Pharm - Depression Flashcards
What are the main drugs used for depression
Sertraline
Citalopram
Fluoxetine
Venlafaxine
Mitrazapine
What is the primary mechanism of action for Sertraline
Inhibits serotonin reuptake transporters in the presynaptic neurones, mainly in the hippocampus. This therefore reduces uptake and thus increases accumulation of serotonin. Serotonin in the CNS plays a role in regulation of mood, personality and wakefulness
What is the primary mechanism of action for Citalopram
Inhibits serotonin reuptake transporters in the presynaptic neurones, mainly in the hippocampus. This therefore reduces uptake and thus increases accumulation of serotonin. Serotonin in the CNS plays a role in regulation of mood, personality and wakefulness
What is the primary mechanism of action for Fluoxetine
Inhibits serotonin reuptake transporters in the presynaptic neurones, mainly in the hippocampus. This therefore reduces uptake and thus increases accumulation of serotonin. Serotonin in the CNS plays a role in regulation of mood, personality and wakefulness
What is the primary mechanism of action for Venlafaxine
More potent inhibitor of serotonin reuptake than norepinephrine reuptake. Norepinephrine in the CNS is implicated in the regulation of emotions and cognition. (Inhibits reuptake of both Sertonin and Norepinephrine)
What is the primary mechanism of action for Mirtazapine
Antagonises central presynaptic alpha-2 adrenergic receptors, which cause increased release of serotonin and norepinephrine.
Antagonises central 5-HT2 receptors which leaves 5-HT1 receptors unopposed causing anti-depressant effects.
What is the drug target for Sertraline
Serotonin transporter
What is the drug target for Citalopram
Serotonin transporter
What is the drug target for Fluoxetine
Serotonin transporter
What is the drug target for Venlafaxine
Serotonin transporter
Norepinephrine transporter
What is the drug target for Mirtazapine
Alpha-2 receptor
5-HT2 receptor
What are the main side effects for Sertraline
GI effects (nausea and diarrhoea), sexual dysfunction. anxiety, insomnia
What are the main side effects for Citalopram
GI effects (nausea and diarrhoea), sexual dysfunction. anxiety, insomnia
What are the main side effects for Fluoxetine
GI effects (nausea and diarrhoea), sexual dysfunction. anxiety, insomnia
What are the main side effects for Venlafaxine
GI effects (nausea and diarrhoea), sexual dysfunction. anxiety, insomnia, hypertension (at higher doses)
What are the main side effects for Mirtazapine
Weight gain, sedation
What else should we know about Sertraline
Mild inhibition of dopamine transporter.
Must be gradually decreased on discontinuation. Partial inhibition of CYP2D6 at high doses (150mg)
What else should we know about Citalopram
Mild antagonist of muscarinic and histamine H1 receptors
Must be gradually decreased on discontinuation
Metabolised by CYP2C19
What else should we know about Fluoxetine
Mild antagonism of 5Ht2A and 5HT2C receptors
Complete inhibition of CYP2D6 and significant inhibition of CYP2C19 (caution with warfarin)
What else should we know about Venlafaxine
Must be gradually decreased on discontinuation
What else should we know about Mirtazapine
Low probability of sexual dysfunction. May exacerbate REM sleep behaviour disorder
Where do SSRIs act
Serotonin reuptake transporter in presynaptic neurone, largely in the hippocampus
Why do we not give citalopram to people who may be taking erythromycin
Prolongs QT interval
Why must we slowly be weaned off one antidepressant before starting a new one
Due to the risk of drug interactions, serotonin syndrome, withdrawal symptoms, or relapse - therefore washout is required
Which antidepressant is best for someone with sleeping problems
Mirtazapine - modestly suppresses REM sleep whilst still having a beneficial impact on sleep continuity and duration due to its anti-histaminergic effects.
