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
2
Q
What is the primary drug target of sertraline?
A
- Na+ dependent serotonin transporter
3
Q
What is the drug target type of sertraline?
A
- Transport protein antagonist
4
Q
What is the location of action of sertraline?
A
- Presynaptic neurones of the CNS
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
7
Q
What are the main adverse effects of sertraline (4)?
A
- GI function (nausea / diarrhoea)
- Sexual dysfunction
- Anxiety
- Insomnia
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
9
Q
What is citalopram used for?
A
- Citalopram is a selective serotonin reuptake inhibitor (SSRI) used in the treatment of depression
10
Q
What is the primary drug target of citalopram?
A
- Na+ dependent serotonin transporter
11
Q
What is the drug target type of citalopram?
A
- Tranport protein antagonist
12
Q
What is the location of action of citalopram?
A
- Presynaptic neurones of the CNS
13
Q
What are the main adverse effects of citalopram (4)?
A
- GI function (nausea / diarrhoea)
- Sexual dysfunction
- Anxiety
- Insomnia
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
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
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
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
What is the location of action of venlafaxine?
* Presynaptic neurones of the CNS
29
What is the mechanism of action of venlafaxine?
* 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
What are the main adverse effects of venlafaxine (5)?
* GI function (Nausea / Diarrhoea)
* Sexual dysfunction
* Hypertension
* Anxiety
* Insomnia
31
What is the process of discontinuation of venlafaxine?
* Must be gradually decreased
32
What is mirtazapine used for?
* 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
What is the mechanism of action of mirtazapine?
* 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
What are the primary drug targets of mirtazapine?
* Serotonin receptor 2A (5-HT2A receptor)
* Alpha-2A adrenergic receptor (ADRA2A receptor)
35
What is the drug target type of mirtazapine?
* Receptor antagonist
36
What is the location of action of mirtazapine?
* Presynaptic neurones of the CNS
38
What are the main adverse effects of mirtazapine (4)?
* Weight gain
* Sedation
* Sexual dysfunction (rare)
* May exacerbate REM sleep behaviour
