Therapeutic Function

Antidepressant

Biological Activity

Selective serotonin reuptake inhibitor; antidepressant. Binds to the human 5-HT transporter with a K i of 1.6 nmol/l. Also available as part of the Serotonin Uptake Inhibitor Tocriset? .

Biochem/physiol Actions

Fluvoxamine maleate is a selective neuronal serotonin reuptake inhibitor. It functions as an antidepressant and anti-obsessive agent. It is useful in treating obsessive compulsive disorder and panic disorder.

Veterinary Drugs and Treatments

Fluvoxamine may be considered for use in treating a variety of behavior- related diagnoses in dogs and cats, including aggression and stereotypic behaviors (and other obsessive-compulsive behaviors).

Drug interactions

Potentially hazardous interactions with other drugsAminophylline and theophylline: increased aminophylline and theophylline concentrations - avoid; if not possible, halve aminophylline or theophylline dose and monitor levels.Analgesics: increased risk of bleeding with aspirin and NSAIDs; risk of CNS toxicity increased with tramadol; concentration of methadone possibly increased.Anti-arrhythmics: increased risk of toxicity with mexiletine.Anticoagulants: effect of coumarins possibly enhanced; possibly increased risk of bleeding with dabigatran.Antidepressants: avoid with reboxetine, MAOIs, moclobemide and St John’s wort; possibly enhanced serotonergic effects with mirtazapine; fluvoxamine inhibits metabolism of duloxetine - avoid; can increase tricyclics concentration; metabolism of agomelatine reduced; possible increased risk of convulsions with vortioxetine.Antiepileptics: antagonise anticonvulsant threshold; concentration of carbamazepine, fosphenytoin and phenytoin increased.Antimalarials: avoid with artemether/lumefantrine and piperaquine with artenimol.Antipsychotics: concentration of asenapine, haloperidol, clozapine and olanzapine increased; increased risk of ventricular arrhythmias with droperidol and possibly pimozide - avoid.Antivirals: concentration possibly increased by ritonavir.Ciclosporin: may increase ciclosporin concentration.Clopidogrel: possibly reduced antiplatelet effect.Cytotoxics: concentration of pomalidomide increasedDapoxetine: possible increased risk of serotonergic effects - avoid.Dopaminergics: increased risk of CNS toxicity with rasagiline - avoid; hypertension and CNS excitation with selegiline - avoid. 5HT1 agonists: risk of CNS toxicity increased with sumatriptan; possibly increased risk of serotonergic effects with naratriptan; inhibits metabolism of frovatriptan; possibly inhibits metabolism of zolmitriptan - reduce zolmitriptan dose.Linezolid: use with care, possibly increased risk of side effects.Lithium: increased risk of CNS effects - monitor levels.Melatonin: concentration of melatonin increased - avoid.Methylthioninium: risk of CNS toxicity - avoid if possible.Muscle relaxants: increased risk of toxicity with tizanidine - avoidPirfenidone: concentration of pirfenidone increased - avoid.

Metabolism

Fluvoxamine undergoes extensive hepatic transformation by CYP2D6, mainly via oxidative demethylation, into at least 9 metabolites. The 2 major metabolites showed negligible pharmacological activity. The other metabolites are not expected to be pharmacologically active.Excretion is mainly in the urine; about 2% of a dose is excreted as unchanged drug.

Brand name

Luvox (Solvay Pharmaceuticals);FLOXYFRAL.

General Description

Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards