Pharmacology Of Depression Flashcards
What is the primary mechanism of action of Sertraline?
Inhibition of serotonin reuptake resulting 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 drug target of Sertraline?
Serotonin transporter
What are the main side effects of Sertraline?
GI effects - nausea, diarrhoea
Sexual dysfunction
Anxiety
Insomnia
What else does Sertraline inhibit?
Mild inhibition of dopamine receptor
At high doses - partial inhibition of CYP2D6
What is the primary mechanism of action of Citalopram?
Inhibition of serotonin reuptake resulting in an accumulation of serotonin
What is the primary drug target of Citalopram?
Serotonin transporter
What are the main side effects of Citalopram?
GI effects - nausea, diarrhoea
Sexual dysfunction
Anxiety
Insomnia
What other effects does Citalopram have?
Mild antagonism of muscarinic and histamine (H1) receptors
What is Citalopram metabolised by?
CYP2C19
What is the primary mechanism of action of Fluoxetine?
Inhibition of serotonin reuptake resulting in an accumulation of serotonin
What is the primary drug target of Fluoxetine?
Serotonin transporter
What are the main side effects of Fluoxetine?
Nausea, diarrhoea
Sexual dysfunction
Anxiety
Insomnia
What other effects does Fluoxetine have?
Mild antagonism of 5HT2A and 5HT2C receptors
Complete inhibition of CYP2D6 and significant inhibition of CYP2C19 (caution with warfarin)
What is the primary mechanism of action of Venlaflaxine?
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 drug targets of Venlafaxine?
Serotonin transporter
Noradrenaline transporter
What are the main side effects of Venlafaxine?
Nausea, diarrhoea
Sexual dysfunction
Anxiety
Insomnia
Hypertension (at higher doses)
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 drug targets of Mirtazapine (for depression)?
Alpha-2-receptor
5-HT2 receptor
What are the main side effects of Mirtazapine?
Weight gain
Sedation
What may Mirtazapine exacerbate if present?
REM sleep behaviour disorder
Which drugs must be gradually decreased on discontinuation and why?
Sertraline
Citalopram
Venlafaxine
Caution is required when switching from one antidepressant to another due to the risk of drug interactions, serotonin syndrome, withdrawal symptoms, or relapse
Washout is required before starting a new drug
What are the other drug targets for Mirtazapine?
Histamine (H1) receptor - sedation
5HT3 receptor - anti-emetic
