Quiz 1 Flashcards

(52 cards)

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
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
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
10. Which GABA-A receptor subunit is necessary for the sedative actions of phenobarbital? (1 pt) Alpha / gamma-2 / delta
Alpha
26
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
Alprazolam No effect Ethanol Decrease Pentobarbital Decrease
27
What is the effect of the following drugs on the activity of GABA-A receptors (don’t worry about subtype)? (1 pt each) 4. Flumazenil Increase / decrease / no effect 5. Lorazepam Increase / decrease / no effect 6. Phenobarbital Increase / decrease / no effect
Flumazenil No effect Lorazepam Increase Phenobarbital Increase
28
Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once) 7. Oxazepam 8. Midazolam 9. Diazepam A. pre-anesthetic B. anxiolytic C. alcohol w/d
``` Oxazepam = Anxiolytic Midazolam = Pre-anesthetic Diazepam = Alcohol w/d ```
29
10. Which GABA-A receptor subunit is necessary for the sedative actions of eszopiclone? (1 pt) Alpha-1 / gamma-2 / beta-2
Alpha-1
30
BDZ's actions are all due to what receptors
GABA A
31
How do BDZ's work at GABA A receptors
Increase affinity of GABA binding site for agonists | Increase frequency of chloride channel openings
32
What subunits are required for sedation?
Alpha-1
33
What subunits are required for anxiolytic/anticonvulsant?
Alpha-2 and 3
34
What subunits are required for amnestic properties?
Alpha-5
35
What is flumazenil?
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
What are picrotoxin, bicuculline?
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
To what subunit does GABA bind?
Beta
38
What enzymes metabolize BDZ to active metabolites?
CYP3A4, CYP2D19
39
What enzymes metabolize BDZ to inactive metabolites?
Conjugation
40
What things inhibit metabolism of BDZ? What does this do to BDZ levels?
Cimetidine, disulfiram, oral contraceptives
41
What things increase metabolism of BDZ? What does this do to BDZ levels?
Chronic ethanol, isoniazid, phenytoin
42
Which BDZs bind to only alpha-1 subunits? Why are these beneficial?
Zolpidem, zaleplon, eszopliclone, indiplone Very potent sedative effets but less effects on REM Less rebound insomnia, less tolerance/dependence
43
Which drug is selective for alpha 2?
Clobazam Approved for lennox-gastaut syndrome Less sedative and cognitive side effects
44
What are bretazenil, imidazenil?
Full agonists for alpha 5 | Antagonists at alpha 1
45
How does BDZ tolerance occur?
All pharmacodynamic Body's response to the drug decreases NOT Less drug in the body
46
What effect do you mostly form tolerance to?
More to sedation Less to anticonvulsant Very little to anxiolysis
47
Tolerance to sedation requires what subunit
Alpha-5
48
How do you treat dependence?
Switch to a long-acting BDZ | Substitute with Zolpidem
49
How do BDZ's affect mesolimbic dopamine activity?
Very little effect
50
What are Buspirone, Gepirone?
5-HT1a partial agonists Take weeks to work bc up/down regulation of 5-HT
51
What is ondansetron?
5-HT3 antagonist Directly blocks 5HT transmission Used for ethanol or barb w/d
52
How does clonidine work?
Decreases NE release via autoreceptor acrtivation