Fluvoxamine

Fluvoxamine
Clinical data
Trade namesLuvox, others
AHFS/Drugs.comMonograph
MedlinePlusa695004
License data
Pregnancy
category
Routes of
administration
By mouth
Drug classSelective serotonin reuptake inhibitor (SSRI)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability53% (90% confidence interval: 44–62%)[3]
Protein binding77–80%[3][4]
MetabolismLiver (primarily O-demethylation)[5]
Major: CYP2D6 or CYP1A2[5][6][3]
Minor: CYP3A4, CYP2C19, and/or CYP1A2[6][3]
Elimination half-life12–13 hours (single dose), 22 hours (repeated dosing)[3]
ExcretionKidney (98%; 94% as metabolites, 4% as unchanged drug)[3]
Identifiers
  • 2-{[(E)-{5-Methoxy-1-[4-(trifluoromethyl)phenyl] pentylidene}amino]oxy}ethanamine[7]
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.125.476 Edit this at Wikidata
Chemical and physical data
FormulaC15H21F3N2O2
Molar mass318.340 g·mol−1
3D model (JSmol)
  • FC(F)(F)c1ccc(\C(=N\OCCN)CCCCOC)cc1
  • InChI=1S/C15H21F3N2O2/c1-21-10-3-2-4-14(20-22-11-9-19)12-5-7-13(8-6-12)15(16,17)18/h5-8H,2-4,9-11,19H2,1H3/b20-14+ checkY
  • Key:CJOFXWAVKWHTFT-XSFVSMFZSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Fluvoxamine, sold under the brand name Luvox among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class.[8] It is primarily used to treat major depressive disorder and, perhaps more-especially, obsessive–compulsive disorder (OCD),[9] but is also used to treat anxiety disorders[10] such as panic disorder, social anxiety disorder, and post-traumatic stress disorder.[11][12][13]

Fluvoxamine's side-effect profile is similar to that of other SSRIs. Common adverse effects include constipation, gastrointestinal problems, headache, anxiety, irritation, sexual problems, dry mouth, sleep problems and an increased risk of suicide at the start of treatment. These effects appear to be significantly weaker than with other SSRIs, with the exception of gastrointestinal side-effects.[14]

Fluvoxamine appears to be more tolerable than other SSRIs, particularly with respect to cardiovascular complications.[15] Compared to escitalopram and sertraline, fluvoxamine's gastrointestinal profile may be less intense,[16] often being limited to nausea.[12] Mosapride has demonstrated efficacy in treating fluvoxamine-induced nausea.[17] It is also advised practice to divide total daily doses of fluvoxamine greater than 100 milligrams, with the higher fraction being taken in the evening (e.g., 50 mg at the beginning of the waking day and 200 mg at bedtime). In any case, high starting daily doses of fluvoxamine rather than the recommended gradual titration (starting at 50 milligrams and gradually titrating, up to 300 if necessary) may increase the likelihood of nausea.[18]

It is on the World Health Organization's List of Essential Medicines.[19]

  1. ^ Use During Pregnancy and Breastfeeding
  2. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  3. ^ a b c d e f Cite error: The named reference LUVOX was invoked but never defined (see the help page).
  4. ^ van Harten J (March 1993). "Clinical pharmacokinetics of selective serotonin reuptake inhibitors". Clinical Pharmacokinetics. 24 (3): 203–220. doi:10.2165/00003088-199324030-00003. PMID 8384945. S2CID 84636672.
  5. ^ a b Cite error: The named reference AltamuraCaldiroliBuoli2015 was invoked but never defined (see the help page).
  6. ^ a b Cite error: The named reference Wyska2019 was invoked but never defined (see the help page).
  7. ^ "Luvox". ChemSpider. Royal Society of Chemistry. Archived from the original on 15 November 2013. Retrieved 21 October 2013.
  8. ^ "Fluvoxamine Maleate Information". U.S. Food and Drug Administration (FDA). 15 July 2015. Archived from the original on 29 November 2019. Retrieved 28 November 2019.
  9. ^ McCain JA (July 2009). "Antidepressants and suicide in adolescents and adults: a public health experiment with unintended consequences?". P & T. 34 (7): 355–378. PMC 2799109. PMID 20140100.
  10. ^ "Fluvoxamine for the treatment of anxiety disorders in children and adolescents. The Research Unit on Pediatric Psychopharmacology Anxiety Study Group". The New England Journal of Medicine. 344 (17): 1279–1285. April 2001. doi:10.1056/NEJM200104263441703. PMID 11323729.
  11. ^ Figgitt DP, McClellan KJ (October 2000). "Fluvoxamine. An updated review of its use in the management of adults with anxiety disorders". Drugs. 60 (4): 925–954. doi:10.2165/00003495-200060040-00006. PMID 11085201. S2CID 265712201.
  12. ^ a b Irons J (December 2005). "Fluvoxamine in the treatment of anxiety disorders". Neuropsychiatric Disease and Treatment. 1 (4): 289–299. PMC 2424117. PMID 18568110.
  13. ^ Asnis GM, Hameedi FA, Goddard AW, Potkin SG, Black D, Jameel M, et al. (August 2001). "Fluvoxamine in the treatment of panic disorder: a multi-center, double-blind, placebo-controlled study in outpatients". Psychiatry Research. 103 (1): 1–14. doi:10.1016/S0165-1781(01)00265-7. PMID 11472786. S2CID 40412606.
  14. ^ Vezmar, S. et al., « Pharmacokinetics and Efficacy of Fluvoxamine and Amitriptyline in Depression », J Pharmacol Sci, vol. 110, no 1, 2009, p. 98 – 104 (ISSN 1347-8648)
  15. ^ Westenberg HG, Sandner C (April 2006). "Tolerability and safety of fluvoxamine and other antidepressants". International Journal of Clinical Practice. 60 (4): 482–491. doi:10.1111/j.1368-5031.2006.00865.x. PMC 1448696. PMID 16620364.
  16. ^ Oliva V, Lippi M, Paci R, Del Fabro L, Delvecchio G, Brambilla P, et al. (July 2021). "Gastrointestinal side effects associated with antidepressant treatments in patients with major depressive disorder: A systematic review and meta-analysis". Progress in Neuro-Psychopharmacology & Biological Psychiatry. 109. Elsevier BV: 110266. doi:10.1016/j.pnpbp.2021.110266. PMID 33549697. S2CID 231809760.
  17. ^ Ueda N, Yoshimura R, Shinkai K, Terao T, Nakamura J (November 2001). "Characteristics of fluvoxamine-induced nausea". Psychiatry Research. 104 (3). Elsevier BV: 259–264. doi:10.1016/s0165-1781(01)00320-1. PMID 11728615. S2CID 38761139.
  18. ^ Ware MR (1 March 1997). "Fluvoxamine: A Review of the Controlled Trials in Depression". The Journal of Clinical Psychiatry. 58 (suppl 5). Physicians Postgraduate Press, Inc.: 15–23. ISSN 0160-6689. PMID 9184623. Archived from the original on 6 December 2022. Retrieved 1 December 2023.
  19. ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.