Pharm - Depression

Question 1

What are the main drugs used for depression

Answer 1

Sertraline
Citalopram
Fluoxetine
Venlafaxine
Mitrazapine

Question 2

What is the primary mechanism of action for Sertraline

Answer 2

Inhibits serotonin reuptake transporters in the presynaptic neurones, mainly in the hippocampus. This therefore reduces uptake and thus increases accumulation of serotonin. Serotonin in the CNS plays a role in regulation of mood, personality and wakefulness

Question 3

What is the primary mechanism of action for Citalopram

Answer 3

Inhibits serotonin reuptake transporters in the presynaptic neurones, mainly in the hippocampus. This therefore reduces uptake and thus increases accumulation of serotonin. Serotonin in the CNS plays a role in regulation of mood, personality and wakefulness

Question 4

What is the primary mechanism of action for Fluoxetine

Answer 4

Inhibits serotonin reuptake transporters in the presynaptic neurones, mainly in the hippocampus. This therefore reduces uptake and thus increases accumulation of serotonin. Serotonin in the CNS plays a role in regulation of mood, personality and wakefulness

Question 5

What is the primary mechanism of action for Venlafaxine

Answer 5

More potent inhibitor of serotonin reuptake than norepinephrine reuptake. Norepinephrine in the CNS is implicated in the regulation of emotions and cognition. (Inhibits reuptake of both Sertonin and Norepinephrine)

Question 6

What is the primary mechanism of action for Mirtazapine

Answer 6

Antagonises central presynaptic alpha-2 adrenergic receptors, which cause increased release of serotonin and norepinephrine.

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

Question 7

What is the drug target for Sertraline

Answer 7

Serotonin transporter

Question 8

What is the drug target for Citalopram

Answer 8

Serotonin transporter

Question 9

What is the drug target for Fluoxetine

Answer 9

Serotonin transporter

Question 10

What is the drug target for Venlafaxine

Answer 10

Serotonin transporter
Norepinephrine transporter

Question 11

What is the drug target for Mirtazapine

Answer 11

Alpha-2 receptor
5-HT2 receptor

Question 12

What are the main side effects for Sertraline

Answer 12

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

Question 13

What are the main side effects for Citalopram

Answer 13

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

Question 14

What are the main side effects for Fluoxetine

Answer 14

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

Question 15

What are the main side effects for Venlafaxine

Answer 15

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

Question 16

What are the main side effects for Mirtazapine

Answer 16

Weight gain, sedation

Question 17

What else should we know about Sertraline

Answer 17

Mild inhibition of dopamine transporter.

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

Question 18

What else should we know about Citalopram

Answer 18

Mild antagonist of muscarinic and histamine H1 receptors

Must be gradually decreased on discontinuation

Metabolised by CYP2C19

Question 19

What else should we know about Fluoxetine

Answer 19

Mild antagonism of 5Ht2A and 5HT2C receptors

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

Question 20

What else should we know about Venlafaxine

Answer 20

Must be gradually decreased on discontinuation

Question 21

What else should we know about Mirtazapine

Answer 21

Low probability of sexual dysfunction. May exacerbate REM sleep behaviour disorder

Question 22

Where do SSRIs act

Answer 22

Serotonin reuptake transporter in presynaptic neurone, largely in the hippocampus

Question 23

Why do we not give citalopram to people who may be taking erythromycin

Answer 23

Prolongs QT interval

Question 24

Why must we slowly be weaned off one antidepressant before starting a new one

Answer 24

Due to the risk of drug interactions, serotonin syndrome, withdrawal symptoms, or relapse - therefore washout is required

Question 25

Which antidepressant is best for someone with sleeping problems

Answer 25

Mirtazapine - modestly suppresses REM sleep whilst still having a beneficial impact on sleep continuity and duration due to its anti-histaminergic effects.