Fluvoxamine

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Not to be confused with Fluoxetine.
Fluvoxamine
Fluvoxamine2DACS.svg
Fluvoxamine3Dan.gif
Systematic (IUPAC) name
2-{[(E)-{5-Methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene}amino]oxy}ethanamine[1]
Clinical data
Trade names Faverin, Fevarin, Floxyfral, Luvox
AHFS/Drugs.com monograph
MedlinePlus a682275
Pregnancy cat.
  • C
Legal status
Routes Oral
Pharmacokinetic data
Bioavailability 53% (90% confidence interval: 44-62%)[2]
Protein binding 80%[2]
Metabolism Hepatic (via cytochrome P450 enzymes. Mostly via oxidative demethylation)[2]
Half-life 12-13 hours (single dose), 22 hours (repeated dosing)[2]
Excretion Renal (98%; 94% as metabolites, 4% as unchanged drug)[2]
Identifiers
CAS number 54739-18-3 YesY
ATC code N06AB08
PubChem CID 5324346
DrugBank DB00176
ChemSpider 4481878 YesY
UNII O4L1XPO44W YesY
KEGG D07984 YesY
ChEBI CHEBI:5138 YesY
ChEMBL CHEMBL814 YesY
Chemical data
Formula C15H21F3N2O2 
Mol. mass 318.335
 N (what is this?)  (verify)

Fluvoxamine (brand names: Faverin, Fevarin, Floxyfral, and Luvox) is a medication which functions as a selective serotonin reuptake inhibitor (SSRI) and σ1 receptor agonist. Fluvoxamine is used primarily for the treatment of obsessive-compulsive disorder (OCD),[3] and is also used to treat major depressive disorder (MDD), and anxiety disorders such as panic disorder and post-traumatic stress disorder (PTSD).[4] Fluvoxamine CR (controlled release) is approved to treat social anxiety disorder.[5]

The FDA has added a black box warning for this drug in reference to increased risks of suicidal thinking and behavior in young adults and children.

Medical uses[edit]

Fluvoxamine's only FDA approved indication is in the treatment of OCD,[6] although in other countries (e.g. Australia[7] and the UK[8]) it has indications for MDD, as well. Fluvoxamine has been found to be useful in the treatment of MDD, and anxiety disorders such as panic disorder, social anxiety disorder, post-traumatic stress disorder (PTSD), and obsessive-compulsive spectrum disorders. Fluvoxamine is indicated for children and adolescents with OCD.[9] The drug works long-term, and retains its therapeutic efficacy for at least a year.[10] It has also been found to possess some analgesic properties in line with other SSRIs and tricyclic antidepressants.[11][12][13]

Some evidence shows fluvoxamine may be a helpful adjunct in the treatment of schizophrenia, improving the depressive, negative, and cognitive symptoms of the disorder.[14] Its actions at the sigma receptor may afford it a unique advantage among antidepressants in treating the cognitive symptoms of schizophrenia.[15]

Adverse effects[edit]

Gastrointestinal side effects are more common in those receiving fluvoxamine than with other SSRIs.[16] Otherwise, fluvoxamine's side-effect profile is very similar to other SSRIs.[2][6][7][8][17][18]

Common (1-10% incidence) adverse effects
  • Nausea
  • Vomiting
  • Anorexia (weight loss)
  • Agitation
  • Nervousness
  • Anxiety
  • Insomnia
  • Somnolence
  • Tremor
  • Headache
  • Dizziness
  • Palpitations
  • Tachycardia (high heart rate)
  • Abdominal pain
  • Dyspepsia (indigestion)
  • Diarrhoea
  • 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
  • Hyperprolactinaemia (elevated plasma prolactin levels leading to galactorrhoea, amenorrhoea [cessation of menstrual cycles], etc.)
  • Bone fractures
  • Glaucoma
  • Mydriasis
  • Urinary incontinence
  • Urinary retention
  • Bed-wetting
  • Serotonin syndrome — a potentially fatal condition characterised by abrupt onset muscle rigidity, hyperthermia (elevated body temperature), rhabdomyolysis, mental status changes (e.g. coma, hallucinations, agitation), etc.
  • Neuroleptic malignant syndrome — practically identical presentation to serotonin syndrome except with a more prolonged onset
  • Akathisia — a sense of inner restlessness that presents itself with the inability to stay still
  • Paraesthesia
  • Dysgeusia
  • Haemorrhage
  • Withdrawal symptoms
  • Weight changes
  • Suicidal ideation and behaviour
  • Violence towards others [19]
  • Hyponatraemia
  • Syndrome of inappropriate antidiuretic hormone secretion

Interactions[edit]

Fluvoxamine inhibits the following cytochrome P450 enzymes:[20][21][22][23][24][25][26][27]

By so doing, fluvoxamine can increase serum concentration of the substrates of these enzymes.[20]

