Pharma - Depression Flashcards

1
Q

What is the primary 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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2
Q

What is the drug target for sertraline?

A

Serotonin transporter

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3
Q

What are the main side effects of the sertraline?

A

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

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4
Q

What are the physiological side effects of sertraline?

A

→ mild inhibition of dopamine transporter

→ partial inhibition of CYP2D6 at high doses

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5
Q

Why should sertraline be gradually decreased at discontinuation?

A

due to partial inhibition of CYP2D6 at high doses (150 mg)

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6
Q

What is the primary 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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7
Q

What is the drug target for citalopram?

A

Serotonin transporter

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8
Q

What are the main side effects of the citalopram?

A

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

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9
Q

What are the physiological side effects of citalopram?

A

Mild antagonism of muscarinic and histamine (H1) receptors

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10
Q

Why should citalopram be gradually decreased at discontinuation?

A

Must be gradually decreased on discontinuation. Metabolized by CYP2C19.

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11
Q

What is the primary 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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12
Q

What is the drug target for fluoxetine?

A

Serotonin transporter

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13
Q

What are the main side effects of the fluoxetine?

A

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

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14
Q

What are the physiological side effects of fluoxetine?

A

Mild antagonism of 5HT2A and 5HT2C receptors

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15
Q

Why should fluoxetine be gradually decreased at discontinuation?

A

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

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16
Q

What is the primary 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.

17
Q

What is the drug target for fluoxetine?

A

Serotonin transporter

18
Q

What are the main side effects of the fluoxetine?

A

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

19
Q

What are the physiological side effects of fluoxetine?

A

Mild antagonism of 5HT2A + 5HT2C receptors

20
Q

Why should fluoxetine be gradually decreased at discontinuation?

A

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

21
Q

What is the primary mechanism of action of 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.

22
Q

What is the drug target for Venlafaxine?

A

→ Serotonin transporter

→ Noradrenaline transporter

23
Q

What are the main side effects of the Venlafaxine?

A
→ GI effects (nausea, diarrhoea)
→ sexual dysfunction
→ anxiety
→ insomnia
→ hypertension (at high doses)
24
Q

What are the physiological side effects of Venlafaxine?

A

Must be gradually decreased on discontinuation

25
Q

What is the primary 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.

26
Q

What is the drug target for Mirtazapine?

A

→ Alpha-2 receptor

→ 5-HT2 receptor

27
Q

What are the main side effects of the Mirtazapine?

A

→ Weight gain
→ sedation
→ Low probability of sexual dysfunction
→ May exacerbate REM sleep behaviour disorder