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Pharmacology And Theraputics 1b > Pharmacology of Depression > Flashcards

Pharmacology of Depression Flashcards

1
Q

What is the mechanism of action of sertraline?

A
  • Inhibition of serotonin reuptake causing accumulation of serotonin
  • sertraline plays a role in regulation of mood, personality and wakefulness
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2
Q

What is the drug target of sertraline?

A

serotonin transporter

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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

What are the other minor effects of sertraline?

A
  • mild inhibition of the dopamine transporter
  • partial inhibiton of enzyme involved in metabolising drugs (CYP2D6) at high dosages
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5
Q

What is the process of discontinuing sertraline?

A

gradually decreased over time

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6
Q

What is the primary mechanism of action of citalopram?

A

Inhibition of serotonin reuptake causing accumulation of serotonin

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7
Q

What is the drug target of citalopram?

A

Serotonin transporter

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8
Q

What are the main side effects of citalopram?

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

What are the other minor effects of citalopram?

A

mild antagonism of muscarinic and histamine (H1) receptors)

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10
Q

What is citalopram metabolised by?

A

CYP2C19

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11
Q

What is the process of discontinuing citalopram?

A

gradually decreased over time

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12
Q

What is the primary mechanism of action of Fluoxetine?

A

Inhibition of serotonin reuptake; accumulation of serotonin

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13
Q

What is the drug target of Fluoxetine?

A

Serotonin transporter

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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 are the other minor effects of Fluoxetine?

A
  • Mild antagonism of serotonin receptors (5HT2A and 5HT2C)
  • Complete inhibition of enzymes which metabolise drugs (CYP2D6 and significant inhibition of CYP2C19)
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16
Q

What drug contraindicates with Fluoxetine?

A

Warfarin

17
Q

What is the mechanism of action of Venlafaxine?

A
  • Inhibitor of serotonin reuptake
  • less potent inhibitor of norepinephrine reuptake
    (noradrenaline regulates emotions and cognition)
18
Q

What is the drug target of Venlafaxine?

A

Serotonin and Noradrenalin transporter

19
Q

What are the main side effects of Venlafaxine?

A
  • GI effects (nausea, diarrhoea)
  • sexual dysfunction
  • anxiety
  • insomnia
  • hypertension (at higher doses)
  • prolonged QT interval
20
Q

What is the process of discontinuing Venlafaxine?

A

gradual decrease over time

21
Q

What is the primary mechanism of action of Mirtazapine?

A
  • Antagonises central pre-synaptic alpha-2-adrenergic receptors
  • This increases release of serotonin and norepinephrine
  • Antagonises central 5HT2 receptors, which leaves 5HT1 receptors unopposed causing anti-depressant effects.
22
Q

What are the drug targets of Mirtazapine?

A
  • alpha-2 receptor
  • 5-HT2 receptor
23
Q

What are the main side effects of Mirtazapine?

A
  • weight gain
  • sedation
24
Q

What are the less common side effects of Mirtazapine?

A

May exacerbate REM sleep behaviour disorder

25
Q

What is an advantage of taking mirtazapine?

A

Low probability of sexual dysfunction

26
Q

What are the disadvantages of taking Mirtazapine?

A
  • low selectivity
  • highest affinity is to H1 receptors causing sedation (not therapeutic objective)
27
Q

Why should you avoid taking erythromycin and citalopram simultaneously?

A

both prolong the Q-T interval

28
Q

What, other than drugs can increase the Q-T interval?

A
  • increasing age
  • female
  • CVD
  • certain metabolic disorders (hypokalaemia)
29
Q

What causes the plateau when studying the effectiveness of SSRIs?

A

there are only a limited amount of serotonin reuptake sites on the presynaptic neurone, therefore they become fully blocked and maxed out, so an increased dose has no increased therapeutic effect.

30
Q

Why is there a washout period when changing anti-depressants?

A

risk of:

  • drug-drug interactions
  • serotonin syndrome
  • withdrawal symptoms
  • relapse
31
Q

What is the impact of Mirtazapine on sleep?

A
  • suppresses REM sleep
  • increases sleep continuity and duration due to anti-histaminergic effects
32
Q

Why does blood pressure need to be measured when administering Venlafaxine?

A
  • adrenergic effects of venlafaxine appear with doses of >150 mg/day
  • apparent increase in blood pressure and increased heart rate are observed when the daily dose exceeds 300 mg
33
Q

What receptor does Mirtazapine have the highest affinity for, and what is the effect?

A
  • Histamine (H1) receptor
  • sedation
34
Q

What happens at high doses of Mirtazapine?

A

antihistamine effect is offset by increased noradrenergic transmission, reducing the sedating effect.

Pharmacology And Theraputics 1b (10 decks)

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