Pharmacology of depression

Question 1

What drugs are used to treat depression?

Answer 1

• Sertraline
• Citalopram
• Fluoxetine
• Venlafaxine
• Mirtazapine

Question 2

What is the drug target of sertraline?

Answer 2

Serotonin transporter

Question 3

What is the primary mechanism of action of sertraline?

Answer 3

Inhibition of serotonin reuptake -> accumulation of serotonin.
Serotonin in the CNS plays a role in the regulation of mood, personality, and wakefulness.

Question 4

What is the side effect of sertraline?

Answer 4

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia

Question 5

What else might sertraline bind to?

Answer 5

Mild inhibition of dopamine transporter



Question 6

What is the drug target for citalopram?

Answer 6

Serotonin transporter

Question 7

What is the primary mechanism of action for citalopram?

Answer 7

Inhibition of serotonin reuptake -> accumulation of serotonin.
Serotonin in the CNS plays a role in the regulation of mood, personality, and wakefulness.

Question 8

What are the side effects of citalopram?

Answer 8

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia

Question 9

What else might citalopram bind to?

Answer 9

Mild antagonism of muscarinic and histamine (H1) receptors

Question 10

What is the primary target of fluoxetine?

Answer 10

Serotonin transporter

Question 11

What is the mechanism of action of fluoxetine?

Answer 11

Inhibition of serotonin reuptake -> accumulation of serotonin. Serotonin in the central nervous system plays a role in the regulation of mood, personality, and wakefulness

Question 12

What are the side effects of fluoxetine?

Answer 12

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia

Question 13

What else might fluoxetine bind to?

Answer 13

Mild antagonism of 5HT2A and 5HT2C receptor

Question 14

Which drug must you be careful using fluoxetine with?

Answer 14

Significant inhibition of CYP2C19 (caution with warfarin).

Question 15

What is the drug target of venlafaxine?

Answer 15

Serotonin transporter

Noradrenaline transporter

Question 16

What is the primary mechanism of action for venlafaxine?

Answer 16

Venlafaxine is a more potent inhibitor of serotonin reuptake than norepinephrine reuptake.
Noradrenaline in the central nervous system is implicated in the regulation of emotions and cognition.

Question 17

What are the side effects of venlafaxine?

Answer 17

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia, hypertension (at higher doses)

Question 18

What is the drug target of mirtazapine?

Answer 18

Alpha-2 receptor
5-HT2 receptor



Question 19

What is the primary mechanism of action for mirtazapine?

Answer 19

Antagonises central presynaptic alpha-2-adrenergic receptors -> increased release of serotonin and norepinephrine.

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



Question 20

What are the side effects of mirtazapine?

Answer 20

Weight gain, sedation

Question 21

What effect can sertraline have on the dopamine transporter?

Answer 21

Mild inhibition of dopamine transporter



Question 22

How should sertraline be discontinued?

Answer 22

Must be gradually decreased on discontinuation. Partial inhibition of CYP2D6 at high doses (150 mg).

Question 23

What is the effect of citalopram on muscarinic & histamine (H1) receptors?

Answer 23

Mild antagonism

Question 24

How should citalopram be discontinued?

Answer 24

Must be gradually decreased on discontinuation. Metabolized by CYP2C19.

Question 25

Which enzymes does fluoxetine inhibit?

Answer 25

Complete inhibition of CYP2D6 and significant inhibition of CYP2C19 (caution with warfarin).

Question 26

How must venlafaxine be discontinued?

Answer 26

Must be gradually decreased on discontinuation

Question 27

What can mirtazapine exacerbate?

Answer 27

May exacerbate REM sleep behaviour disorder