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PHAR2005 > Anxiolytics and Hypnotics > Flashcards

Anxiolytics and Hypnotics Flashcards

1
Q

How many subunits form a GABAAR and what is their arrangement?

A

5

A2B2Y

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2
Q

Where does GABA bind to GABAAR?

A

Between A and B (two sites)

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3
Q

What is the effect of GABA binding to GABAAR?

A

Opens Cl- channel

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4
Q

Where do benzodiazepines bind to GABAAR?

A

Between A and Y

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5
Q

What is the effect of benzodiazepine binding to GABAAR?

A

Increased Cl- channel opening frequency

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6
Q

Do benzodiazepines open Cl- channel without simultaneous GABA binding to GABAAR?

A

No

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7
Q

What is the effect of B-carboline binding to GABAAR benzodiazepine binding site?

A

Prevents GABA binding from opening Cl- channel

Closes channel if GABA already bound

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8
Q

What are the effects of B-carboline?

A

Anxiety

Insomnia

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9
Q

Name a benzodiazepine antagonist

A

Flumazenil

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10
Q

What are the effects of benzodiazepines?

A 
Sedation
Anxiolysis
Hypnosis
Muscle relaxation
Anti-convulsant
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11
Q

What are uses of short-acting benzodiazepines?

A

Amnesics

Hyponotics

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12
Q

What are uses of long-acting benzodiazepines?

A

Anxiolytics

Anti-convulsants

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13
Q

Where do Z drugs act?

A

Benzodiazepine binding site on GABAARs

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14
Q

What are the effects of Z drugs?

A

Anxiolysis
Sedation
Hypnosis

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15
Q

What are the side effects of benzodiazepines?

A

Confusion
Drowsiness
Muscle incoordination

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16
Q

What are the factors affecting benzodiazepine tolerance?

A

Receptor occupancy
Dose duration
Number of surface receptors

17
Q

What are the effects of benzodiazepine dependence?

A

Anxiety
Tremor
Appetite loss
Insomnia

18
Q

What are the names of the natural anxiolytics in the brain?

A

Neurosteroids (e.g. allopregnanolone)
Diazepam binding inhibitor protein (e.g. endozepine)
Serotonergic system

19
Q

What is the effect of 5HT1ARs?

A

Inhibitory

20
Q

What is the effect of buspirone?

A

5HT1AR partial agonist
Acute: binds presynaptic 5HT1ARs - less presynaptic 5HT release - less inhibition of postsynaptic neuron
Chronic: desensitises presynaptic 5HT1ARs - more presynaptic 5HT release - more inhibition of postsynaptic neuron

21
Q

Name a B-adrenoceptor antagonist and its use

A

Propranolol

Acts on PNS to treat physical signs of anxiety

22
Q

Name 3 barbiturates and their uses

A

Thiopental - anaesthesia
Secobarbital - insomnia
Phenobarbitone - epilepsy

23
Q

What are the problems with barbiturates?

A

Cause respiratory depression

No antidote

24
Q

How do barbiturates act on GABAARs?

A

Binding with GABA: channel open for longer - potentiation

Barbiturate binding alone: directly opens channel

PHAR2005 (24 decks)

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