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BRS2 Pharmacology and Therapeutics > Pharmacology of Depression - Core Drugs & Case Study > Flashcards

Pharmacology of Depression - Core Drugs & Case Study Flashcards

1
Q

What are the 5 core drugs for depression treatment

Learned about in Phase 1 medicine

A

Sertraline

Citalopram

Fluoxetine

Venlafaxine

Mirtazapine

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2
Q

In 2020 - sertraline was the 16th most commonly prescribed drug in West London area

What is the primary mechanism of action of sertraline?

A

Inhibition of sertraline re-uptake transporter

Results in accumulation of serotonin

Serotonin plays role in CNS in the regulation of mood, personality and wakefulness

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3
Q

What role does serotonin play in the CNS?

A

Regulation

  • Mood
  • Personality
  • Wakefulness
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4
Q

What is the drug target for Sertraline?

A

Serotonin transporter

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5
Q

What are the main side effects of taking sertraline?

A

GI side effects

  • Nausea
  • Diarrhoea

Sexual dysfunction

Anxiety

Insomnia

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6
Q

How does sertraline effect the dopamine transporter?

A

Mild inhibition of dopamine transporter

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7
Q

What does sertraline inhibit at high doses?

A

Partial inhibition of CYP2D6 at high doses (150mg)

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8
Q

How should one discontinue use of sertraline?

A

Must be gradually decreased on discontinuation

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9
Q

In 2020 - Citalopram was 27th most commonly prescribed drug in West London area

What is the primary mechanism of action of Citalopram?

A

Inhibition of serotonin reuptake

Results in an accumulation of serotonin which plays role in CNS in the regulation of mood, personality and wakefulness

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10
Q

What is the drug target of Citalopram?

A

Serotonin transporter

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11
Q

What are the main side effects of taking Citalopram?

A

GI side effects

  • Nausea
  • Diarrhoea

Sexual dysfunction

Anxiety

Insomnia

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12
Q

How might Citalopram affect muscarinic and histamine (H1) receptors?

A

Mild antagonism of muscarinic and histamine (H1) receptors

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13
Q

What metabolises Citalopram?

A

CYP2C19

  • An enzyme protein
  • Member of CYP2C subfamily of cytochrome P450
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14
Q

What must be done in the discontinuation of Citalopram?

A

Must be gradually decreased on discontinuation

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15
Q

What is CYP2C19?

A
  • An enzyme protein

- Member of CYP2C subfamily of cytochrome P450

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16
Q

What is CYP2D6?

A
  • An enzyme

- Part of cytochrome P450 family

17
Q

In 2020 - Fluoxetine was 68th most commonly prescribed drug in West London area

What is the primary mechanism of action of Fluoxetine?

A

Inhibition of serotonin re-uptake

Results in an accumulation of serotonin which plays role in CNS in the regulation of mood, personality and wakefulness

18
Q

What is the drug target of Fluoxetine?

A

Serotonin transporter

19
Q

What are the main side effects of taking Fluoxetine?

A

GI side effects

  • Nausea
  • Diarrhoea

Sexual dysfunction

Anxiety

Insomnia

20
Q

What effect can Fluoxetine have on 5HT2A and 5HT2C receptors?

A

Mild antagonism of these receptors

21
Q

What effect can Fluoxetine have on CYP2D6 and CYP2C19?

A

Complete inhibition of CYP2D6

Significant inhibition of CYP2C19 (caution with warfarin)

22
Q

In 2020 - Venlafaxine was 83rd most commonly prescribed drug in West London area

What was the primary mechanism of action of Venlafaxine?

A

Inhibition of serotonin re-uptake + norepinephrine re-uptake

Results in an accumulation of neurotransmitter in synapse

23
Q

What are the drug targets of Venlafaxine?

A

Serotonin transporter

Noradrenaline transporter

24
Q

What are the main side effects of taking Venlafaxine?

A

GI effects

  • Nausea
  • Diarrhoea

Sexual dysfunction

Anxiety

Insomnia

Hypertension (at higher doses)

25
Q

What must be done in the discontinuation of Venlafaxine?

A

Must gradually decrease Venlafaxine on discontinuation

26
Q

In 2020 - Mirtazapine was 30th most commonly prescribed drug in West London area.

What is the primary mechanism of action of Mirtazapine?

