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Selective Serotonin Reuptake Inhibitors (SSRIs), Treatment of serotonin…
Selective Serotonin Reuptake Inhibitors (SSRIs)
Drugs
Sertraline
Citalopram
Paroxetine
Fluvoxamine
Escitalopram
Fluoxetine
MOA
Selectively block reuptake of serotonin into neurons in the CNS
A delay of 2 to 4 weeks to show effects
Disadvantages
serotonin syndrome
less effective than TCAs in treating severe depression
CYP450 inhibition
Advantages
less sedative and anticholinergic effects than TCAs
less dangerous when overdose
effective in treating moderate depression
no cheese reaction
Drug-drug Interactions
SSRIs are CYP450 inhibitors
: inhibit metabolism of other drugs, increasing their plasma level
MAOIs
: serotonin syndrome (hyperthermia, CV collapse, muscle rigidity, rapid changes in mental status & vital signs, autonomic instability, neuromuscular abnormalities, death
Sertraline
Food increases bioavailability. Extensive 1st pass effect. Desmethylsertraline (metabolite) has a longer half-life.
Very weak CYP450 interaction (slight effect on CYP2D6). Less sedating than paroxetine. Increase number of GI distress. Can induce mania.
Other indications
anxiety disorders, bulimia nervosa (psychiatric disorder), nocturnal enuresis
Not recommended in pts under 18yo - AEs: insomnia, aggression, excitement within first few weeks)
Biotransformation in liver
Active metabolites, eg. fluoxetine
CYP450 isoforms - polymorphism interindividual variability
Paroxetine
potent CYP2D6 inhibitor. more anticholinergic effects. sedating (good initial relief for anxiety and insomnia). Pregnancy category: D
Citalopram
Safer. Less DDI / CYP450 inhibition. May be sedative. Escitalopram (S isomer) has less AEs.
Fluoxetine
active metabolite: norfluoxetine (half-life: 8 days)
potent CYP2D6 inhibitor
More likely to induce mania
Fluovoxamine
less nausea
selective potent CYP1A2 inhibitor
Adverse effects (SSS)
Stomach (GI): nausea, anorexia
Sexual dysfunction: loss of libido, failure of orgasm
Serotonin syndrome (intoxication/drug interactions)
CNS: insomnia, fatigue
Treatment of serotonin syndrome
: benzodiazepine, cyproheptadine, hydration/cooling