Pharmacology of Depression Flashcards
What is the drug target for sertraline?
Serotonin transporter
Outline 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 are the main side effects associated with the use of Sertraline?
GI effects (nausea, diarrhoea) sexual dysfunction, anxiety, insomnia
Sertraline use is associated with mild inhibition of which transporter?
Dopamine
How must Sertraline use be discontinued?
Must be gradually decreased on discontinuation
High doses of Sertraline (150mg) result in partial inhibition of which enzyme?
CYP2D6
What is the drug target for Citalopram
Serotonin transporter
Outline 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 are the main side effects associated with Citalopram use?
GI effects (nausea and diarrhoea), sexual dysfunction, anxiety and insomnia
Citalopram is a mild antagonist of which receptors?
Muscarinic and histamine H1
citalopram is metabolised by which enzymes?
CYP2C19
What is the drug target of Fluoxetine?
Serotonin transporters
Outline the primary mechanism of action of Fluoxetine
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 are the main side effects associated with the use of Fluoxetine?
GI effects (nausea and diarrhoea), sexual dysfunction, anxiety, insomnia
Fluoxetine is a mild antagonist of which receptors?
5HT2A and 5HT2C
Fluoxetine causes inhibition of which enzymes?
Complete inhibition of CYP2D6 and significant inhibiton of CYP2C19
What is the drug target for Venlafaxine?
Serotonin transporters and Noradrenaline transporters
Outline the primary 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 main side effects associated with use of Venlafaxine
GI effects, sexual dysfunction, insomnia and hypertension at higher doses
What is the drug target of Mirtazapine?
Alpha-2 receptors and 5-HT2 receptors
Outline 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 main side effects associated with Mirtazapine use?
Weight gain and sedation
Which behaviour disorder is at risk of being exacerbated with use of Mertazapine?
May exacerbate REM sleep behaviour disorder
