no sedation or addiction

Tox: headache, dizzy, nervous; several weeks for full effect