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Pharm Penultimate Exam > Sedative Hypnotics and Anxiolytics > Flashcards

Sedative Hypnotics and Anxiolytics Flashcards

1
Q

Anxiety brain circuitry is found where?

A

Amygdala

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2
Q

Difference between Sedation, Hypnosis, Anesthesia, and Coma

A

Sedation – Reduced Responsiveness
Hypnosis – Drug Induced Sleep
Anesthesia – Amnesia, analgesia, lost muscle tone
Coma – Unconsciousness for 6+ hours,no sleep cycles

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3
Q

GABA is produced from ______

A

Glutamate

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4
Q

What types of Channels does GABA act on

A

A - Ligand Gated Cl- Channel

B, C – GPCR

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5
Q

Diseases associated with GABA

A

Epilepsy, Muscle Spacticity, Addition/Alcoholism

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6
Q

Details of the GABA A receptor

A

Pentamer

Different subunit combinations possible (usually 2 alpha1, 2 beta2, and 1 gamma2)

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7
Q

Benzos prefer to bind…..

Z compounds prefer to bind…

A

Benzo – alpha 2, 3 5
Z – alpha 1 receptors
(This is why sedative/hypnotic drugs can work differently)

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8
Q

Effect of Cl- GABA channels on neuronal potential

A

Moves close to Cl- equilibrium potential (-70) decrasing likelihood of cell firing.

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9
Q

How does GABA A work normally?

A

Two GABA molecules bind the GABA A receptor, causing Cl- influx that hyperpolarizes the cell membrane

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10
Q

How do benzodiazepines interact with GABA A? How is this different from Z compounds?

A

They allosterically bind to a site distant from the GABA binding site, enhancing the activity of GABA at that site. Z compounds bind to the BZD site directly

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11
Q

Difference in the function of Benzos and Barbs

A

benzos increse frequency of openings

barbs increase the duration of opening

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12
Q

At high doses Barbiturates become…

A

GABA-mimetics

May act at AMPA glutamate receptors

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13
Q

What do molecules with inverse agonist action do? Exampe?

A

bind the BZD site and make it harder for GABA to open the channel

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14
Q

Example of a BZS site antagonist

A

Flumenazil

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15
Q

Important details about Midazolam

A

Rapid onset, fast recovery

Acute seizure control, pre-surgery anxiolysis, amnesia, sedation

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16
Q

Important details about Alprazolam

A

Mainly for panic, GAD

Rapid Acting, Moderate Duration

17
Q

Important details about flurazepam

A

Long duration
For insomnia
Next day sedation is possible, intermediate should maybe be an intermediate

18
Q

Benzos are broken down by…

A

CYP 3A4, 2C19. Grapefruit juice can interfere

19
Q

Benzo adverse effects

A 
Amnesia (in short acting)
Daytime sedation (in longer acting)
Resp/CV Depression
Withdrawl
Dependence
Potentiated by P450 inhibitors
20
Q

How to treat a Benzo overdose

A

Maintain airway, renal fxn
Positive inotropic drugs
Flumazenil

21
Q

Effects of Benzo withdrawl

A

Since receptors are downregulated, removal of Benzos will cause an increase in excitability, increasing lieklihood of patient seizures

22
Q

Benzo or Barb – who is easier to OD on

A

barb – stronger action at GABA-A, ability t open GABA channels

23
Q

How are Barbiturates commonly used? Rarely used?

A

Severely brain injured patients to induce coma to bring down intracranial pressure
Rarely – Seizures, Anesthesia

24
Q

The death penalty drug

A

Pentobarbital

25
Q

Important details about Buspirone

A

5HT1A partial agonist
Less sedation, withdrawl, abuse. Slow Onset
Used for GAD (NOT for panic)

26
Q

BZDs used as hypnosedatives

A

Triazolam (short)
Temazepam (medium)
Flurazepam (long)

27
Q

Z compounds used to treat insomnia

A

Zolpidem
Zeleplon
esZopiclone

28
Q

Z compounds are selective for ____ containing receptors

A

alpha1

29
Q

Important details about Ramelteon

A

MT1, MT2 agonist

acts on SCN to promote sleep

30
Q

Which sleep stage has K complexes + sleep spindles

A

Stage 2

31
Q

Effect of BZD/Barbs on sleep stages

A

Longer 2

Shorter 3/4/REM

32
Q

Effect of Z compounds on sleep stages

A

Longer (Or Same) 2

Shorter (or same) REM

Pharm Penultimate Exam (12 decks)

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