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pharmacology & therapeutics > Pharmacology of Depression > Flashcards

Pharmacology of Depression Flashcards

Sertraline Citalopram Fluoxetine Venlafaxine Mirtazapine

1
Q

What is sertraline used for?

A
  • Sertraline is a selective serotonin reuptake inhibitor (SSRI) indicated to treat major depressive disorder, social anxiety disorder and many other psychiatric conditions
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2
Q

What is the primary drug target of sertraline?

A
  • Na+ dependent serotonin transporter
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3
Q

What is the drug target type of sertraline?

A
  • Transport protein antagonist
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4
Q

What is the location of action of sertraline?

A
  • Presynaptic neurones of the CNS
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5
Q

What is the mechanism of action of sertraline?

A
  • Sertaline binds on the serotonin transporters on the presynaptic neurones of the CNS
  • Inhibits the reabsorption of serotonin (5-HT)
  • Accumulation of serotonin in the synapse
  • Serotonin is the central nervous system plays a role in the regulation of mood, personality, and wakefulness
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7
Q

What are the main adverse effects of sertraline (4)?

A
  • GI function (nausea / diarrhoea)
  • Sexual dysfunction
  • Anxiety
  • Insomnia
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8
Q

What is the effect of sertraline on the other neurotransmitters (not serotonin)?

A
  • Dopamine:
    • Mild inhibition of Na+ dependent dopamine transporter
  • Noradrenaline:
    • Mild inhibition of Na+ dependent noradrenaline transporter → increase of noradrenaline in the synapse → May decrease SNS response activation → Increase heart tone
  • CYP2D6:
    • Partial inhibition of CYP2D6 (encodes a member of the cytochrome P450 superfamily of enzymes) at high doses
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9
Q

What is citalopram used for?

A
  • Citalopram is a selective serotonin reuptake inhibitor (SSRI) used in the treatment of depression
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10
Q

What is the primary drug target of citalopram?

A
  • Na+ dependent serotonin transporter
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11
Q

What is the drug target type of citalopram?

A
  • Tranport protein antagonist
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12
Q

What is the location of action of citalopram?

A
  • Presynaptic neurones of the CNS
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13
Q

What are the main adverse effects of citalopram (4)?

A
  • GI function (nausea / diarrhoea)
  • Sexual dysfunction
  • Anxiety
  • Insomnia
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14
Q

What is the mechanism of action of citalopram?

A
  • Citalopram binds on the serotonin transporters on the presynaptic neurones of the CNS
  • Inhibits the reabsorption of serotonin (5-HT)
  • Accumulation of serotonin in the synapse
  • Serotonin is the central nervous system plays a role in the regulation of mood, personality, and wakefulness
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15
Q

What is the effect of citalopram on the other receptors?

A
  • H1 receptors:
    • Mild inhibition of muscarinic and histamine (H1) receptors → inhibiting the vasodilator effects of histamine → sedative
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17
Q

What is fluoxetine used for?

A
  • Fluoxetine is a selective serotonin reuptake inhibitor used to treat major depressive disorder, bulimia, OCD, premenstrual dysphoric disorder, panic disorder, and bipolar I
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18
Q

What is the primary drug target of fluoxetine?

A
  • Na+ depndent serotonin transporter
19
Q

What is the drug target type of fluoxetine?

A
  • Tranport protein antagonist
20
Q

What is the location of action of fluoxetine?

A
  • Presynaptic neurones of the CNS
21
Q

What is the mechanism of action of fluoxetine?

A
  • Fluoxetine binds on the serotonin transporters on the presynaptic neurones of the CNS
  • Inhibits the reabsorption of serotonin (5-HT)
  • Accumulation of serotonin in the synapse
  • Serotonin is the central nervous system plays a role in the regulation of mood, personality, and wakefulness
22
Q

What are the main adverse effects of fluoxetine (4)?

A
  • GI function (nausea / diarrhoea)
  • Sexual dysfunction
  • Anxiety
  • Insomnia
23
Q

What is the effect of fluoxetine on the other receptors?

A
  • 5HT2C & 5HT2A receptor:
    • Mild inhibition of 5-hydroxytryptamine receptor 2C (5HT2C) & 5-hydroxytryptamine receptor 2A (5HT2A) → Decrease in serotonin reuptake
  • CYP2D6 &CYP2D19:
    • Complete inhibition of CYP2D6 and significant inhibition of CYP2D19 → decrease in metabolism of xenobiotics (decrease in metabolism of s-enantiomer of warfarin) → increase in haemorrhage
25
Q

What is venlafaxine used for?

A
  • Venlafaxine is a selective serotonin and norepinephrine reuptake inhibitor (SNRI) used for the treatment of major depression
26
Q

What are the primary drug targets of venlafaxine?

A
  • Na+ dependent serotonin transporter
  • Na+ dependent noradrenaline transporter
27
Q

What is the drug target type of venlafaxine?

A
  • Transport protein antagonist
28
Q

What is the location of action of venlafaxine?

A
  • Presynaptic neurones of the CNS
29
Q

What is the mechanism of action of venlafaxine?

A
  • Inhibit reuptake of serotonin (5-HT) & norepinephrine (NE)
    • Greater potency of 5-HT than for NE receptor
    • Noradrenaline in the central nervous system is implicated in the regulation of emotions and cognition.
30
Q

What are the main adverse effects of venlafaxine (5)?

A
  • GI function (Nausea / Diarrhoea)
  • Sexual dysfunction
  • Hypertension
  • Anxiety
  • Insomnia
31
Q

What is the process of discontinuation of venlafaxine?

A
  • Must be gradually decreased
32
Q

What is mirtazapine used for?

A
  • Mirtazapine is a tetracyclic antidepressant used in the treatment of major depression and is used off-label as a drug for insomnia and to increase appetite
33
Q

What is the mechanism of action of mirtazapine?

A
  • Antagonist inhibits activity at presynaptic ADRA2A (alpha-2-adrenergic receptors) receptor
  • Inhibit autoreceptor & heteroreceptor in CNS
  • Enhanced release of NE & 5-HT
  • 5-HT2A receptor antagonist
  • Increases 5-HT1A transamination
  • Increase activity of 5-HT
34
Q

What are the primary drug targets of mirtazapine?

A
  • Serotonin receptor 2A (5-HT2A receptor)
  • Alpha-2A adrenergic receptor (ADRA2A receptor)
35
Q

What is the drug target type of mirtazapine?

A
  • Receptor antagonist
36
Q

What is the location of action of mirtazapine?

A
  • Presynaptic neurones of the CNS
38
Q

What are the main adverse effects of mirtazapine (4)?

A
  • Weight gain
  • Sedation
  • Sexual dysfunction (rare)
  • May exacerbate REM sleep behaviour

pharmacology & therapeutics (11 decks)

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