Fluvoxamine

Fluvoxamine

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Not to be confused with Fluoxetine.
Fluvoxamine
Fluvoxamine.svg
Fluvoxamine 3D 4ENH.png
Clinical data
Trade namesFaverin, Fevarin, Floxyfral, Dumyrox, Luvox
AHFS/Drugs.comMonograph
MedlinePlusa682275
Pregnancy
category
  • C
Routes of
administration		Oral (tablets)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability53% (90% confidence interval: 44–62%)[1]
Protein binding80%[1]
MetabolismHepatic (via cytochrome P450 enzymes. Mostly via oxidative demethylation)[1]
Elimination half-life12–13 hours (single dose), 22 hours (repeated dosing)[1]
ExcretionRenal (98%; 94% as metabolites, 4% as unchanged drug)[1]
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard100.125.476 Edit this at Wikidata
Chemical and physical data
FormulaC15H21F3N2O2
Molar mass318.335
3D model (JSmol)
 NoYes (what is this?)  (verify)
Fluvoxamine, sold under the brand name Luvox among others, is a medication which is used primarily for the treatment of obsessive–compulsive disorder (OCD),[3] and is also used to treat major depressive disorder and anxiety disorders such as panic disorder and post-traumatic stress disorder.[4] Fluvoxamine CR (controlled release) is approved to treat social anxiety disorder.[5] It is a selective serotonin reuptake inhibitor (SSRI)[6] and Ïƒ1 receptor agonist.
The FDA has added a black box warning for this drug in reference to increased risks of suicidal thoughts and behavior in young adults and children.

Medical uses[edit]

Fluvoxamine's only FDA approved indication is in the treatment of OCD,[7] although in other countries (e.g. Australia,[8] the UK,[9] and Russia[10]) it also has indications for major depressive disorder. Fluvoxamine has been found to be useful in the treatment of major depressive disorder, anxiety disorders such as panic disorder, social anxiety disorder, and posttraumatic stress disorder, and other obsessive–compulsive spectrum disorders. Fluvoxamine is indicated for children and adolescents with OCD.[11] The drug works long-term, and retains its therapeutic efficacy for at least a year.[12] It has also been found to possess some analgesic properties in line with other SSRIs and tricyclic antidepressants.[13][14][15]
Some evidence shows fluvoxamine may be a helpful adjunct in the treatment of schizophrenia, improving the depressive, negative, and cognitive symptoms of the disorder.[16] Its actions at the sigma receptor may afford it a unique advantage among antidepressants in treating the cognitive symptoms of schizophrenia.[17]

Adverse effects[edit]

Gastrointestinal side effects are more common in those receiving fluvoxamine than with other SSRIs.[18] Otherwise, fluvoxamine's side-effect profile is very similar to other SSRIs.[1][7][8][9][19][20]
Common (1–10% incidence) adverse effects
  • Nausea
  • Vomiting
  • Weight loss
  • Yawning
  • Loss of Appetite
  • Agitation
  • Nervousness
  • Anxiety
  • Insomnia
  • Somnolence
  • Tremor
  • Headache
  • Dizziness
  • Palpitations
  • Tachycardia (high heart rate)
  • Abdominal pain
  • Dyspepsia (indigestion)
  • Diarrhea
  • Constipation
  • Dry mouth
  • Hyperhidrosis (excess sweating)
  • Asthenia (weakness)
  • Malaises
  • Sexual dysfunction (including delayed ejaculation, erectile dysfunction, decreased libido, etc.)
Uncommon (0.1–1% incidence) adverse effects
  • Hallucination
  • Confusional state
  • Extrapyramidal side effects (e.g. dystonia, parkinsonism, tremor, etc.)
  • Orthostatic hypotension
  • Cutaneous hypersensitivity reactions (e.g. oedema [buildup of fluid in the tissues], rash, pruritus)
  • Arthralgia
Rare (0.01–0.1% incidence) adverse effects
  • Mania
  • Seizures
  • Abnormal hepatic (liver) function
  • Photosensitivity (being abnormally sensitive to light)
  • Galactorrhoea (expulsion of breast milk unrelated to pregnancy or breastfeeding)
Unknown frequency adverse effects

