Pharma - Depression Flashcards
What is 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 is the drug target for sertraline?
Serotonin transporter
What are the main side effects of the sertraline?
→ GI effects (nausea, diarrhoea)
→ sexual dysfunction
→ anxiety
→ insomnia
What are the physiological side effects of sertraline?
→ mild inhibition of dopamine transporter
→ partial inhibition of CYP2D6 at high doses
Why should sertraline be gradually decreased at discontinuation?
due to partial inhibition of CYP2D6 at high doses (150 mg)
What is the primary 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 is the drug target for citalopram?
Serotonin transporter
What are the main side effects of the citalopram?
→ GI effects (nausea, diarrhoea)
→ sexual dysfunction
→ anxiety
→ insomnia
What are the physiological side effects of citalopram?
Mild antagonism of muscarinic and histamine (H1) receptors
Why should citalopram be gradually decreased at discontinuation?
Must be gradually decreased on discontinuation. Metabolized by CYP2C19.
What is 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 is the drug target for fluoxetine?
Serotonin transporter
What are the main side effects of the fluoxetine?
→ GI effects (nausea, diarrhoea)
→ sexual dysfunction
→ anxiety
→ insomnia
What are the physiological side effects of fluoxetine?
Mild antagonism of 5HT2A and 5HT2C receptors
Why should fluoxetine be gradually decreased at discontinuation?
Complete inhibition of CYP2D6 and significant inhibition of CYP2C19 (caution with warfarin).
What is 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 is the drug target for fluoxetine?
Serotonin transporter
What are the main side effects of the fluoxetine?
→ GI effects (nausea, diarrhoea)
→ sexual dysfunction
→ anxiety
→ insomnia
What are the physiological side effects of fluoxetine?
Mild antagonism of 5HT2A + 5HT2C receptors
Why should fluoxetine be gradually decreased at discontinuation?
Complete inhibition of CYP2D6 and significant inhibition of CYP2C19 (caution with warfarin).
What is 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 is the drug target for Venlafaxine?
→ Serotonin transporter
→ Noradrenaline transporter
What are the main side effects of the Venlafaxine?
→ GI effects (nausea, diarrhoea) → sexual dysfunction → anxiety → insomnia → hypertension (at high doses)
What are the physiological side effects of Venlafaxine?
Must be gradually decreased on discontinuation
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 is the drug target for Mirtazapine?
→ Alpha-2 receptor
→ 5-HT2 receptor
What are the main side effects of the Mirtazapine?
→ Weight gain
→ sedation
→ Low probability of sexual dysfunction
→ May exacerbate REM sleep behaviour disorder
