Quiz 1 Flashcards
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
Which GABA-A receptor alpha subunit is necessary for the sedative actions of Eszopiclone?
1
Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)
- Lorazepam Barbiturate withdrawal, pre-anesthetic, anxiolytic
- Diazepam Barbiturate withdrawal, pre-anesthetic, anxiolytic
- Midazolam Barbiturate withdrawal, pre-anesthetic, anxiolytic
Lorazepam = Anxiolytic
Diazepam = Barb w/d
Midazolam = Pre-anesthetic
Which of the following drugs decreases the activity of glutamate receptors? (answer yes or no, 1 pt each)
(1 pt each)
- Diazepam Yes or No
- Ethanol Yes or No
- Buspirone Yes or No
Diazepam no
Ethanol yes
Buspirone no
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
Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)
- Alprazolam pre-anesthetic, anxiolytic, Alcohol withdrawal
- Diazepam pre-anesthetic, anxiolytic, Alcohol withdrawal
- Midazolam pre-anesthetic, anxiolytic, Alcohol withdrawal
Alprazolam = anxiolytic
Diazepam = alcohol w/d
Midazolam = pre-anesthetic
- Which GABA-A receptor gamma subunit subtype is necessary for diazepam’s actions?
2
The following drugs decrease the activity of Glutamate receptors. (1 pt each)
- Diazepam True / False
- Ethanol True / False
- Zolpidem True / False
Diazepam false
Ethanol true
Zolpidem false
The following drugs exhibit pharmacokinetic tolerance with repeated daily use? (1 pt each)
- Chlordiazepoxide True / False
- Clonazepam True / False
- Diazepam True / False
all false
. Which GABA-A receptor alpha subunit subtype is necessary for Zolpidem’s
actions?
Alpha 1 or 1
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
The following drugs increase the activity of GABA-A receptors. (1 pt each)
- Chlordiazepoxide True / False
- Zolpidem True / False
- Flumazenil True / False
Chlordiazepoxide True
Zolpidem True
Flumazenil False
The following drugs exhibit pharmacokinetic tolerance with repeated daily use. (1 pt each)
- Zolpidem True / False
- Diazepam True / False
- Ethanol True / False
Zolpidem false
Diazepam false
Ethanol true
Which GABA-A receptor gamma subunit subtype is necessary for diazepam’s actions?
Gamma 2 or just 2
. 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
Which GABA-A receptor alpha subunit is necessary for zolpidem’s actions?
Alpha 1
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
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
What is the effect of the following drugs on the activity of calcium channels (don’t worry about subtype)? (1 pt each)
- Ethanol Increase / decrease / no effect
- Alprazolam Increase / decrease / no effect
- Flumazenil Increase / decrease / no effect
Ethanol Decrease
Alprazolam and Flumazenil no effect
Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)
- Alprazolam
- Diazepam
- Eszopiclone
A. Sedation
B. Anxiolytic
C. Barbituate w/d
Alprazolam = Anxiolytic
Diazepam = Barb w/d
Eszopiclone = Sedation
- Which GABA-A receptor subunit is necessary for the anxiolytic actions of diazepam? (1 pt)
gamma-1 / gamma-2 / beta-4
Gamma-2
What is the effect of the following drugs on the activity of GABA-A receptors (don’t worry about subtype)? (1 pt each)
- Zolpidem Increase / decrease / no effect
- Flurazepam Increase / decrease / no effect
- Phenobarbital Increase / decrease / no effect
All increase
What is the effect of the following drugs on the activity of glutamate receptors (don’t worry about subtype)? (1 pt each)
- Ethanol Increase / decrease / no effect
- Alprazolam Increase / decrease / no effect
- Flumazenil Increase / decrease / no effect
Ethanol Decrease
Alprazolam No effect
Flumazenil No effect
Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)
- Lorazepam
- Midazolam
- Zolpidem
A. Pre-anesthetic
B. Anxiolytic
C. Insomnia
Lorazepam = anxiolytic
Midazolam = Pre-anesthetic
Zolpidem = Insomnia
- Which GABA-A receptor subunit is necessary for the sedative actions of phenobarbital? (1 pt)
Alpha / gamma-2 / delta
Alpha
What is the effect of the following drugs on the activity of glutamate receptors (don’t worry about subtype)? (1 pt each)
- Alprazolam Increase / decrease / no effect
- Ethanol Increase / decrease / no effect
- Pentobarbital Increase / decrease / no effect
Alprazolam No effect
Ethanol Decrease
Pentobarbital Decrease
What is the effect of the following drugs on the activity of GABA-A receptors (don’t worry about subtype)? (1 pt each)
- Flumazenil Increase / decrease / no effect
- Lorazepam Increase / decrease / no effect
- Phenobarbital Increase / decrease / no effect
Flumazenil No effect
Lorazepam Increase
Phenobarbital Increase
Match the drug to its best therapeutic use: (1 pt each; answers may be used more than once)
- Oxazepam
- Midazolam
- Diazepam
A. pre-anesthetic
B. anxiolytic
C. alcohol w/d
Oxazepam = Anxiolytic Midazolam = Pre-anesthetic Diazepam = Alcohol w/d
- Which GABA-A receptor subunit is necessary for the sedative actions of eszopiclone? (1 pt)
Alpha-1 / gamma-2 / beta-2
Alpha-1
BDZ’s actions are all due to what receptors
GABA A
How do BDZ’s work at GABA A receptors
Increase affinity of GABA binding site for agonists
Increase frequency of chloride channel openings
What subunits are required for sedation?
Alpha-1
What subunits are required for anxiolytic/anticonvulsant?
Alpha-2 and 3
What subunits are required for amnestic properties?
Alpha-5
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
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
To what subunit does GABA bind?
Beta
What enzymes metabolize BDZ to active metabolites?
CYP3A4, CYP2D19
What enzymes metabolize BDZ to inactive metabolites?
Conjugation
What things inhibit metabolism of BDZ? What does this do to BDZ levels?
Cimetidine, disulfiram, oral contraceptives
What things increase metabolism of BDZ? What does this do to BDZ levels?
Chronic ethanol, isoniazid, phenytoin
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
Which drug is selective for alpha 2?
Clobazam
Approved for lennox-gastaut syndrome
Less sedative and cognitive side effects
What are bretazenil, imidazenil?
Full agonists for alpha 5
Antagonists at alpha 1
How does BDZ tolerance occur?
All pharmacodynamic
Body’s response to the drug decreases
NOT
Less drug in the body
What effect do you mostly form tolerance to?
More to sedation
Less to anticonvulsant
Very little to anxiolysis
Tolerance to sedation requires what subunit
Alpha-5
How do you treat dependence?
Switch to a long-acting BDZ
Substitute with Zolpidem
How do BDZ’s affect mesolimbic dopamine activity?
Very little effect
What are Buspirone, Gepirone?
5-HT1a partial agonists
Take weeks to work bc up/down regulation of 5-HT
What is ondansetron?
5-HT3 antagonist
Directly blocks 5HT transmission
Used for ethanol or barb w/d
How does clonidine work?
Decreases NE release via autoreceptor acrtivation