Pharmacology of Depression Flashcards
What is the Primary mechanism of action of Sertraline?
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.
What is the primary target of Sertraline?
Serotonin transporter
What are the main side effects of Sertraline?
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
What is the effect of Sertraline on the Dopamine transporter?
Mild inhibition of dopamine transporter
How should you discontinue Sertraline?
Must be gradually decreased on discontinuation. Partial inhibition of CYP2D6 at high doses (150 mg)
What is the mechanism of action of Citalopram?
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.
What is the primary target of Citalopram?
Serotonin transporter
What are the main side effects of Citalopram?
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
What is the effect of Citalopram on Histamine receptors?
Mild antagonism of muscarinic and histamine (H1) receptors
How should Citalopram be discontinued?
Must be gradually decreased on discontinuation. Metabolized by CYP2C19
What is the mechanism of action of Fluexotine?
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.
What is the primary target of Fluexotine?
Serotonin transporter
What are the main side effects of Fleuxotine?
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
What is the effect of Fluexotine on 5HT2A and 5HT2C receptors?
Mild antagonism of 5HT2A and 5HT2C receptors
Which drug should you be cautious of using Fluexotine with?
WARFARIN
Complete inhibition of CYP2D6 and significant inhibition of CYP2C19 (caution with warfarin)
What is the mechanism of action of 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 primary targets of Venlafaxine?
Serotonin transporter
Noradrenaline transporter
What are the side effects of Venlafaxine?
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia, hypertension (at higher doses)
How should Venlafaxine be discontinued?
Gradually
What is the primary mechanism of action of Mirtazapine?
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.
What are the primary targets of Mirtazapine?
Alpha-2 receptor
5-HT2 receptor
What are the main side effects of Mirtazapine?
Weight gain, sedation, Low probability of sexual dysfunction. May exacerbate REM sleep behaviour disorder
