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L2 pharmacology > CNS 1 - Anxiolytics and Hypnotics > Flashcards

CNS 1 - Anxiolytics and Hypnotics Flashcards

1
Q

What are hypnotics used to treat?

A

Sleep disorders

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2
Q

What happens in the body during a fear response? (4)

A
  • Autonomic nervous system activation
  • Corticosteroid secretion (cortisol)
  • Increased alertness
  • Defensive behaviours
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3
Q

What is anxiety?

A

Anticipatory fear response which is often independent of external events

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4
Q

What are some types of anxiety observed in humans? (4)

A
  • Panic disorder
  • Social anxiety disorder
  • PTSD
  • Generalised anxiety
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5
Q

What animal models are used for studying anxiety? (3)

A
  • Elevated Plus Maze/Cross Test
  • Light/Dark Box
  • Conflict Test
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6
Q

How does the Elevated Plus Maze/Cross Test work?

A
  • Barrier on one side of the cross and open on the other side
  • Rodent in the middle has the choice to walk in the open or enclosed region
  • Usually rodents are afraid of the open side
  • After treatment with anxiolytics, the rodent shows no preference between open/enclosed regions of the cross
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7
Q

How does the Light/Dark Box test work?

A
  • Half the box is light, other half is dark
  • Usually the rodent will prefer to hide in the dark side
  • After treatment with anxiolytics, the rodent shows no preference between the light/dark side
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8
Q

How do Conflict tests work?

A
  • Associate a treat with a sound and a mild electric shock
  • Anxiolytics cause the rodents to ignore the sound and shock and go for the treat anyway
  • Rodents still show the fear response when treated with analgesics/antidepressants which shows that the fear system is distinct from these
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9
Q

What were the first drugs used as anxiolytics?

A

Benzodiazepines

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10
Q

What is the target of benzodiazepines?

A

GABAa receptors

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11
Q

What kind of receptor is GABAa?

A

Ligand gated ion channel (ionotropic)

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12
Q

What is GABA?

A

Main inhibitory neurotransmitter in the CNS

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13
Q

Which drugs can bind to GABAa receptors and what is their effect? (3)

A
  • Benzodiazepines
  • Barbiturates
  • Ethanol
    All increase the activity of GABAa receptors therefore increasing inhibition in the CNS
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14
Q

What is the structure of GABAa receptors? (3)

A
  • 5 subunits (pentameric)
  • 2 alpha, 2 beta and a something else (different combinations of subunit determine the function)
  • 2 GABA binding sites
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15
Q

How many GABA binding sites are there on GABAa receptors?

A
  • 2
  • Both need to be occupied for the channel to open
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16
Q

Where do benzodiazepines bind to GABAa receptors?

A

Benzodiazepine binding site is between the alpha and gamma subunit

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17
Q

Where does GABA bind to GABAa receptors?

A

GABA binding sites are between the alpha and beta subunits

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18
Q

Which ion are GABAa receptors selective for?

A

Chloride (i.e. inhibitory because the membrane potential becomes more negative)

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19
Q

What is an orthosteric binding site?

A

Active site where the normal agonist for a receptor binds

20
Q

What binds to the orthosteric binding site on GABAa receptors? (4)

A
  • GABA
  • Muscimol (agonist)
  • Bicuculline (competitive antagonist, blocks the binding site)
  • Picrotoxin (non-competitive antagonist, blocks the pore)
21
Q

What is an allosteric binding site?

A
  • Where allosteric modulators bind
  • Separate from the main orthosteric site
22
Q

What symptoms do bicuculline and picrotoxin cause?

A

Seizures (main one) and anxiety

23
Q

What is an allosteric modulator?

A

A substance that modifies the behaviour of the receptor when an agonist is bound to the orthosteric binding site

24
Q

What does a competitive antagonist to the allosteric site do?

A

Binds to the allosteric site and prevents the allosteric agonist from modifying the receptors’ behaviour

25
Q

What binds to the allosteric binding site on GABAa receptors? (2)

A
  • Benzodiazepines e.g. diazepam (positive allosteric modulator)
  • Flumazenil (competitive antagonist for the benzodiazepine allosteric site)
26
Q

What is flumazenil used for?

A

Treating overdoses of benzodiazepines

27
Q

Which alpha subunits are benzodiazepine sensitive? (4)

A

Alpha 1, 2, 3 and 5

28
Q

What are the physiological effects of benzodiazepines? (5)

A
  • Anxiolytic
  • Hypnosis (sleepy)
  • Anterograde amnesia (rohypnol)
  • Anti-convulsant
  • Reduction of muscle tone (relaxation)
29
Q

Which alpha subunit is in GABAa receptors which are involved in anxiolysis?

A

Alpha 2

30
Q

How do benzodiazepines work?

A
  • Increases the frequency of opening of GABAa receptors in the presence of GABA binding (positive allosteric modulator)
  • Binding of benzodiazepines to the allosteric site on GABAa increases the receptors’ affinity for GABA
31
Q

What is a negative allosteric modulator for GABAa receptors? (2)

A
  • Beta carbolines
  • Convulsions as side effect (reduced activity of GABA)
32
Q

Why does diazepam have such long lasting action?

A

Produces a metabolite when broken down in the body which has activity as a positive allosteric modulator so prolongs the activity of the drug

33
Q

What is diazepam also known as?

A

Valium

34
Q

What are the adverse side effects of benzodiazepines? (4)

A
  • Misuse (taking too much)
  • Tolerance
  • Physical dependence with withdrawal symptoms
  • Fatal in overdose when combined with other CNS depressants
35
Q

Why are benzodiazepines safe when taken on their own?

A
  • Benzodiazepines only increase the activity of GABAergic neurones that are already active (GABA needs to be bound in order for benzodiazepines to have an effect)
  • This means that overdose of this alone is not fatal, just fall asleep
36
Q

What are barbiturates used for and why?

A
  • Euthanasia
  • As you increase the concentration they start acting as an orthosteric agonist (unlike benzodiazepines) so increase all GABAergic activity in the CNS leading to coma and death
37
Q

What happens when benzodiazepines are taken with alcohol?

A

The depressive effects are additive so overdose can be fatal

38
Q

Which drugs are used now to treat anxiety? (5)

A
  • Propranolol
  • Antidepressants (SSRIs e.g. sertraline)
  • Buspirone
  • Antipsychotics
  • Antiepileptics
39
Q

What kind of drug is propranolol?

A

Beta blocker

40
Q

What kind of drug is sertraline?

A

SSRI

41
Q

What kind of drug is buspirone?

A

5HT1A partial agonist

42
Q

Which drugs are used to treat insomnia? (4)

A
  • Benzodiazepines e.g. lorazepam
  • Melatonin receptor agonists
  • Orexin receptor antagonists
  • Anti-histamines
43
Q

How do anti-histamines treat insomnia? (2)

A
  • H1 receptors in the brain are involved in alertness
  • H1 receptor antagonists help with sleep
44
Q

What is an inverse agonist?

A

Binds to a receptor and stabilises it in a way which reduces constitutive activity

45
Q

What is constitutive activity?

A

When a channel sometimes spontaneously opens in the absence of an agonist

L2 pharmacology (9 decks)

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