Quiz 1 Flashcards

1
Q

How would switching from a short‑acting benzodiazepine to a longer acting benzodiazepine affect the severity of benzodiazepine withdrawal symptoms? (1 pt)

	 Increase, Decrease, No change
A

Decrease

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2
Q

Which GABA-A receptor alpha subunit is necessary for the sedative actions of Eszopiclone?

A

1

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3
Q

Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)

  1. Lorazepam Barbiturate withdrawal, pre-anesthetic, anxiolytic
  2. Diazepam Barbiturate withdrawal, pre-anesthetic, anxiolytic
  3. Midazolam Barbiturate withdrawal, pre-anesthetic, anxiolytic
A

Lorazepam = Anxiolytic

Diazepam = Barb w/d

Midazolam = Pre-anesthetic

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4
Q

Which of the following drugs decreases the activity of glutamate receptors? (answer yes or no, 1 pt each)
(1 pt each)

  1. Diazepam Yes or No
  2. Ethanol Yes or No
  3. Buspirone Yes or No
A

Diazepam no
Ethanol yes
Buspirone no

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5
Q

How would switching from a longer acting benzodiazepine to a short‑acting benzodiazepine affect the severity of residual daytime drowsiness caused by this treatment? (1 pt)

Increase, Decrease, No change

A

Decrease

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6
Q

Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)

  1. Alprazolam pre-anesthetic, anxiolytic, Alcohol withdrawal
  2. Diazepam pre-anesthetic, anxiolytic, Alcohol withdrawal
  3. Midazolam pre-anesthetic, anxiolytic, Alcohol withdrawal
A

Alprazolam = anxiolytic

Diazepam = alcohol w/d

Midazolam = pre-anesthetic

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7
Q
  1. Which GABA-A receptor gamma subunit subtype is necessary for diazepam’s actions?
A

2

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8
Q

The following drugs decrease the activity of Glutamate receptors. (1 pt each)

  1. Diazepam True / False
  2. Ethanol True / False
  3. Zolpidem True / False
A

Diazepam false
Ethanol true
Zolpidem false

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9
Q

The following drugs exhibit pharmacokinetic tolerance with repeated daily use? (1 pt each)

  1. Chlordiazepoxide True / False
  2. Clonazepam True / False
  3. Diazepam True / False
A

all false

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10
Q

. Which GABA-A receptor alpha subunit subtype is necessary for Zolpidem’s

actions?
A

Alpha 1 or 1

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11
Q

How would switching from a short‑acting benzodiazepine to a longer-acting

Benzodiazepine, affect the severity of benzodiazepine withdrawal symptoms 

 (increase, decrease, no change) (1 pt)
A

Decrease

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12
Q

The following drugs increase the activity of GABA-A receptors. (1 pt each)

  1. Chlordiazepoxide True / False
  2. Zolpidem True / False
  3. Flumazenil True / False
A

Chlordiazepoxide True
Zolpidem True
Flumazenil False

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13
Q

The following drugs exhibit pharmacokinetic tolerance with repeated daily use. (1 pt each)

  1. Zolpidem True / False
  2. Diazepam True / False
  3. Ethanol True / False
A

Zolpidem false
Diazepam false
Ethanol true

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14
Q

Which GABA-A receptor gamma subunit subtype is necessary for diazepam’s actions?

A

Gamma 2 or just 2

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15
Q

. How would switching from a long‑acting benzodiazepine to a shorter acting

Benzodiazepine affect the severity of residual daytime drowsiness caused by this 

treatment?   (increase, decrease, no change)
A

Decrease

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16
Q

Which GABA-A receptor alpha subunit is necessary for zolpidem’s actions?

A

Alpha 1

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17
Q

Which of the following drugs decreases the activity of glutamate receptors? (3 pts)

A. Diazepam
B. Ethanol
C. Zolpidem
D. All of the above

A

Ethanol

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18
Q

Which of the following drugs exhibit both pharmacokinetic and pharmacodynamic tolerance with repeated daily use? (3 pts)

		A. Pentobarbital 
		B. Ethanol
		C. Diazepam
		D. A and B only
		E. All of the above
A

D. A and B only

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19
Q

What is the effect of the following drugs on the activity of calcium channels (don’t worry about subtype)? (1 pt each)

  1. Ethanol Increase / decrease / no effect
  2. Alprazolam Increase / decrease / no effect
  3. Flumazenil Increase / decrease / no effect
A

Ethanol Decrease

Alprazolam and Flumazenil no effect

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20
Q

Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)

  1. Alprazolam
  2. Diazepam
  3. Eszopiclone

A. Sedation
B. Anxiolytic
C. Barbituate w/d

A

Alprazolam = Anxiolytic

Diazepam = Barb w/d

Eszopiclone = Sedation

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21
Q
  1. Which GABA-A receptor subunit is necessary for the anxiolytic actions of diazepam? (1 pt)
    gamma-1 / gamma-2 / beta-4
A

Gamma-2

22
Q

What is the effect of the following drugs on the activity of GABA-A receptors (don’t worry about subtype)? (1 pt each)

