Pharmacology Of Depression Flashcards
Sertraline mechanism of action
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.
Drug target of sertraline
Seratonin transporter
Sertraline main side effects
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
Extra info on Sertraline
Mild inhibition of dopamine transporter
Must be gradually decreased on discontinuation. Partial inhibition of CYP2D6 at high doses (150 mg).
In 2020 – Sertraline was the 16th most commonly prescribed drug in West London area
Citalopram mechanism of action
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.
Citalopram target
Seratonin transporter
Side effects of Citalopram
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
Extra info on sitalopram
Mild antagonism of muscarinic and histamine (H1) receptors
Must be gradually decreased on discontinuation. Metabolized by CYP2C19.
In 2020 – Citalopram was the 27th most commonly prescribed drug in West London area
Fluoxetine mechanism of action
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.
Target of fluoxetine
Seratonin transporter
Side effects of fluoxetine
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
Extra info on fluoxetine
Mild antagonism of 5HT2A and 5HT2C receptors
Complete inhibition of CYP2D6 and significant inhibition of CYP2C19 (caution with warfarin).
In 2020 – Fluoxetine was the 68th most commonly prescribed drug in West London area
Velafaxine mechanism of action
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.
Drug target of venlafaxine
Serotonin transporter
Noradrenaline transporter
Side effects of venlafaxine
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia, hypertension (at higher doses)
Venlafaxine extra info
Must be gradually decreased on discontinuation
In 2020 – Venlafaxine was the 83rd most commonly prescribed drug in West London area
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.
Mirtazapine drug target
Highest to lowest affinity
Histamine receptors H1
Alpha 2 receptor
5HT2
5HT3 (anti emetic)
Side effects of mirtazapine
Weight gain and sedation
Extra info on mertazapine
Low probability of sexual dysfunction. May exacerbate REM sleep behaviour disorder
It is a noradrenerguc and specific seratonergic antidepressant NaSSA
In 2020 – Mirtazapine was the 30th most commonly prescribed drug in West London area
Management
SSRI first line
Trial 2 until failure or intolerance
Then SNRI or mirtazapine
Then TCA
