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BAHS 505 > CNS depressants > Flashcards

CNS depressants Flashcards

1
Q

What two benzodiazepines did we discuss in class?

A

Diazepam and triazolam

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2
Q

Class of diazepam?

A

Benzodiazepine

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3
Q

Mechanism of action for diazepam?

A

Enhance GABA mediated CI- conductance and neuronal inhibition

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4
Q

Which benzodiazepine mediates Cl- conductance to inhibit neuronal transmission?

A

Diazepam

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5
Q

Which benzo is long-acting?

A

Diazepam

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6
Q

How does diazepam provide a calming, anxiolytic effect?

A

Because it is long acting, it provides a steady state concentration in the CNS.

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7
Q

Why shouldn’t you take diazepam long term?

A

Can build up in system

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8
Q

Class of triazolam?

A

Benzodiazepine

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9
Q

Which benzo is short-acting?

A

Triazolam

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10
Q

Which benzo is not for anxiety but rather for sleep disorders?

A

Triazolam

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11
Q

Sleeping aid benzo?

A

Triazolam

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12
Q

Which two drugs are NBRAs (non-benzodiazepine receptor agonist)?

A

Zolpidem (Ambien) + Eszopiclone (Lunesta)

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13
Q

More common name of Zolpidem?

A

Ambien

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14
Q

Class of Zolpidem (Ambien)?

A

NBRA (non-benzo receptor agonist)

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15
Q

Which NBRA is selective for type 1 benzo receptors?

A

Zolpidem

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16
Q

Zolpidem binds which receptors?

A

Selectively binds type 1 benzo receptors

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17
Q

Half-life of zolpidem?

A

2-6 hours

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18
Q

Active metabolites of zolpidem?

A

None

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19
Q

Mechanism of action of zolpidem?

A

Binds to benzo type 1 receptor to enhance GABA-mediated Cl- conductance and neuronal inhibition

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20
Q

Zolpidem and Eszopiclone are _________-acting.

A

short-acting

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21
Q

Which NBRA is useful for acute treatment of sleep disorders?

A

Zolpidem

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22
Q

Which state of sleep is conserved when using Zolpidem?

A

Stage 3

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23
Q

Antagonist of Zolpidem?

A

Flumazenil

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24
Q

Class of Eszopiclone?

