fluvoxamine
Boxed Warning
Suicidality risk in children, adolescents, and young adults under 25 during initial treatment.
Fluvoxamine is an SSRI primarily approved for obsessive-compulsive disorder (OCD). It is a potent inhibitor of CYP1A2 and CYP2C19 and also has sigma-1 receptor agonist activity, which may contribute to its anxiolytic properties.
25mg, 50mg, 100mg, 200mg
Tablets: 25mg, 50mg, 100mg; Extended-release capsules (CR): 100mg, 150mg
Category C (risk cannot be ruled out)
Selective serotonin reuptake inhibitor (SSRI) that potently inhibits the serotonin transporter (SERT). Also acts as a sigma-1 receptor agonist, which may provide additional anti-anxiety and neuroprotective effects.
Short half-life. CR formulation available. Tablets can be split for gradual reduction.
Shorter half-life than most SSRIs; slower taper pace recommended. Tablets can be dissolved in water for precise dosing.
Toxicity
Serotonin syndrome with serotonergic combinations. Significant drug interactions due to CYP1A2 inhibition (e.g., with theophylline, clozapine, tizanidine).
Pharmacokinetics
Completely absorbed after oral administration. Bioavailability ~53% due to first-pass metabolism. Tmax 3–8 hours. Food does not significantly affect absorption.
~25 L/kg
Extensively metabolized hepatically via CYP2D6 and CYP1A2. Potent inhibitor of CYP1A2 and CYP2C19, moderate inhibitor of CYP2C9 and CYP3A4. No active metabolites.
Renal (~94% as metabolites, ~2% unchanged).
~77–80%
~1400 mL/min (apparent oral clearance)
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