L17: Sedative-Hypnotics

Question 1

Alprazolam, Diazepam, Lorazepam, and Lidazolam all belong to which drug class?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines

Answer 1

E. Benzodiazepines

Question 2

Zolpidem, Eszopiclone, and Suvorexant all belong to which drug class?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines

Answer 2

C. Sleep Aids

Question 3

What drug class does Flumazenil belong to?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines

Answer 3

A. GABA Antagonists

Question 4

Both Phenobarbital and Methohexital belong to which drug class?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines

Answer 4

D. Barbituates

Question 5

Which drug class do Baclofen, Tizanadine, and Cyclobenzaprine belong to?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines

Answer 5

B. Centrally Acting Muscle Relaxants

Question 6

True or False: azolam’s have a SHORTER half life compared to azepams’s

Answer 6

True

Question 7

True or False: Suvorexant is an orexant antagonist

Answer 7

True

Question 8

All of these act on GABA-R, except which two?

Answer 8

Melantonin
Suvorexant

Question 9

True or False: Promethazine and Hydroxazine act on histamine receptor

Answer 9

True

Question 10

____: short acting benzo
____: intermediate acting benzo
____: long acting benzo

Answer 10

Triazolam
Alprazolam
Flurazepam

Question 11

____: ultra-short acting barbituate
____: short acting barbituate
____: long acting barbituate

Answer 11

Thiopental
Secobarbital
Phenobarbital

Question 12

Which is safer: Benzos or Barbituates?

Answer 12

Benzos

-Barbituates can lead to medullary depression, coma, etc

Question 13

GABA binds to GABA-A receptors, which cause __ channels to __
A. Na; close
B. Cl; close
C. Cl; open
D. Na; open

Answer 13

C. Cl; open

• Influx of Cl- into the cell hyper-polarizes the cell , leading to decreased neuronal firing

Question 14

True or False: Barbituates can act without GABA present

Answer 14

True

Question 15

Which three drugs bind to the alpha subunit of GABA only?

Answer 15

1. Flumazenil
2. Zolpidem
3. Benzodiazepines

Question 16

True or False: Zolpidem is less effective at treating anxiety. However, less apt to cause tolerance or dependence!

Answer 16

True

Question 17

True or False: Barbituates bind to alpha and beta subunits

Answer 17

True

Question 18

What makes barbituates so dangerous?

Answer 18

1. Do not require GABA binding
2. Opens Cl- channel for longer, without GABA regulation

Question 19

If a patient overdoses on a Benzodiazepine or Zolpidem, which drug can be given to reverse the effects?

Answer 19

Flumazenil

Question 20

Shorter acting drugs, such as ____ and ___ have triazole ring

Answer 20

Triazolam and Alprazolam
- aka: azolams

Question 21

What are four therapeutic effects of benzos?

Answer 21

1. Sedative
2. Hypnotic
3. Anti-convulsant
4. Muscle relaxant

Question 22

How do the -azolams and -azepams work?
A. antagonist at benzodiazepine sites on GABA-A
B. binds to GABA-A receptor subunits, facilitates Cl- channel opening

Answer 22

B. binds to GABA-A receptor subunits, facilitates Cl- channel opening

• membrane hyperpolarization

Question 23

What can the -azolams and
-azepams be used to treat?

Answer 23

1. Acute anxiety states
2. Panic attacks
3. Insomnia

Question 24

All of the -azolams and -azepams have hepatic metabolism, except which two (have OH group)?

Answer 24

Oxazepam and Lorazepam
- these drugs are better choice for someone with decreased liver function

Question 25

True or False: Taking ETOH with benzos (-azolams and -azepams) results in an additive effect

Answer 25

True

Question 26

True or False: Tolerance and dependence can result with use of benzodiazepines (-azolams and -azepams)

Answer 26

True

Question 27

_____: antagonist at benzodiazepine sites on GABA-A receptor, used to manage benzodiazepine overdose

Answer 27

Flumazenil

Question 28

Which drugs are most long acting?