  1. Zolpidem Increase / decrease / no effect
  2. Flurazepam Increase / decrease / no effect
  3. Phenobarbital Increase / decrease / no effect
A

All increase

23
Q

What is the effect of the following drugs on the activity of glutamate receptors (don’t worry about subtype)? (1 pt each)

  1. Ethanol Increase / decrease / no effect
  2. Alprazolam Increase / decrease / no effect
  3. Flumazenil Increase / decrease / no effect
A

Ethanol Decrease

Alprazolam No effect

Flumazenil No effect

24
Q

Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)

  1. Lorazepam
  2. Midazolam
  3. Zolpidem

A. Pre-anesthetic
B. Anxiolytic
C. Insomnia

A

Lorazepam = anxiolytic

Midazolam = Pre-anesthetic

Zolpidem = Insomnia

25
Q
  1. Which GABA-A receptor subunit is necessary for the sedative actions of phenobarbital? (1 pt)
    Alpha / gamma-2 / delta
A

Alpha

26
Q

What is the effect of the following drugs on the activity of glutamate receptors (don’t worry about subtype)? (1 pt each)

  1. Alprazolam Increase / decrease / no effect
  2. Ethanol Increase / decrease / no effect
  3. Pentobarbital Increase / decrease / no effect
A

Alprazolam No effect
Ethanol Decrease
Pentobarbital Decrease

27
Q

What is the effect of the following drugs on the activity of GABA-A receptors (don’t worry about subtype)? (1 pt each)

  1. Flumazenil Increase / decrease / no effect
  2. Lorazepam Increase / decrease / no effect
  3. Phenobarbital Increase / decrease / no effect
A

Flumazenil No effect
Lorazepam Increase
Phenobarbital Increase

28
Q

Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)

  1. Oxazepam
  2. Midazolam
  3. Diazepam

A. pre-anesthetic
B. anxiolytic
C. alcohol w/d

A
Oxazepam = Anxiolytic
Midazolam = Pre-anesthetic
Diazepam = Alcohol w/d
29
Q
  1. Which GABA-A receptor subunit is necessary for the sedative actions of eszopiclone? (1 pt)

Alpha-1 / gamma-2 / beta-2

A

Alpha-1

30
Q

BDZ’s actions are all due to what receptors

A

GABA A

31
Q

How do BDZ’s work at GABA A receptors

A

Increase affinity of GABA binding site for agonists

Increase frequency of chloride channel openings

32
Q

What subunits are required for sedation?

A

Alpha-1

33
Q

What subunits are required for anxiolytic/anticonvulsant?

A

Alpha-2 and 3

34
Q

What subunits are required for amnestic properties?

A

Alpha-5

35
Q

What is flumazenil?

A

BDZ Competitive ANTAGONIST (does NOT have a measurable response in healthy individuals, just in people taking BDZ’s. Increases amount of BDZ required for a response)

USED FOR BDZ OVERDOSE

36
Q

What are picrotoxin, bicuculline?

A

BDZ NONCOMPETITIVE antagonists

Picrotoxin blocks the channel

Bicuculline binds GABA site to block GABA from binding. it is noncompetitive because it doesn’t bind BDZ site - it binds the GABA site so even if BDZ binds GABA can’t

37
Q

To what subunit does GABA bind?

A

Beta

38
Q

What enzymes metabolize BDZ to active metabolites?

A

CYP3A4, CYP2D19

39
Q

What enzymes metabolize BDZ to inactive metabolites?

A

Conjugation

40
Q

What things inhibit metabolism of BDZ? What does this do to BDZ levels?

A

Cimetidine, disulfiram, oral contraceptives

41
Q

What things increase metabolism of BDZ? What does this do to BDZ levels?

A

Chronic ethanol, isoniazid, phenytoin

42
Q

Which BDZs bind to only alpha-1 subunits? Why are these beneficial?

A

Zolpidem, zaleplon, eszopliclone, indiplone
Very potent sedative effets but less effects on REM

Less rebound insomnia, less tolerance/dependence

43
Q

Which drug is selective for alpha 2?

A

Clobazam
Approved for lennox-gastaut syndrome
Less sedative and cognitive side effects

44
Q

What are bretazenil, imidazenil?

A

Full agonists for alpha 5

Antagonists at alpha 1

45
Q

How does BDZ tolerance occur?

A

All pharmacodynamic
Body’s response to the drug decreases
NOT
Less drug in the body

46
Q

What effect do you mostly form tolerance to?

A

More to sedation
Less to anticonvulsant
Very little to anxiolysis

47
Q

Tolerance to sedation requires what subunit

A

Alpha-5

48
Q

How do you treat dependence?

A

Switch to a long-acting BDZ

Substitute with Zolpidem

49
Q

How do BDZ’s affect mesolimbic dopamine activity?

A

Very little effect

50
Q

What are Buspirone, Gepirone?

A

5-HT1a partial agonists

Take weeks to work bc up/down regulation of 5-HT

51
Q

What is ondansetron?

A

5-HT3 antagonist
Directly blocks 5HT transmission
Used for ethanol or barb w/d

52
Q

How does clonidine work?

A

Decreases NE release via autoreceptor acrtivation