Pharmacology of Depression Flashcards
what is the target for sertraline?
serotonin transporter
mild dopamine transporter
what is the MOA of sertraline?
inhibition of serotonin reuptake = serotonin accumulates
what are the main side effects of sertraline?
GI effects - nausea, diarrhoea
sexual dysfunction
anxiety
insomnia
what other receptor does sertraline act on?
inhibits dopamine transporter mildly
what is the MOA of citalopram?
inhibition of serotonin reuptake = serotonin accumulation
what is the target for citalopram?
serotonin transporter
what are the common side effects for citalopram?
GI effects - diarrhoea, nausea
insomnia
anxiety
what other receptors does citalopram work on?
antagonist of muscarinic and H1 receptors
what is the MOA for fluoxetine?
inhibition of serotonin reuptake = accumulation of serotonin
what is the role of serotonin in the CNS?
regulation of mood, personality and wakefulness
what are the common side effects of fluoxetine?
GI effects - nausea, diarrhoea
sexual dysfunction
anxiety
insomnia
what cautions must be taken with fluoxetine?
warfarin
complete inhibition of CYP2D6 and partial inhibition of CYP2C19
what is the MOA of venlafaxine?
inhibition of serotonin reuptake, and a bit of noradrenaline
what is the role of noradrenaline in the CNS?
regulation of emotions and cognition
what is the target for venlafaxine?
noradrenaline and serotonin transporter
what are the common side effects of venlafaxine?
GI effects - nausea, diarrhoea sexual dysfunction anxiety insomnia hypertension at high doses
what is the MOA of mirtazapine?
antagonises central presynaptic alpha-2-adrenergic receptor – increased release of serotonin and noradrenaline
antagonises central 5HT2 receptor leaving 5HT1 open to serotonin and anti-depressant effects
what is the target for mitrazapine?
alpha-2 receptor
5-HT2 receptor
what are the common side effects of mirtazapine?
weight gain, sedation
what disorder should be taken into account for mirtazapine?
may exacerbate REM sleep behaviour disorder - helps REM sleep and consistency of sleep
why must sertraline and venlafaxine be weaned off slowly?
potential for rebound depression, serotonin syndrome
what receptor does mirtazapine have the highest affinity for?
H1 receptor - causing sedation at low doses
how are the effects of mirtazapine binding to H1 offset at higher doses?
sedation effects are overcome by increased noradrenergic transmission
first line treatment for depression
SSRI
what do you have to do before switching from SSRI to any other
trial at least 2 SSRIs
what to try if SSRI failure or bad SEs (2nd line)
SNRI
mitrazapine