Answer 28

Diazepam and Chlorazepate

Question 29

Which receptor is associated with wakefulness, food intake, and energy/glucose metabolism? Which is associated with circadian, energy balance, and insulin secretion?

Answer 29

1) Orexin 2) Melatonin

Question 30

Benzodiazepines affect sleep by decreasing ___, duration of of stages _ and _, and number of ____

Answer 30

sleep latency; stages 3 and 4; number of awakenings

Question 31

True or False: Benzos decrease duration in REM, but not as much as barbituates do

Answer 31

True

Question 32

REM Rebound is commonly associated with abrupt cessation of which drug class? A. Anti-histamines B. Sedatives C. Benzos D. Barbituates

Answer 32

C. Benzos - characterized by: increased frequency and intensity of dreams

Question 33

How the sedative-hypnotics, Zolpidem and Eszopiclone, act? What do they treat? A. Agonist at melatonin receptor B. Enhance GABA effects C. Inhibit orexin 1 and 2

Answer 33

B. Enhance GABA effects Treats: insomnia

Question 34

True or False: Hypotension is associated with use of Zolpidem and Eszopiclone

Answer 34

True

Question 35

____: A schedule IV controlled substance that inhibits orexin 1 and 2 receptors A. Diazepam B. Chlorazepate C. Suvorexant

Answer 35

C. Suvorexant

Question 36

True or False: Suvorexant is associated with daytime somnolence, worsening depression, and SI

Answer 36

True

Question 37

How does Suvorexant work?

Answer 37

Decreases sleep latency Enhances sleep maintenance

Question 38

True or False: The barbituates thiopental and thiamylal have longer half lives

Answer 38

False - shorter - Presence of sulfur decreases their solubility and duration of action

Question 39

What is the barbituate methohexital used for? phenobarbital?

Answer 39

Anesthesia Seizure

Question 40

True or False: Barbituates have extension CNS effects, may lead to tolerance and dependence

Answer 40

True

Question 41

True or False: Lipid solubility allows benzodiazepines to readily cross BBB

Answer 41

False - this is the case with barbituates

Question 42

True or False: Redistribution is important for termination of action of US acting barbituates (e.g thiopental)

Answer 42

True

Question 43

What are three unique side effects of barbituates?

Answer 43

1. Allergic reactions 2. Aggravation of acute intermittent porphyria 3. Respiratory depression - no cure 4. Withdrawal syndrome

Question 44

Barbituates and DDI?

Answer 44

1. Additive effect with CNS depressants 2. MAO Inhibitors enhance CNS depression 3. Induction of hepatic enzymes

Question 45

____ and ____ are histamine H2 receptor inverse agonists

Answer 45

Hydroxyzine and Promethazine

Question 46

True or False: Barbituate use can make warfarin less effective

Answer 46

True

Question 47

____ is a competitive antagonist of beta-1 adrenergic receptor in the heart that is used for situational anxiety

Answer 47

Propranolol - has extensive 1st pass met

Question 48

___: facilitates GABA and is used to treat muscle spasms. Redistribution is important for its termination. However, is can lead to withdrawal syndrome. A. Cyclobenzaprine B. Tizanidine C. Baclofen D. Diazepam

Answer 48

D. Diazepam

Question 49

____ is a GABA-B receptor agonist used to treat spasticity associated with MS -- can cause CNS depression/dependency A. Cyclobenzaprine B. Tizanidine C. Baclofen D. Diazepam

Answer 49

C. Baclofen

Question 50

____ is used to treat muscle spasms of local origin and inhibits both gamma and alpha motor systems A. Cyclobenzaprine B. Tizanidine C. Baclofen D. Diazepam

Answer 50

A. Cyclobenzaprine

Question 51

____ is an alpha 2 adrenergic agonist used to relax skeletal muscles -- can result in hypotension A. Cyclobenzaprine B. Tizanidine C. Baclofen D. Diazepam

Answer 51

B. Tizanidine

Question 52

ok

Answer 52