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).