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Pharmacology Y2 > Depression > Flashcards

Depression Flashcards

1
Q

Describe the mechanism of action of sertraline (SSRIs)

A
  • Inhibition of serotonin re-uptake results in an accumulation of serotonin.
  • mild inhibition of dopamine transporter
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2
Q

What is the target of sertraline?

A

Serotonin reuptake transporter in pre-synpatic neurones

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3
Q

What are the main side effects of sertraline?

A
  • GI effects (nausea, diarrhoea)
  • sexual dysfunction
  • anxiety
  • insomnia
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4
Q

Why do anti-depressants need to gradually be decreased on discontinuation?

A
  • to reduce withdrawal symptoms
  • to prevent relapse of depression
  • to reduce risk of drug interactions (liver enzyme metabolism is affected by many drugs)
  • to prevent serotonin syndrome
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5
Q

What is serotonin syndrome?

A

Too much serotonin due to multiple anti-depressants . It can cause….

  • confusion
  • tachycardia
  • loss of muscle co-ordination
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6
Q

What is the mechanism of action for Citalopram (SSRI)?

A

Inhibition of serotonin reuptake results in an accumulation of serotonin

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7
Q

What is Citalopram’s target?

A

Serotonin transporter on presynaptic neurones

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8
Q

What are some of the side effects of using Citalopram?

A
  • GI effects (nausea, diarrhoea)
  • sexual dysfunction
  • anxiety
  • insomnia
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9
Q

What other receptors are affected by Citalopram and how are they affected?

A
  • muscarinic receptors
  • histamine (H1) receptors
    MILD ANTAGONIST (inhibition of function)
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10
Q

What is the Fluoxetine’s mechanism of action (SSRI)?

A

Inhibition of serotonin reuptake results in an accumulation of serotonin.

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11
Q

What is Fluoxetine’s target?

A

Serotonin transporter on presynaptic neurones

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12
Q

What are some of the side effects of using Fluoxetine?

A
  • GI effects (nausea, diarrhoea)
  • sexual dysfunction
  • anxiety
  • insomnia
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13
Q

What other receptors are affected by Fluoxetine and how are they affected?

A

5-HT2A receptors
5-HT2C receptors
MILD ANTAGONIST (inhibition of function)

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14
Q

What enzymes are affected by Fluoxetine and how are they affected?

A
  • Complete inhibition of CYP2D6
  • Significant inhibition of CYP2C19
    BOTH ARE P450 enzymes.
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15
Q

Describe the mechanism of action of Venlafaxine (SNRI).

A

Serotonin + norepinephrine re-uptake inhibitor

more so serotonin

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16
Q

What does Venlafaxine target?

A
  • Serotonin re-uptake transporters
  • Noradrenaline re-uptake transporters
    Both of these transporters are on the pre-synaptic neurones.
17
Q

What are the side effects of using Venlafaxine?

A
  • GI effects (nausea, diarrhoea)
  • sexual dysfunction
  • anxiety
  • insomnia
  • hypertension (at higher doses)
18
Q

What are the contra-indications of Venlafaxine?

A

Uncontrolled hypertension

This is because Venlafaxine increases adrenaline, which mediates (increases) BP and HR.

19
Q

What is the mechanism of action of Mirtazapine?

A
  • Antagonises (inhibits) central presynaptic alpha-2-adrenergic receptors, which causes an increased release of serotonin and norepinephrine.
  • Antagonises central 5-HT2 receptors, which leaves 5-HT1 receptors (serotonin binds to these receptors) unopposed, causing anti-depressant effects.
  • Antagonises H1 receptors which causes sedation + increased duration of sleep
20
Q

What receptors does Mirtazapine target?

A
  • a-2 adrenergic receptors
  • 5-HT2 receptors
  • 5-HT3 receptors
  • H1 receptors
21
Q

What are some of the side effects of Mirtazapine?

A
  • Weight gain
  • Sedation
  • may exacerbate REM sleep behaviours
  • sexual dysfunction is RARE
22
Q

Mirtazapine has low selectivity (but it’s still effective). Describe its affinity to different target receptors at low doses.

A 
HIGHEST AFFINITY
1. H1 receptor (sedation)
2. Alpha-2 receptor (Anti-depressant)
3. 5-HT2 receptor (Anti-depressant)
4. 5-HT3 receptor (anti-emetic)
LOWEST AFFINITY
23
Q

What happens to the affinity of Mirtazapine to its receptors at higher doses?

A

Antihistamine effect is offset by increased noradrenergic transmission
(anti-depressant effect > sedative effect)

24
Q

What is the role of serotonin in the CNS?

A

Involved in the regulation of mood, personality, and wakefulness.

25
Q

What is the role of norepinephrine in the CNS?

A

Involved in the regulation of emotions and cognition.

Pharmacology Y2 (9 decks)

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