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Fluvoxamine

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Fluvoxamine

Fluvoxamine
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
MedlinePlus
Pregnancy
category
  • C
Legal status
Routes of
administration
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]
Biological 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 Registry Number  Y
ATC code N06
PubChem CID:
IUPHAR/BPS
DrugBank  N
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  Y
ChEMBL  Y
Chemical data
Formula C15H21F3N2O2
Molecular mass 318.335
 N   

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.

Contents

  • Medical uses 1
  • Adverse effects 2
    • Interactions 2.1
  • Pharmacology 3
  • History 4
  • References 5
  • External links 6

Medical uses

Fluvoxamine's only FDA approved indication is in the treatment of OCD,[6] although in other countries (e.g. Australia,[7] UK[8] and Russian Federation[9]) 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.[10] The drug works long-term, and retains its therapeutic efficacy for at least a year.[11] It has also been found to possess some analgesic properties in line with other SSRIs and tricyclic antidepressants.[12][13][14]

Some evidence shows fluvoxamine may be a helpful adjunct in the treatment of schizophrenia, improving the depressive, negative, and cognitive symptoms of the disorder.[15] Its actions at the sigma receptor may afford it a unique advantage among antidepressants in treating the cognitive symptoms of schizophrenia.[16]

Adverse effects

Gastrointestinal side effects are more common in those receiving fluvoxamine than with other SSRIs.[17] Otherwise, fluvoxamine's side-effect profile is very similar to other SSRIs.[2][6][7][8][18][19]

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

Interactions

Fluvoxamine inhibits the following cytochrome P450 enzymes:[21][22][23][24][25][26][27][28]

By so doing, fluvoxamine can increase serum concentration of the substrates of these enzymes.[21]

Pharmacology

Fluvoxamine is a potent and selective serotonin reuptake inhibitor with around 100-fold affinity for the serotonin transporter over the norepinephrine transporter.[22] It has negligible affinity for the dopamine transporter or any other receptor, with the sole exception of the σ1 receptor.[29] It behaves as a potent agonist at this receptor and has the highest affinity of any SSRI for doing so.[29] This may contribute to its antidepressant and anxiolytic effects and may also afford it some efficacy in treating the cognitive symptoms of depression.[16]

History

Fluvoxamine was developed by Kali-Duphar,[30] part of Solvay Pharmaceuticals, Belgium, now Abbott Laboratories, and introduced as Floxyfral in Switzerland and Solvay in West Germany in 1983.[30] It was approved by the FDA on 5 Dec, 1994 and introduced as Luvox in the US.[31] In India, it is available, among several other brands, as Uvox by Abbott.[32] It was one of the first SSRI antidepressants to be launched, and is prescribed in many countries to patients with major depression.[33] It was the first SSRI, a nonTCA drug, approved by the U.S. FDA specifically for the treatment of OCD.[34] At the end of 1995, more than ten million patients worldwide had been treated with fluvoxamine.[35] Fluvoxamine was the first SSRI to be registered for the treatment of obsessive compulsive disorder in children by the FDA in 1997.[36] In Japan, fluvoxamine was the first SSRI to be approved for the treatment of depression in 1999[37] and was later in 2005 the first drug to be approved for the treatment of social anxiety disorder.[38] Fluvoxamine was the first SSRI approved for clinical use in the United Kingdom.[39]

References

  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.  
  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.  
  8. ^ a b Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press.  
  9. ^ "Summary of Full Prescribing Information: Fluvoxamine". Drug Registry of Russia (RLS) Drug Compendium (in Russian). Retrieved 21 March 2015. 
  10. ^ "US-FDA Fluvoxamine Product Insert". March 2005. 
  11. ^ 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.  
  12. ^ 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.  
  13. ^ 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.  
  14. ^ 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.  
  15. ^ Ritsner, MS (2013). Polypharmacy in Psychiatry Practice, Volume I. Springer Science+Business Media Dordrecht.  
  16. ^ 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.  
  17. ^ Brayfield, A, ed. (13 August 2013). Fluoxetine Hydrochloride. Martindale: The Complete Drug Reference (London, UK: Pharmaceutical Press). Retrieved 24 November 2013. 
  18. ^ Taylor, D; Paton, C; Shitij, K (2012). The Maudsley prescribing guidelines in psychiatry. West Sussex: Wiley-Blackwell.  
  19. ^ "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. 
  20. ^ "Top Ten Legal Drugs Linked to Violence". Time Inc. 7 January 2011. Retrieved 10 September 2014. 
  21. ^ a b Ciraulo, DA; Shader, RI (2011). Pharmacotherapy of Depression (2nd ed.). Springer. p. 49.  
  22. ^ a b Brunton, L; Chabner, B; Knollman, B (2010).  
  23. ^ P., Baumann (1996). "Pharmacokinetic-pharmacodynamic relationship of the Selective serotonin reuptake inhibitors". Clinical Pharmacokinetics 31 (6): 444–469.  
  24. ^ 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.  
  25. ^ DeVane, CL (1998). "Translational pharmacokinetics: current issues with newer antidepressants". Depression and Anxiety 8 (Suppl 1): 64–70.  
  26. ^ Bondy, Brigitta; Illja Spellmann (2007). "Pharmacogenetics of Antipsychotics: Useful For the Clinician?". Curr Opin Psychiatry (Medscape: Lippincott Williams & Wilkins) 20 (1): 126–130.  
  27. ^ 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.  
  28. ^ Waknine, Yael (April 13, 2007). "Prescribers Warned of Tizanidine Drug Interactions". Medscape News. Medscape. Retrieved 2008-02-01. 
  29. ^ 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.  
  30. ^ a b Sittig's Pharmaceutical Manufacturing Encyclopedia (PDF) (3rd ed.). William Andrew. 2008. p. 1699.  
  31. ^ "Drugs.com―Fluvoxamine". Retrieved 18 October 2013. 
  32. ^ "Brand Index―Fluvoxamine India". Archived from the original on 2013-10-18. Retrieved 18 October 2013. 
  33. ^ 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).  
  34. ^ "OCD Medication". Archived from the original on 2013-10-17. Retrieved 17 October 2013. 
  35. ^ Fluvoxamine Product Monograph. 1999. 
  36. ^ "Luvox Approved For Obsessive Compulsive Disorder in Children and Teens". http://www.pslgroup.com/dg/2261a.htm. 
  37. ^ 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.  
  38. ^ "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. 
  39. ^ Walker, R; Whittlesea, C, ed. (2007) [1994]. Clinical Pharmacy and Therapeutics (4th ed.). Edinburgh: Churchill Livingstone Elsevier.  

External links

  • Fluvoxamine consumer information from Drugs.com
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