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Cology 2 Exam 1 > Benzos > Flashcards

Benzos Flashcards

1
Q

What alpha subunit(s) are required for sedative actions?

A

alpha-1

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2
Q

What alpha subunit(s) are required for anxiolytic actions?

A

Alpha-2 and 3

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3
Q

What alpha subunit(s) are required for anticonvulsant actions?

A

Alpha-2 and 3

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4
Q

What alpha subunit(s) are required for amnestic action?

A

Alpha-5

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5
Q

What subunit does BDZ bind to?

A

Alpha

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6
Q

What subunit does GABA bind to?

A

Beta

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7
Q

What subunits are required for BDZ action?

A

gamma-2, beta, and certain alpha subunits

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8
Q

What is flumazenil?

A

Flumazenil is a BDZ competitive antagonist; it binds the alpha subunit (BDZ binding site), shifting the response curve to the right (requires higher BDZ conc for effect)

NO EFFECT in healthy individuals - just people taking BDZ’s

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9
Q

What is picrotoxin?

A

A BDZ noncompetitive antagonist; it blocks the channel so GABA can’t go through. BDZ can still bind

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10
Q

What is bicuculline?

A

BDZ noncompetitive antagonist
Binds the GABA receptor
BDZ can still bind and increase affinity for GABA but GABA can’t bind so no effect!

NONCOMPETITIVE for BDZ
COMPETITIVE for GABA

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11
Q

What CNS effect(s) mediates the anxiolytic effect of BDZ’s?

A

Regulate firing of raphe nuclei neurons

Inhibits firing of the amygdala neurons

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12
Q

What CNS effect(s) mediates the amnestic effect of BDZ’s?

A

Inhibition of hippocampal LTP

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13
Q

What CNS effect(s) mediates the muscle relaxant effect of BDZ’s?

A

Enhanced presynaptic inhibition of the spinal cord

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14
Q

What CNS effect(s) mediates the anticonvulsant effect of BDZ’s?

A

Inhibit firing of epileptic foci

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15
Q

How do BDZ’s affect sleep?

A

Decrease sleep latency (time to fall asleep) and increase sleep time

They increase stage 2 sleep

DECREASE stage 1, 3, 4, and REM sleep (thought to mediate aggression - less REM sleep)

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16
Q

What effect do BDZ’s have on ion channels?

A

Increases frequency of chloride channel opening

Doesn’t increase duration of channel opening

17
Q

What drugs inhibit metabolism of BDZ? What does this do to BDZ levels?

A

Cimetidine, Disulfiram, and oral contraceptives increase BDZ levels by inhibiting metabolism

18
Q

What drugs increase metabolism of BDZ? What does this do to BDZ levels?

A

Chronic ethanol, isoniazid, and phenytoin decrease BDZ levels by increasing metabolism (inducing CYP3A4)

GRAPEFRUIT JUICE also induces CYP3A4

19
Q

Describe flumazenil

A

Nonselective antagonist (binds alpha subunit, blocks BDZ from binding)
No effect alone (no effect in non-BDZ users)
Used for BDZ overdose (blocks BDZ from binding)
Extensive first-pass metabolism; IV only
t1/2 is 1hr

20
Q

Is BDZ tolerance pharmacokinetic or pharmacodynamic? What does this mean?

A

Pharmacodynamic, meaning the body responds differently to the drug. There isn’t enzyme upregulation, there is subunit composition change to decrease responsiveness

CROSS-tolerance occurs to other sedatives

21
Q

If someone is tolerant to BDZ, can they take other sedatives?

A

There is cross-tolerance to other sedatives because the tolerance to BDZ is due to pharmacodynamics

22
Q

Tolerance to BDZ’s depends on the effect. Which effects show tolerance?

A

More to sedation
Less to anticonvulsant
Very little to anxiolysis

23
Q

Tolerance to sedation requires what subunit

A

Alpha-5

24
Q

How do you treat dependence of BDZ?

A

Switch to longer acting BDZ
Decrease dose over 10-21 days
or
Substitute with Zolpidem

25
Q

Physical dependence is due to altered GABA-A receptor subunit composition. What happens?

A

Less alpha-1 and gamma-2 subunits

26
Q

What effect do BDZ’s have on dopamine activity?

A

Very little effect on mesolimbic dopamine activity, so there’s very little abuse liability

Cology 2 Exam 1 (14 decks)

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