Interactions[edit]

Fluvoxamine inhibits the following cytochrome P450 enzymes:[22][23][24][25][26][27][28][29]
By so doing, fluvoxamine can increase serum concentration of the substrates of these enzymes.[22]
Fluvoxamine has been observed to increase serum concentrations of mirtazapine, which is mainly metabolized by CYP1A2, CYP2D6, and CYP3A4, by 3- to 4-fold in humans.[30]Caution and adjustment of dosage as necessary are warranted when combining fluvoxamine and mirtazapine.[30]

Pharmacology[edit]

Binding profile[31]
SiteKi (nM)
SERT11
NET1,119
5-HT2C5,786
Îħ1-adrenergic1,288
σ136
Fluvoxamine is a potent selective serotonin reuptake inhibitor with around 100-fold affinity for the serotonin transporter over the norepinephrine transporter.[23] It has negligible affinity for the dopamine transporter or any other site, with the sole exception of the Ïƒ1 receptor.[32] It behaves as a potent agonist at this receptor and has the highest affinity (36 nM) of any SSRI for doing so.[32] This may contribute to its antidepressant and anxiolytic effects and may also afford it some efficacy in treating the cognitive symptoms of depression.[17]

History[edit]

Luvox (fluvoxamine) 100 mg film-coated scored tablets
Fluvoxamine was developed by Kali-Duphar,[33] part of Solvay Pharmaceuticals, Belgium, now Abbott Laboratories, and introduced as Floxyfral in Switzerland and Solvay in West Germany in 1983.[33] It was approved by the FDA on 5 Dec, 1994 and introduced as Luvox in the US.[34] In India, it is available, among several other brands, as Uvox by Abbott.[35] It was one of the first SSRI antidepressants to be launched, and is prescribed in many countries to patients with major depression.[36] It was the first SSRI, a non-TCA drug, approved by the U.S. FDA specifically for the treatment of OCD.[37] At the end of 1995, more than ten million patients worldwide had been treated with fluvoxamine.[38]Fluvoxamine was the first SSRI to be registered for the treatment of obsessive compulsive disorder in children by the FDA in 1997.[39] In Japan, fluvoxamine was the first SSRI to be approved for the treatment of depression in 1999[40] and was later in 2005 the first drug to be approved for the treatment of social anxiety disorder.[41] Fluvoxamine was the first SSRI approved for clinical use in the United Kingdom.[42]The largest manufacturer of fluvoxamine, drug substance, is Synthon BV (The Netherlands).

See also[edit]

References[edit]

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  3. Jump up^ "FDA Advisory Committee Recommends Luvox (Fluvoxamine) Tablets for Obsessive Compulsive Disorder," PRNewswire, 10/18/93
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  38. Jump up^ Fluvoxamine Product Monograph. 1999. Missing or empty |title= (help)
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  40. Jump up^ Higuchi, T; Briley, M (February 2007). "Japanese experience with milnacipran, the first serotonin and norepinephrine reuptake inhibitor in Japan". Neuropsychiatric Disease and Treatment. 3 (1): 41–58. doi:10.2147/nedt.2007.3.1.41. PMC 2654524 Freely accessible. PMID 19300537.
  41. Jump up^ "Solvay's Fluvoxamine maleate is first drug approved for the treatment of social anxiety disorder in Japan". http://www.solvaypress.com/pressreleases/0,,33713-2-83,00.htm.External link in |journal= (help)
  42. Jump up^ Walker, R; Whittlesea, C, eds. (2007) [1994]. Clinical Pharmacy and Therapeutics (4th ed.). Edinburgh: Churchill Livingstone Elsevier. ISBN 978-0-7020-4293-5.
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