|Trade names||Luvox, Faverin, Fluvoxin, others|
|Drug class||Selective serotonin reuptake inhibitor (SSRI)|
|Bioavailability||53% (90% confidence interval: 44–62%)|
|Metabolism||Hepatic (via cytochrome P450 enzymes. Mostly via oxidative demethylation)|
|Elimination half-life||12–13 hours (single dose), 22 hours (repeated dosing)|
|Excretion||Renal (98%; 94% as metabolites, 4% as unchanged drug)|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||318.335 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Fluvoxamine, sold under brand names such as Luvox or Fevarin, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is primarily used to treat major depressive disorder and obsessive–compulsive disorder (OCD), but is also used to treat anxiety disorders such as panic disorder, social anxiety disorder, and post-traumatic stress disorder.
Fluvoxamine's side-effect profile is very similar to other SSRIs: constipation, gastrointestinal problems, headache, anxiety, irritation, sexual problems, dry mouth, sleep problems and a risk of suicide at the start of treatment by lifting the psychomotor inhibition, but these effects appear to be significantly weaker than with other SSRIs (except gastrointestinal side-effects). The tolerance profile is superior in some respects to other SSRIs, particularly with respect to cardiovascular complications, despite its age.
A clinical trial published in The Lancet in October 2021 claims that fluvoxamine reduces severity of COVID-19 symptoms.
It is on the World Health Organization's List of Essential Medicines.
In many countries (e.g., Australia, the UK, and Russia) it is commonly used for major depressive disorder. Fluvoxamine is also approved in the United States for OCD, and social anxiety disorder. In Japan it is also approved to treat OCD, SAD and MDD. Fluvoxamine is indicated for children and adolescents with OCD. The drug works long-term, and retains its therapeutic efficacy for at least one year. It has also been found to possess some analgesic properties in line with other SSRIs and tricyclic antidepressants.
There is tentative evidence that fluvoxamine is effective for social phobia in adults. Fluvoxamine is also effective for GAD, SAD, panic disorder and separation anxiety disorder in children and adolescents. There is tentative evidence that fluvoxamine may help some people with negative symptoms of chronic schizophrenia.
In October 2021, a large clinical trial in Brazil reported that treating high-risk outpatients with an early diagnosis of COVID-19 with 100 mg fluvoxamine twice daily for 10 days reduced by up to about 65% the risk of hospitalization (retention in a COVID-19 emergency setting or transfer to a tertiary hospital). The effect was reduced to about 32% with low adherence, possibly due to intolerance. There was also a reduction in the number of deaths by up to about 90% with high adherence. The drug was studied because of its anti-inflammatory effects and its activity against the sigma-1 receptor, but the mechanism of action against COVID-19 remains uncertain.
Gastrointestinal side effects are more common in those receiving fluvoxamine than with other SSRIs. Otherwise, fluvoxamine's side-effect profile is very similar to other SSRIs.
Fluvoxamine inhibits the following cytochrome P450 enzymes:
By so doing, fluvoxamine can increase serum concentration of the substrates of these enzymes.
The plasma levels of oxidatively metabolized benzodiazepines (e.g., triazolam, midazolam, alprazolam and diazepam) are likely to be increased when co-administered with fluvoxamine. However the clearance of benzodiazepines metabolized by glucuronidation (e.g., lorazepam, oxazepam, temazepam) is unlikely to be affected by fluvoxamine. It appears that benzodiazepines metabolized by nitro-reduction (clonazepam, nitrazepam) are unlikely to be affected by fluvoxamine. Using fluvoxamine and alprazolam together can increase alprazolam plasma concentrations. If alprazolam is coadministered with fluvoxamine, the initial alprazolam dose should be reduced to the lowest effective dose.
Fluvoxamine and ramelteon coadministration is not indicated.
Fluvoxamine has been observed to increase serum concentrations of mirtazapine, which is mainly metabolized by CYP1A2, CYP2D6, and CYP3A4, by three- to four-fold in humans. Caution and adjustment of dosage as necessary are warranted when combining fluvoxamine and mirtazapine.
Fluvoxamine seriously affects the pharmacokinetics of tizanidine and increases the intensity and duration of its effects. Because of the potentially hazardous consequences, the concomitant use of tizanidine with fluvoxamine, or other potent inhibitors of CYP1A2, should be avoided.
Fluvoxamine's interaction with St John's wort can lead to increased serotonin levels and potentially lead to serotonin syndrome.
Fluvoxamine is a potent selective serotonin reuptake inhibitor with around 100-fold affinity for the serotonin transporter over the norepinephrine transporter. It has negligible affinity for the dopamine transporter or any other site, with the sole exception of the σ1 receptor. It behaves as a potent agonist at this receptor and has the highest affinity (36 nM) of any SSRI for doing so. This may contribute to its antidepressant and anxiolytic effects and may also afford it some efficacy in treating the cognitive symptoms of depression. Unlike some other SSRI, fluvoxamine's metabolites are pharmacologically neutral.
Fluvoxamine was developed by Kali-Duphar, part of Solvay Pharmaceuticals, Belgium, now Abbott Laboratories, and introduced as Floxyfral in Switzerland in 1983. It was approved by the U.S. Food and Drug Administration (FDA) in 1994, and introduced as Luvox in the US. In India, it is available, among several other brands, as Uvox by Abbott. It was one of the first SSRI antidepressants to be launched, and is prescribed in many countries to patients with major depression. It was the first SSRI, a non-TCA drug, approved by the U.S. FDA specifically for the treatment of OCD. At the end of 1995, more than ten million patients worldwide had been treated with fluvoxamine.[failed verification] Fluvoxamine was the first SSRI to be registered for the treatment of obsessive compulsive disorder in children by the FDA in 1997. In Japan, fluvoxamine was the first SSRI to be approved for the treatment of depression in 1999 and was later in 2005 the first drug to be approved for the treatment of social anxiety disorder. Fluvoxamine was the first SSRI approved for clinical use in the United Kingdom.
Manufacturers include BayPharma, Synthon, and Teva, among others. Luvox was notably used by Eric Harris, one of the Columbine shooters.