L17: Sedative-Hypnotics Flashcards

1
Q

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

A

E. Benzodiazepines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

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

A

C. Sleep Aids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

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

A

A. GABA Antagonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

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

A

D. Barbituates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

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

A

B. Centrally Acting Muscle Relaxants

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

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

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

True or False: Suvorexant is an orexant antagonist

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

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

A

Melantonin
Suvorexant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

True or False: Promethazine and Hydroxazine act on histamine receptor

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

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

A

Triazolam
Alprazolam
Flurazepam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

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

A

Thiopental
Secobarbital
Phenobarbital

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Which is safer: Benzos or Barbituates?

A

Benzos

-Barbituates can lead to medullary depression, coma, etc

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

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

A

C. Cl; open

  • Influx of Cl- into the cell hyper-polarizes the cell , leading to decreased neuronal firing
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

True or False: Barbituates can act without GABA present

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

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

A
  1. Flumazenil
  2. Zolpidem
  3. Benzodiazepines
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

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

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

True or False: Barbituates bind to alpha and beta subunits

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What makes barbituates so dangerous?

A
  1. Do not require GABA binding
  2. Opens Cl- channel for longer, without GABA regulation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

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

A

Flumazenil

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

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

A

Triazolam and Alprazolam
- aka: azolams

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What are four therapeutic effects of benzos?

A
  1. Sedative
  2. Hypnotic
  3. Anti-convulsant
  4. Muscle relaxant
22
Q

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

A

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

  • membrane hyperpolarization
23
Q

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

A
  1. Acute anxiety states
  2. Panic attacks
  3. Insomnia
24
Q

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

A

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

25
Q

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

A

True

26
Q

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

A

True

27
Q

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

A

Flumazenil

28
Q

Which drugs are most long acting?

A

Diazepam and Chlorazepate

29
Q

Which receptor is associated with wakefulness, food intake, and energy/glucose metabolism?

Which is associated with circadian, energy balance, and insulin secretion?

A

1) Orexin
2) Melatonin

30
Q

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

A

sleep latency; stages 3 and 4; number of awakenings

31
Q

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

A

True

32
Q

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

A

C. Benzos

  • characterized by: increased frequency and intensity of dreams
33
Q

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

A

B. Enhance GABA effects

Treats: insomnia

34
Q

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

A

True

35
Q

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

A

C. Suvorexant

36
Q

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

A

True

37
Q

How does Suvorexant work?

A

Decreases sleep latency
Enhances sleep maintenance

38
Q

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

A

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

39
Q

What is the barbituate methohexital used for? phenobarbital?

A

Anesthesia
Seizure

40
Q

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

A

True

41
Q

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

A

False - this is the case with barbituates

42
Q

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

A

True

43
Q

What are three unique side effects of barbituates?

A
  1. Allergic reactions
  2. Aggravation of acute intermittent porphyria
  3. Respiratory depression - no cure
  4. Withdrawal syndrome
44
Q

Barbituates and DDI?

A
  1. Additive effect with CNS depressants
  2. MAO Inhibitors enhance CNS depression
  3. Induction of hepatic enzymes
45
Q

____ and ____ are histamine H2 receptor inverse agonists

A

Hydroxyzine and Promethazine

46
Q

True or False: Barbituate use can make warfarin less effective

A

True

47
Q

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

A

Propranolol
- has extensive 1st pass met

48
Q

___: 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

A

D. Diazepam

49
Q

____ 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

A

C. Baclofen

50
Q

____ 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

A

A. Cyclobenzaprine

51
Q

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

A

B. Tizanidine

52
Q

ok

A