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Flashcards in Quiz 1 Deck (52):
1

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

Decrease

2

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

1

3

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

3. Lorazepam Barbiturate withdrawal, pre-anesthetic, anxiolytic

4. Diazepam Barbiturate withdrawal, pre-anesthetic, anxiolytic

5. Midazolam Barbiturate withdrawal, pre-anesthetic, anxiolytic

Lorazepam = Anxiolytic

Diazepam = Barb w/d

Midazolam = Pre-anesthetic

4

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

6. Diazepam Yes or No

7. Ethanol Yes or No

8. Buspirone Yes or No

Diazepam no
Ethanol yes
Buspirone no

5

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

Decrease

6

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

5. Alprazolam pre-anesthetic, anxiolytic, Alcohol withdrawal

6. Diazepam pre-anesthetic, anxiolytic, Alcohol withdrawal

7. Midazolam pre-anesthetic, anxiolytic, Alcohol withdrawal

Alprazolam = anxiolytic

Diazepam = alcohol w/d

Midazolam = pre-anesthetic

7


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


2

8

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

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

Diazepam false
Ethanol true
Zolpidem false

9

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

4. Chlordiazepoxide True / False
5. Clonazepam True / False
6. Diazepam True / False

all false

10

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

actions?

Alpha 1 or 1

11

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)

Decrease

12

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

Chlordiazepoxide True
Zolpidem True
Flumazenil False

13


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

4. Zolpidem True / False
5. Diazepam True / False
6. Ethanol True / False

Zolpidem false
Diazepam false
Ethanol true

14

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

Gamma 2 or just 2

15

. 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)

Decrease

16

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

Alpha 1

17

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

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

Ethanol

18

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

D. A and B only

19

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

4. Ethanol Increase / decrease / no effect

5. Alprazolam Increase / decrease / no effect

6. Flumazenil Increase / decrease / no effect

Ethanol Decrease

Alprazolam and Flumazenil no effect

20

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

7. Alprazolam
8. Diazepam
9. Eszopiclone

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

Alprazolam = Anxiolytic

Diazepam = Barb w/d

Eszopiclone = Sedation

21

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

Gamma-2

22

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

All increase

23

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

4. Ethanol Increase / decrease / no effect

5. Alprazolam Increase / decrease / no effect

6. Flumazenil Increase / decrease / no effect

Ethanol Decrease

Alprazolam No effect

Flumazenil No effect

24

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

7. Lorazepam
8. Midazolam
9. Zolpidem


A. Pre-anesthetic
B. Anxiolytic
C. Insomnia

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