fluvoxamine

Brand: Luvox, Luvox CR

⚠ BBW Prototype: fluoxetine
Drug Class: SSRI
Drug Family: antidepressant
Subclass: selective serotonin reuptake inhibitor
Organ Systems: cns

Mechanism of Action

Inhibits neuronal reuptake of serotonin via SERT blockade; uniquely binds to sigma-1 receptors which may contribute to its anxiolytic and anti-inflammatory properties. A potent inhibitor of multiple CYP enzymes.

SERT (serotonin transporter)

Indications

  • OCD (FDA-approved)
  • social anxiety disorder (CR formulation)
  • off-label: depression
  • off-label: PTSD
  • off-label: COVID-19 (investigational)

Contraindications

  • concurrent MAOI use
  • concurrent alosetron use
  • concurrent thioridazine use
  • concurrent tizanidine use
  • concurrent pimozide use

Adverse Effects

Common

  • nausea
  • somnolence
  • insomnia
  • dry mouth
  • dizziness
  • sexual dysfunction

Serious

  • serotonin syndrome
  • suicidal ideation
  • mania activation
  • hyponatremia

Pharmacokinetics (ADME)

Absorption well absorbed orally; bioavailability ~53%; food has no significant effect
Distribution protein binding ~80%; widely distributed
Metabolism primarily hepatic via CYP1A2; potent inhibitor of CYP1A2, CYP2C19, and CYP3A4
Excretion primarily renal; dose adjustment in hepatic impairment
Half-life 15.6 hours (range 9-28 hours)
Onset 2-4 weeks for OCD response
Peak 3-8 hours
Duration 24 hours
Protein Binding 80%
Vd 25 L/kg

Drug Interactions

Drug / Agent Mechanism Severity
MAOIs serotonin syndrome contraindicated
tizanidine CYP1A2 inhibition dramatically increases tizanidine levels; hypotension and CNS depression contraindicated
theophylline CYP1A2 inhibition increases theophylline levels; toxicity risk major
clozapine CYP1A2 inhibition increases clozapine levels 5-10 fold major
warfarin CYP1A2/2C9 inhibition may increase warfarin levels moderate

Nursing Considerations

  1. Fluvoxamine is a potent CYP1A2 and CYP2C19 inhibitor — review all concurrent medications for interactions before administering, particularly clozapine, theophylline, and warfarin.
  2. FDA-approved specifically for OCD rather than depression; ensure indication is correct when verifying medication orders.
  3. Monitor for signs of serotonin syndrome: agitation, hyperthermia, tachycardia, clonus, and hyperreflexia — particularly if combined with tramadol, triptans, or other serotonergic agents.
  4. Educate that nausea is most prominent in first 1-2 weeks and generally resolves; taking with food helps minimize GI symptoms.

Clinical Pearls

  • Fluvoxamine's potent CYP1A2 inhibition creates clinically important drug interactions; it increases clozapine levels by 5-10 fold, which requires dose adjustment in patients starting fluvoxamine.
  • Fluvoxamine's sigma-1 receptor agonism has generated interest as an anti-inflammatory agent during COVID-19 infection, with some positive trial data for preventing progression to severe disease.

Safety Profile

Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required

Concordance Terms

Cross-referenced clinical concepts — click any term to see all content where it appears.