Pharmacology[edit]

Fluvoxamine is a potent and selective serotonin reuptake inhibitor with around 100-fold affinity for the serotonin transporter over the norepinephrine transporter.[21] It has negligible affinity for the dopamine transporter or any other receptor, with the sole exception of the σ1 receptor.[28] It behaves as a potent agonist at this receptor and has the highest affinity of any SSRI for doing so.[28] This may contribute to its antidepressant and anxiolytic effects and may also afford it some efficacy in treating the cognitive symptoms of depression.[15]

History[edit]

Fluvoxamine was developed by Kali-Duphar,[29] part of Solvay Pharmaceuticals, Belgium, now Abbott Laboratories, and introduced as Floxyfral in Switzerland and Solvay in West Germany in 1983.[29] It was approved by the FDA on 5 Dec, 1994 and introduced as Luvox in the US.[30] In India, it is available, among several other brands, as Uvox by Abbott.[31] It was one of the first SSRI antidepressants to be launched, and is prescribed in many countries to patients with major depression.[32] It was the first SSRI, a nonTCA drug, approved by the U.S. FDA specifically for the treatment of OCD.[33] At the end of 1995, more than ten million patients worldwide had been treated with fluvoxamine.[34] Fluvoxamine was the first SSRI to be registered for the treatment of obsessive compulsive disorder in children by the FDA in 1997.[35] In Japan, fluvoxamine was the first SSRI to be approved for the treatment of depression in 1999[36] and was later in 2005 the first drug to be approved for the treatment of social anxiety disorder.[37] Fluvoxamine was the first SSRI approved for clinical use in the United Kingdom.[38]

References[edit]

