Hypnotics + Sedatives

Question 1

List the six major CNS depressants

Answer 1

General anesthetics
Narcotics

Ethanol
Barbiturates

Benzodiazepines
Non-benzodiazepine hypnotics

Question 2

Name three positive allosteric modulators at GABA(A) receptors

Answer 2

Benzodiazepines

Flumazenil

Non-benzodiazepines

Question 3

Compare/contrast barbiturates with benzodiazepines with respect to

Daytime sedation
Effect on sleep cycle

Answer 3

Sedation
+barb = yes
+BNZ = not necessarily

Effect on sleep cycle
+barb = yes
+BNZ = yes, but less than barb’s

Question 4

Compare/contrast barbiturates with benzodiazepines with respect to

Tolerance
Abuse potential

Answer 4

Tolerance
+barb = yes (PK/PD)
+BNZ = yes (PD)

Abuse potential
+barb = high
+BNZ = moderate

Question 5

Compare/contrast barbiturates with benzodiazepines with respect to

Safeties in overdose
Drug interactions

Answer 5

Safety in OD
+barb = no (low TI)
+BNZ = yes (when used alone)

Drug interactions:
+barb = many (induce CYP450 and UDP)
+BNZ = few

Question 6

List the four major pharmacological effects

Answer 6

Various stage of CNS depression

Anti-seizure activity

Psychomotor impairment

Drowsiness, confusion, amnesia

Question 7

For following benzodiazepines, distinguish between short, intermediate, and long-acting:

Midazolam
Triazolam
Oxazepam
Alprazolam
Temazepam
Diazepam
Flurazepam

Answer 7

“Try My OATS Funky Doctor”

Triazolam, Midazolam = short

Oxazepam, Alprazolam, Temazepam = intermediate

Flurazepam, Diazepam = long

Question 8

Correlate long and short acting benzodiazepines with the incidence of daytime sedation and rebound insomnia

Answer 8

Daytime sedation
+long = yes
+short = no

Rebound insomnia
+short = allow
+long = limits

Question 9

List the benzodiazepine antagonist used for benzodiazepine intoxication

Answer 9

Flumazenil

Question 10

List three non-benzodiazepine hypnotics that are functionally but not chemically related to BDZ and list their major uses (sleep maintenance vs sleep induction)

Answer 10

Zaleplon
+sleep induction

Zolpidem
+sleep induction
+sleep maintenance

Eszoplicone
+sleep maintenance

Question 11

Briefly describe the MOA and clinical use of ramelteon and suvorexant

Answer 11

Ramelteon
+use: hypnotic (not controlled)
+MOA: melatonin R agonist

Suvorexant
+use: sleep onset and sleep maintenance
+MOA: orexin R antagonist

Question 12

List common properties of CNS depressants

Answer 12

Tolerance

Cross-tolerance

Additivity

Physical dependence

High abuse potential

Question 13

List 4 pharmacological effects of benzodiazepines?

Answer 13

Anxiolytics

Sedative hypnotic

Anticonvulsant

Muscle relaxant

Question 14

List 4 side effects of benzodiazepines?

Answer 14

Drowsiness

Confusion

Amnesia

Psychomotor impairment

Question 15

List anxiolytics

Answer 15

Benzodiazepines

Non-BNZ (buspirone)

SSRIs

Beta-adrenergic antagonists

Question 16

What are midazolam and clonazepam also approved for?

Answer 16

Midazolam = surgery

Clonazepam = epilepsy