Hypnotics Flashcards

1
Q

Name the 3 barbituates

A

phenobarbital
pentobarbital
thiopental

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2
Q

Where do barbs bind?

A

in the transmembranous portion of the GABA-A receptors

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3
Q

What is the mechanism of barbs?

A

prolong duration of binding of GABA to GABA-A receptors –> promotes inhibition of neurons

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4
Q

Which isoforms of GABA-A do barbs bind?

A

all of them

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5
Q

What is the elimination half life of barbs from the blood?

A

4-5 days

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6
Q

How do you help barbs be excreted in the urine?

A

give bicarb

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7
Q

Why give bicarb in barb overdose?

A

barbs are more readily absorbed back into the blood when the blood is more acidic

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8
Q

Barbs cause prolonged sleep in which phase?

A

2

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9
Q

Barbs prolong/decrease REM

A

decrease

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10
Q

Barbs prolong/decrease stage 4

A

decrease

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11
Q

Fastest barb

A

thiopental

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12
Q

What is the toxic effect of barbs at high doses?

A

affect electrical conductivity in ALL tissues

paralysis –> arrest –> death

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13
Q

Benzos

A

diazepam
lorazepam
triazolam
alprazolam

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14
Q

Mechanism of benzos

A

bind GABA-A on extracellular surface

increase frequency of Cl- channel opening events

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15
Q

Barbs and liver

A

barbs sped up their own metabolism as well as metabolism of other drugs

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16
Q

Barbs: pharmacokinetic or pharmacodynamic tolerance?

A

both

17
Q

Benzos: pharmacokinetic or pharmacodynamic tolerance?

A

primarily pharmacodynamic

downregulation of GABA-A receptors

18
Q

Benzos cause this great effect

A

anterograde amnesia

19
Q

Flumazenil function/mechanism

A

reverse benzo effect

binding site agonist

20
Q

This drug is used to reverse the effects of benzos

A

flumazenil

21
Q

Zolpidem
Zaleplon
Eszoplicone

A

non-benzodiazepine benzodiazepine agonists
Ezzzzz
z’s in all the names

22
Q

What is so special about the zzzz drugs?

A

the bind a subset of GABA-A receptors
better sleep
ware off more quickly

23
Q

Buspirone mechanism

A

partial 5-HT-1A agonst

24
Q

Buspirone use

A

anxiety

25
Q

Ramelteon mechanism

A

melatonin agonist