Depression Pharmacology Flashcards

1
Q

What are the drugs for depression? (5)

A

Sertraline
Citalopram
fluoxetine
venlafaxine
mirtazapine

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2
Q

What is the drug target of sertraline?

A

Serotonin transporter

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3
Q

What is the mechanism of action of sertraline?

A

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

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4
Q

What are the main side effects of sertraline?

A

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

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5
Q

What does sertraline also have mild inhibition of?

A

Mild inhibition of dopamine transporter

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6
Q

How should you discontinue sertraline?

A

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

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7
Q

What is the drug target of citalopram?

A

Serotonin transporter

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8
Q

What is the mechanism of action of citalopram?

A

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

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9
Q

What are the main side effects of citalopram?

A

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

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10
Q

What mild antagonism does citalopram also have?

A

Mild antagonism of muscarinic and histamine (H1) receptors

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11
Q

How do you stop giving citalopram and what metabolises it?

A

Must be gradually decreased on discontinuation. Metabolized by CYP2C19.

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12
Q

What is the drug target of fluoxetine?

A

Serotonin transporter

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13
Q

What is the mechanism of action of fluoxetine?

A

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

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14
Q

What are the main side effects of fluoxetine?

A

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

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15
Q

What is fluoxetine also a mild antagonist of?

A

Mild antagonism of 5HT2A and 5HT2C receptors

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16
Q

What does fluoxetine inhibit?

A

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

17
Q

What is the drug target of venlafaxine?

A

Serotonin transporter

Noradrenaline transporter

18
Q

What is the mechanism of action for venlafaxine?

A

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.

19
Q

What are the main side effects of venlafaxine?

A

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

20
Q

What must you do on discontinuation of venlafaxine?

A

gradual discontinuation

21
Q

What is the drug target for mirtazapine?

A

Alpha-2 receptor

5-HT2 receptor

22
Q

What is the mechanism of action of mirtazapine?

A

Antagonises central presynaptic alpha-2-adrenergic receptors, which causes an increased release of serotonin and norepinephrine.
Antagonises central 5HT2 receptors, which leaves 5HT1 receptors unopposed causing anti-depressant effects.

23
Q

What are the side effects of mirtazapine?

A

Weight gain, sedation

24
Q

What is a possible side effect of mirtazapine?

A

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

25
Q

What questionnaire can be used to help diagnose depression?

A

PATIENT HEALTH QUESTIONNAIRE-9 (PHQ-9)

26
Q

What are the types of depression?

A

mild
moderate
moderately severe
severe

27
Q
A

Alleviate depressive symptoms: Improve his mood
Help with sleep difficulties
Improve his self-esteem
Improve his ability to think clearly

28
Q

What are the 3 most commonly prescribed SSRIs?

A

Sertraline
Citalopram
Fluoxetine

29
Q

What is the mechanism of action of SSRIs?

A

Selective serotonin reuptake inhibitors (SSRIs)

30
Q

What should you be careful of with citalopram (and erythromycin)?

A

they both prolong the QT interval

most manufacturers advise asvoiding the use of 2 or more drugs that are associated with QT prolongation

31
Q

What are risk factors for predisposed QT interval? (4)

A

increasing age
female sex
cardiac disease
and some metabolic disturbances (notable hypokalaemia)

32
Q
A

Dose increase doesn’t really benefit depression improvement, but does worsen side effects
the plateau is due to all the 5-HTs already being occupied

33
Q
A

very basic wise, there isn’t enough receptors- like they’re fully blocked so can’t be reuptaken but cant speed up the uptake

34
Q

What is the drug target type for venlafaxine and mirtazapine, and what are they?

A
35
Q

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

A

Caution is required when switching from one antidepressant to another due to the risk of drug interactions, serotonin syndrome, withdrawal symptoms, or relapse.
Washout required before starting new drug

36
Q
A

Adrenergic effects of venlafaxine appear with doses administrated more than 150 mg/day, apparent increase in blood pressure and increased heart rate are observed when the daily dose exceeds 300 mg

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

37
Q

What are the drug targets of mirtazapine, what are tis effects and what does it have highest affinity for (highest to lowest)?

A
38
Q

Which effect would be induced first at low dose of mirtazapine?

A