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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
Q

Which NBRA binds all three benzo receptor types?

A

Eszopiclone

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26
Q

Half-life of Eszopiclone?

A

6 hours

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27
Q

Active metabolite of Eszopiclone?

A

None

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28
Q

Mechanism of Eszopiclone?

A

Binds to all subtypes of benzo receptors to enhance GABA-mediated Cl- conductance and neuronal inhibition

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29
Q

Which NBRA is appropriate for chronic treatment of sleep disorders?

A

Eszopiclone

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30
Q

Antagonist of Eszopiclone?

A

Flumazenil

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31
Q

Mechanism of NBRAs?

A

Binds to benzo receptors to enhance GABA-mediated Cl- conductance and neuronal inhibition

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32
Q

Class of belsomra?

A

Orexin receptor antagonist

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33
Q

Effect of belsomra?

A

Causes wakefulness

34
Q

Belsomra acts on which receptors?

A

Highly selective antagonist for orexin receptors

35
Q

Belsomra is a highly-selective ___________ for orexin receptors.

A

Antagonist

36
Q

Which two drugs act on alcohol receptors?

A

Ethanol and methanol

37
Q

Ethanol works on which receptors?

A

Alcohol receptors

38
Q

What parts of the brain are most sensitive to ethanol?

A

Polysynaptic reticular activating system and the cerebral cortex

39
Q

Effect of ethanol on the lipid bilayer of the plasma membrane? Result?

A

Dissolves the lipid bilayer of plasma membrane reduces membrane viscosity and disrupts protein function

40
Q

Effect of ethanol on membrane viscosity?

A

Reduces viscosity

41
Q

Effect of ethanol on proteins?

A

Disrupts protein function

42
Q

Mechanism of action of ethanol?

A

Increases GABA-mediated Cl- conductance through the GABA receptor + decreases glutamate-mediated cation conductance through 5HT receptors

43
Q

Part one of ethanol mechanism: Increases GABA-mediated Cl- conductance through __________ receptors

A

GABA

44
Q

Part two of ethanol mechanism: Decreases glutamate-mediated cation conductance through ________ receptors.

A

5HT

45
Q

Effect of ethanol on 5HT receptors?

A

Decreases glutamate mediated cation conductance through 5HT receptors

46
Q

Effect of ethanol on GABA receptors?

A

Increases GABA-mediated Cl- conductance through the GAB receptor

47
Q

CNS depression of ethanol is:

A

dose-dependent

48
Q

How much depression of the cerebellum does ethanol have? What is the effect of that?

A

180-400 mg depression

Loss of motor control

49
Q

When ethanol depresses the cerebellum, it depresses which function?

A

Motor control

50
Q

How much depression of the midbrain, spinal reflexes, medullary respiratory control does ethanol have?

A

350-600 mg of depression

51
Q

Ethanol has 180-400 mg of depression in the:

A

cerebellum

52
Q

Ethanol has 350-600 mg of depression in the:

A

midbrain, spinal reflexes, medullary respiratory control

53
Q

Ethanol experiences rapid absorption in:

A

small intestines, stomach, and colon

54
Q

Time from last drink of ethanol to maximal concentration in blood is:

A

30-90 minutes

55
Q

What percentage of ethanol is oxidized?

A

90-98%

56
Q

Metabolism of ethanol follows zero-oder kinetics at a rate of about __________.

A

7-10 grams/hour

57
Q

How long does it take to metabolize 4 oz of Jack Daniels?

A

5 hours

58
Q

What are two routes of oxygenation for ethanol?

Both systems form what?

A
  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
Q

Methanol works on what receptors?

A

Alcohol receptors

60
Q

Methanol is metabolized to __________ by ___________. From there, the metabolite of methanol is metabolized to _____________ by _____________.

A

to formaldehyde by alcohol dehydrogenase

to formic acid by aldehyde dehydrogenase

61
Q

What are some adverse side effects of methanol?

A

Metabolic acidosis

Blindness, seizures, coma, death

62
Q

Those who have consumed methanol thinking that it would have the same effect as ethanol often come to the ER complaining of what?

A

Snow storm vision

63
Q

What is flumazenil?

A

GABA antagonist

64
Q

Name a GABA antagonist.

A

Flumazenil

65
Q

Mechanism of action of flumazenil?

A

It competitively blocks the benzos at the GABA receptor, blocking the effects on GABA-mediated Cl- conductance and causing neuronal inhibition.

66
Q

Flumazenil is what type of antagonist?

A

Competitive antagonist for benzodiazepines at the GABA receptor

67
Q

For which two types of drugs is flumazenil effective for overdose reversal?

A

Benzodiazepines + NBRAS

68
Q

Effect of flumazenil on alcohol overdose?

A

None

69
Q

What is used to treat refractory hypersomnolence, a condition similar to narcolepsy?

A

Flumazenil

70
Q

Mechanism of disulfiram?

A

Inhibitor of aldehyde dehydrogenase

71
Q

Effect of disulfiram?

A

Treatment of alcohol abuse

72
Q

Drug-based treatment for alcohol abuse?

A

Disulfiram

73
Q

Mechanism of action of acamprosate?

A

Decreases glutamate neurotransmission (depressive effect)

74
Q

What medication reduces relapse in detox patients?

A

Acamprosate

75
Q

Effect of acamprosate?

A

Reduces relapse in detox patients

76
Q

Class of baclofen?

A

GABA-B receptor agonist (depressive effect)

77
Q

Effect of baclofen?

A

Decreases alcohol withdrawal symptoms, reduces anxiety and cravings?

78
Q

What drug decreases alcohol withdrawal symptoms and reduces anxiety and cravings?

A

Baclofen

79
Q

What is fomepizole?

A

Inhibitor of alcohol dehydrogenase

80
Q

What does fomepizole inhibit?

A

Alcohol dehydrogenase

81
Q

Fomepizole is useful for treating:

A

methanol overdose

82
Q

Effective treatment for methanol overdose?

A

Fomepizole

BAHS 505 (9 decks)

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