A

NRBA

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25
Which NBRA binds all three benzo receptor types?
Eszopiclone
26
Half-life of Eszopiclone?
6 hours
27
Active metabolite of Eszopiclone?
None
28
Mechanism of Eszopiclone?
Binds to all subtypes of benzo receptors to enhance GABA-mediated Cl- conductance and neuronal inhibition
29
Which NBRA is appropriate for chronic treatment of sleep disorders?
Eszopiclone
30
Antagonist of Eszopiclone?
Flumazenil
31
Mechanism of NBRAs?
Binds to benzo receptors to enhance GABA-mediated Cl- conductance and neuronal inhibition
32
Class of belsomra?
Orexin receptor antagonist
33
Effect of belsomra?
Causes wakefulness
34
Belsomra acts on which receptors?
Highly selective antagonist for orexin receptors
35
Belsomra is a highly-selective ___________ for orexin receptors.
Antagonist
36
Which two drugs act on alcohol receptors?
Ethanol and methanol
37
Ethanol works on which receptors?
Alcohol receptors
38
What parts of the brain are most sensitive to ethanol?
Polysynaptic reticular activating system and the cerebral cortex
39
Effect of ethanol on the lipid bilayer of the plasma membrane? Result?
Dissolves the lipid bilayer of plasma membrane reduces membrane viscosity and disrupts protein function
40
Effect of ethanol on membrane viscosity?
Reduces viscosity
41
Effect of ethanol on proteins?
Disrupts protein function
42
Mechanism of action of ethanol?
Increases GABA-mediated Cl- conductance through the GABA receptor + decreases glutamate-mediated cation conductance through 5HT receptors
43
Part one of ethanol mechanism: Increases GABA-mediated Cl- conductance through __________ receptors
GABA
44
Part two of ethanol mechanism: Decreases glutamate-mediated cation conductance through ________ receptors.
5HT
45
Effect of ethanol on 5HT receptors?
Decreases glutamate mediated cation conductance through 5HT receptors
46
Effect of ethanol on GABA receptors?
Increases GABA-mediated Cl- conductance through the GAB receptor
47
CNS depression of ethanol is:
dose-dependent
48
How much depression of the cerebellum does ethanol have? What is the effect of that?
180-400 mg depression | Loss of motor control
49
When ethanol depresses the cerebellum, it depresses which function?
Motor control
50
How much depression of the midbrain, spinal reflexes, medullary respiratory control does ethanol have?
350-600 mg of depression
51
Ethanol has 180-400 mg of depression in the:
cerebellum
52
Ethanol has 350-600 mg of depression in the:
midbrain, spinal reflexes, medullary respiratory control
53
Ethanol experiences rapid absorption in:
small intestines, stomach, and colon
54
Time from last drink of ethanol to maximal concentration in blood is:
30-90 minutes
55
What percentage of ethanol is oxidized?
90-98%
56
Metabolism of ethanol follows zero-oder kinetics at a rate of about __________.
7-10 grams/hour
57
How long does it take to metabolize 4 oz of Jack Daniels?
5 hours
58
What are two routes of oxygenation for ethanol? | Both systems form what?
1. NAD+-dependent alcohol dehydrogenase 2. NADPH-dependent microsomal ethanol oxidizing system Both systems form acetaldehyde, which is converted to acetate by aldehyde dehydrogenase.
59
Methanol works on what receptors?
Alcohol receptors
60
Methanol is metabolized to __________ by ___________. From there, the metabolite of methanol is metabolized to _____________ by _____________.
to formaldehyde by alcohol dehydrogenase | to formic acid by aldehyde dehydrogenase
61
What are some adverse side effects of methanol?
Metabolic acidosis | Blindness, seizures, coma, death
62
Those who have consumed methanol thinking that it would have the same effect as ethanol often come to the ER complaining of what?
Snow storm vision
63
What is flumazenil?
GABA antagonist
64
Name a GABA antagonist.
Flumazenil
65
Mechanism of action of flumazenil?
It competitively blocks the benzos at the GABA receptor, blocking the effects on GABA-mediated Cl- conductance and causing neuronal inhibition.
66
Flumazenil is what type of antagonist?
Competitive antagonist for benzodiazepines at the GABA receptor
67
For which two types of drugs is flumazenil effective for overdose reversal?
Benzodiazepines + NBRAS
68
Effect of flumazenil on alcohol overdose?
None
69
What is used to treat refractory hypersomnolence, a condition similar to narcolepsy?
Flumazenil
70
Mechanism of disulfiram?
Inhibitor of aldehyde dehydrogenase
71
Effect of disulfiram?
Treatment of alcohol abuse
72
Drug-based treatment for alcohol abuse?
Disulfiram
73
Mechanism of action of acamprosate?
Decreases glutamate neurotransmission (depressive effect)
74
What medication reduces relapse in detox patients?
Acamprosate
75
Effect of acamprosate?
Reduces relapse in detox patients
76
Class of baclofen?
GABA-B receptor agonist (depressive effect)
77
Effect of baclofen?
Decreases alcohol withdrawal symptoms, reduces anxiety and cravings?
78
What drug decreases alcohol withdrawal symptoms and reduces anxiety and cravings?
Baclofen
79
What is fomepizole?
Inhibitor of alcohol dehydrogenase
80
What does fomepizole inhibit?
Alcohol dehydrogenase
81
Fomepizole is useful for treating:
methanol overdose
82
Effective treatment for methanol overdose?
Fomepizole

BAHS 505 (9 decks)

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