A

Antagonises presynaptic alpha-2-adrenergic receptors

This causes an increased release of serotonin and norepinephrine

Antagonises central 5HT2 receptors, which leaves 5HT1receptors unopposed —> antidepressant effects

27
Q

In 2020 - Mirtazapine was 30th most commonly prescribed drug in West London area.

What is the primary mechanism of action of Mirtazapine?

A

Antagonises presynaptic alpha-2-adrenergic receptors

  • This causes an increased release of serotonin and norepinephrine

Antagonises central 5HT2 receptors, which leaves 5HT1 receptors unopposed causing anti-depressant effects

28
Q

What are the drug targets of Mirtazapine?

A

Alpha-2 receptor

5-HT2 receptor

29
Q

What are the main side effects of taking Mirtazapine?

A

Weight gain
Sedation

Low probability of sexual dysfunction

May exacerbate REM sleep behaviour disorder

30
Q

What sleep behaviour disorder may be exacerbated by taking Mirtazapine?

A

May exacerbate REM sleep behaviour disorder

31
Q

What is the PHQ-9?

A

A 9 item questionnaire designed to screen for depression in primary care

32
Q

What are the 3 most commonly prescribed SSRIs?

A

Setraline
Citalopram
Fluoxetine

33
Q

For SSRIs:

What is the general

  1. Target?
  2. Location?
  3. Effect?
A
  1. 5-HTT
  2. Pre-synaptic neuron
  3. Increased serotonin availability = anti-depressant effect
34
Q

For SSRIs:

What is the general

  1. Target?
  2. Location?
  3. Effect?
A
  1. 5-HTT
  2. Pre-synaptic neuron (in brain, e.g. in hippocampus)
  3. Increased serotonin availability = anti-depressant effect
35
Q

A patient who is currently on sertraline is being switched to a new anti-depressant.

Why do you think the GP slowly weaned the patient off sertraline first before starting the new anti-depressant?

A

Caution is required when switching from one anti-depressant to another

Due to risk of drug interactions, serotonin syndrome, withdrawal symptoms, or relapse

Washout required before starting new drug

36
Q

Below is the binding affinity for some of the key drug targets for mirtazapine. The key effect of each receptor subtype is also given.

Mirtazapine drug targets & key effect

Affinity (highest —> lowest):

  1. Histamine (H1) receptor – sedation
  2. Alpha-2 receptor – Anti-depressant effect
  3. 5HT2 receptor – Anti-depressant effect
  4. 5HT3 receptor – Anti-emetic effect

Explain this information.
Consider selectivity, affinity and efficacy

A

H1-R:

  • Highest affinity for this receptor so will preferentially block H1-R at low doses
  • Most selective for this receptor
  • First thing patients will experience will be Mirtazapine’s sedating effects
  • Will experience sedation at lower doses than needed for anti-depressant and anti-emetic effect

A2-R & 5HT2-R

  • As you increase the dose, start experiencing anti-depressant effects
  • This reduces the sedative effect somewhat

5HT3-R

-

37
Q

Below is the binding affinity for some of the key drug targets for mirtazapine. The key effect of each receptor subtype is also given.

Mirtazapine drug targets & key effect

Affinity (highest —> lowest):

  1. Histamine (H1) receptor – sedation
  2. Alpha-2 receptor – Anti-depressant effect
  3. 5HT2 receptor – Anti-depressant effect
  4. 5HT3 receptor – Anti-emetic effect
  5. Explain how the effect felt by a patient on Mirtazapine would change with increasing dose, considering affinity and selectivity for each of these targets.
  6. Describe the efficacy of Mirtazapine at each of these targets
A
  1. H1-R:
  • Highest affinity for this receptor so will preferentially block H1-R at low doses
  • Most selective for this receptor
  • First thing patients will experience will be Mirtazapine’s sedating effects
  • Will experience sedation at lower doses than needed for anti-depressant and anti-emetic effect

A2-R & 5HT2-R

  • As you increase the dose, start experiencing anti-depressant effects
  • This reduces the sedative effect somewhat as antihistamine activity is offset by increased noradrenergic transmission

5HT3-R

  • Lowest affinity for this receptor
  • This will help with nausea + vomiting
  • This response will only be seen with very high doses
  1. EFFICACY - zero at each of these targets because Mirtazapine is an ANTAGONIST —-> (it has no effects/doesn’t produce a response, it blocks one instead)

BRS2 Pharmacology and Therapeutics (6 decks)

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