Pharmacology of depression Flashcards
What drugs are used to treat depression?
- Sertraline
- Citalopram
- Fluoxetine
- Venlafaxine
- Mirtazapine
What is the drug target of sertraline?
Serotonin transporter
What is the primary mechanism of action of sertraline?
Inhibition of serotonin reuptake -> accumulation of serotonin.
Serotonin in the CNS plays a role in the regulation of mood, personality, and wakefulness.
What is the side effect of sertraline?
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
What else might sertraline bind to?
Mild inhibition of dopamine transporter
What is the drug target for citalopram?
Serotonin transporter
What is the primary mechanism of action for citalopram?
Inhibition of serotonin reuptake -> accumulation of serotonin.
Serotonin in the CNS plays a role in the regulation of mood, personality, and wakefulness.
What are the side effects of citalopram?
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
What else might citalopram bind to?
Mild antagonism of muscarinic and histamine (H1) receptors
What is the primary target of fluoxetine?
Serotonin transporter
What is the mechanism of action of fluoxetine?
Inhibition of serotonin reuptake -> accumulation of serotonin. Serotonin in the central nervous system plays a role in the regulation of mood, personality, and wakefulness
What are the side effects of fluoxetine?
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
What else might fluoxetine bind to?
Mild antagonism of 5HT2A and 5HT2C receptor
Which drug must you be careful using fluoxetine with?
Significant inhibition of CYP2C19 (caution with warfarin).
What is the drug target of venlafaxine?
Serotonin transporter
Noradrenaline transporter
What is the primary mechanism of action for venlafaxine?
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.
What are the side effects of venlafaxine?
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia, hypertension (at higher doses)
What is the drug target of mirtazapine?
Alpha-2 receptor
5-HT2 receptor
What is the primary mechanism of action for mirtazapine?
Antagonises central presynaptic alpha-2-adrenergic receptors -> increased release of serotonin and norepinephrine.
Antagonises central 5HT2 receptors, which leaves 5HT1 receptors unopposed causing anti-depressant effects.
What are the side effects of mirtazapine?
Weight gain, sedation
What effect can sertraline have on the dopamine transporter?
Mild inhibition of dopamine transporter
How should sertraline be discontinued?
Must be gradually decreased on discontinuation. Partial inhibition of CYP2D6 at high doses (150 mg).
What is the effect of citalopram on muscarinic & histamine (H1) receptors?
Mild antagonism
How should citalopram be discontinued?
Must be gradually decreased on discontinuation. Metabolized by CYP2C19.
Which enzymes does fluoxetine inhibit?
Complete inhibition of CYP2D6 and significant inhibition of CYP2C19 (caution with warfarin).
How must venlafaxine be discontinued?
Must be gradually decreased on discontinuation
What can mirtazapine exacerbate?
May exacerbate REM sleep behaviour disorder