  1. ^ "Luvox". ChemSpider. Royal Society of Chemistry. Retrieved 21 October 2013. 
  2. ^ a b c d e f "PRODUCT INFORMATION LUVOX®". TGA eBusiness Services. Abbott Australasia Pty Ltd. 15 January 2013. Retrieved 21 October 2013. 
  3. ^ "FDA Advisory Committee Recommends Luvox (Fluvoxamine) Tablets for Obsessive Compulsive Disorder," PRNewswire, 10/18/93
  4. ^ Karen J. McClellan, David P. Figgitt (Drugs October 2000). "Fluvoxamine. An Updated Review of its Use in the Management of Adults with Anxiety Disorders". Adis Drug Evaluation 60 (4): 925–954. doi:10.2165/00003495-200060040-00006.  Check date values in: |date= (help)
  5. ^ Stahl, S. Stahl's Essential Psychopharmacology: The Prescriber's Guide. Cambridge University Press. New York, NY. 2009. pp.215
  6. ^ a b "Fluvoxamine Maleate (fluvoxamine maleate) Tablet, Coated [Genpharm Inc.]". DailyMed. Genpharm Inc. October 2007. Retrieved 21 October 2013. 
  7. ^ a b Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3.  edit
  8. ^ a b Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. ISBN 978-0-85711-084-8.  edit
  9. ^ "US-FDA Fluvoxamine Product Insert". March 2005. 
  10. ^ Wilde MI, Plosker GL, Benfield P (November 1993). "Fluvoxamine. An updated review of its pharmacology, and therapeutic use in depressive illness". Drugs 46 (5): 895–924. doi:10.2165/00003495-199346050-00008. PMID 7507038. 
  11. ^ Kwasucki, J; Stepień A; Maksymiuk G; Olbrych-Karpińska B (2002). "Evaluation of analgesic action of fluvoxamine compared with efficacy of imipramine and tramadol for treatment of sciatica—open trial". Wiadomości Lekarskie 55 (1-2): 42–50. PMID 12043315. 
  12. ^ Schreiber, S; Pick CG (August 2006). "From selective to highly selective SSRIs: A comparison of the antinociceptive properties of fluoxetine, fluvoxamine, citalopram and escitalopram". European Neuropsychopharmacology 16 (6): 464–468. doi:10.1016/j.euroneuro.2005.11.013. PMID 16413173. 
  13. ^ Coquoz, D; Porchet HC; Dayer P (September 1993). "Central analgesic effects of desipramine, fluvoxamine, and moclobemide after single oral dosing: a study in healthy volunteers". Clinical Pharmacology and Therapeutics 54 (3): 339–344. doi:10.1038/clpt.1993.156. PMID 8375130. 
  14. ^ Ritsner, MS (2013). Polypharmacy in Psychiatry Practice, Volume I. Springer Science+Business Media Dordrecht. ISBN 9789400758056.  edit
  15. ^ a b Hindmarch, I; Hashimoto, K (April 2010). "Cognition and depression: the effects of fluvoxamine, a sigma-1 receptor agonist, reconsidered". Human Psychopharmacology: Clinical and Experimental 25 (3): 193–200. doi:10.1002/hup.1106. PMID 20373470. 
  16. ^ Brayfield, A, ed. (13 August 2013). Fluoxetine Hydrochloride. Martindale: The Complete Drug Reference (London, UK: Pharmaceutical Press). Retrieved 24 November 2013. 
  17. ^ Taylor, D; Paton, C; Shitij, K (2012). The Maudsley prescribing guidelines in psychiatry. West Sussex: Wiley-Blackwell. ISBN 978-0-470-97948-8.  edit
  18. ^ "Faverin 100 mg film-coated tablets - Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Abbott Healthcare Products Limited. 14 May 2013. Retrieved 21 October 2013. 
  19. ^ "Top Ten Legal Drugs Linked to Violence". Time Inc. 7 January 2011. Retrieved 10 September 2014. 
  20. ^ a b Ciraulo, DA; Shader, RI (2011). Pharmacotherapy of Depression (2nd ed.). Springer. p. 49. doi:10.1007/978-1-60327-435-7. ISBN 978-1-60327-435-7. 
  21. ^ a b Brunton, L; Chabner, B; Knollman, B (2010). Goodman and Gilman's The Pharmacological Basis of Therapeutics (12th ed.). New York: McGraw-Hill Professional. ISBN 978-0-07-162442-8.  edit
  22. ^ P., Baumann (1996). "Pharmacokinetic-pharmacodynamic relationship of the Selective serotonin reuptake inhibitors". Clinical Pharmacokinetics 31 (6): 444–469. doi:10.2165/00003088-199631060-00004. PMID 8968657. 
  23. ^ Gill HS, DeVane CL; Gill, HS (1997). "Clinical Pharmacokinetics of Fluvoxamine: applications to dosage regime design". Journal of Clinical Psychiatry 58 (Suppl 5): 7–14. PMID 9184622. 
  24. ^ DeVane, CL (1998). "Translational pharmacokinetics: current issues with newer antidepressants". Depression and Anxiety 8 (Suppl 1): 64–70. doi:10.1002/(SICI)1520-6394(1998)8:1+<64::AID-DA10>3.0.CO;2-S. PMID 9809216. 
  25. ^ Bondy, Brigitta; Illja Spellmann (2007). "Pharmacogenetics of Antipsychotics: Useful For the Clinician?". Curr Opin Psychiatry (Medscape: Lippincott Williams & Wilkins) 20 (1): 126–130. doi:10.1097/YCO.0b013e328017f69f. PMID 17278909. Retrieved 2008-02-01. 
  26. ^ Kroom, Lisa A. (10-01-2007). "Drug Interactions With Smoking". Am J Health-Syst Pharm. (Medscape: American Society of Health-System Pharmacists) 64 (18): 1917–1921. doi:10.2146/ajhp060414. PMID 17823102. Retrieved 2008-01-31.  Check date values in: |date= (help)
  27. ^ Waknine, Yael (April 13, 2007). "Prescribers Warned of Tizanidine Drug Interactions". Medscape News. Medscape. Retrieved 2008-02-01. 
  28. ^ a b "Sigma-1 receptors and selective serotonin reuptake inhibitors: clinical implications of their relationship". Central Nervous System Agents in Medicinal Chemistry 9 (3): 197–204. September 2009. doi:10.2174/1871524910909030197. PMID 20021354. 
  29. ^ a b Sittig's Pharmaceutical Manufacturing Encyclopedia (3rd ed.). William Andrew. 2008. p. 1699. ISBN 978-0815515265. Retrieved 17 October 2013. 
  30. ^ "Drugs.com―Fluvoxamine". Retrieved 18 October 2013. 
  31. ^ "Brand Index―Fluvoxamine India". Archived from the original on 2013-10-18. Retrieved 18 October 2013. 
  32. ^ Omori, IM; Watanabe N; Nakagawa A; Cipriani A; Barbui C; McGuire H; Churchill R; Furukawa TA (October 2013). "Fluvoxamine versus other anti-depressive agents for depression". Cochrane Database of Systematic Reviews (9). doi:10.1002/14651858.CD006114.pub2. Retrieved 14 October 2013. 
  33. ^ "OCD Medication". Archived from the original on 2013-10-17. Retrieved 17 October 2013. 
  34. ^ Fluvoxamine Product Monograph. 1999. 
  35. ^ "Luvox Approved For Obsessive Compulsive Disorder in Children and Teens". http://www.pslgroup.com/dg/2261a.htm. 
  36. ^ 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. PMID 19300537. 
  37. ^ "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. 
  38. ^ Walker, R; Whittlesea, C, ed. (2007) [1994]. Clinical Pharmacy and Therapeutics (4th ed.). Edinburgh: Churchill Livingstone Elsevier. ISBN 978-0-7020-4293-5.  edit

External links[edit]