Viloxazine



Viloxazine
Systematic (IUPAC) name
2-[(2-ethoxyphenoxy)methyl]morpholine[1]
Identifiers
CAS number 46817-91-8
46817-91-8[2]
35604-67-2 (HCl salt)[3]
ATC code N06AX09
PubChem 5666
Chemical data
O3 
Mol. mass 237.295 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion Renal[4]
Therapeutic considerations
Pregnancy cat.

?

Legal status

Not a controlled substance

Routes Oral, intravenous (infusion)[5]

Viloxazine (Emovit®, Vivalan®, Vivarint®, Vicilan®) is a isomers, the S(-)-isomer being five times as pharmacologically active as the R(+)-isomer.[8]

Uses

Approved

Viloxazine hydrochloride was approved in Italy, Belgium, the United States, England, Ireland, Germany, Portugal, Spain, the former Yugoslavia, France,[9] Slovakia,[10] for the treatment of clinical depression.[11]

Unapproved/off-Label/investigational

Viloxazine has undergone two randomized controlled trials for nocturnal enuresis (bed-wetting) in children, both of those times versus imipramine.[12],[13] By 1990, it was seen as a less cardiotoxic alternative to imipramine, and to be especially effective in heavy sleepers.[14]

In narcolepsy, viloxazine has been shown to suppress auxiliary symptoms such as cataplexy and also abnormal sleep-onset REM[15] without really improving daytime somnolence.[16]

Viloxazine has also been studied for the treatment of alcoholism, with some success.[17]

While viloxazine may be effective in clinical depression, it did relatively poorly in a double-blind randomized controlled trial versus amisulpride in the treatment of dysthymia, according to Leon and colleagues at the University of Valle in Colombia.[18]

Mechanism of action

In 1976, Lippman and Pugsley reported that viloxazine, like serotonin, while its reuptake inhibition was comparable to that of desipramine (i.e., very weak), viloxazine did potentiate serotonin-mediated brain functions in a manner similar to amitriptyline and imipramine, which are relatively potent inhibitors of serotonin reuptake.[19] Unlike any of the other drugs tested, it did not exhibit any anticholinergic effects.[20]

It is also known to up-regulate GABAB receptors in the frontal cortex.[21]

Side effects

Side effects include nausea, vomiting, insomnia, loss of appetite, increased erythrocyte sedimentation, EKG and transaminases, seizure,[22] (there were three cases worldwide, and most animal studies (and clinical trials that included epilepsy patients) indicated the presence of anticonvulsant properties, so is not completely contraindicated in epilepsy[23]), and increased libido.[24]

Drug interactions

Viloxazine is known to increase plasma levels of theophylline and decrease its clearance from the body,[26] sometimes resulting in accidental overdose of theophylline.[27]

References

  1. ^  SID 180462-- PubChem Substance Summary. Retrieved on 5 November, 2005.
  2. ^  MEDLINE subject headings for Viloxazine. Retrieved on 5 November, 2005.
  3. ^  Biam (1999) VILOXAZINE CHLORHYDRATE, MORPHOLINES [online] Available from: http://www.biam2.org/www/Sub3399.html Accessed on 5 November 2005. (French)
  4. ^  Case DE, Reeves PR (1975). "The disposition and metabolism of I.C.I. 58,834 (viloxazine) in humans.". Xenobiotica 5 (2): 113-29. PMID 1154799. List of Library Holdings Worldwide
  5. ^  Bouchard JM, Strub N, Nil R (1997). "Citalopram and viloxazine in the treatment of depression by means of slow drop infusion. A double-blind comparative trial.". Journal of Affective Disorders 46 (1): 51-8. PMID 9387086. Fulltext options List of Library Holdings Worldwide
  6. ^  【合法】個人輸入代行薬【未認可】 (The relevant section is English)
  7. ^  Muller-Oerlinghausen B, Ruther E. "Clinical profile and serum concentration of viloxazine as compared to amitriptyline." Pharmakopsychiatr Neuropsychopharmakol. 1979 Jul;12(4):321-37. PMID 386390
  8. ^  Danchev ND, Rozhanets VV, Zhmurenko LA, Glozman OM, Zagorevskii VA (1984). "[Behavioral and radioreceptor analysis of viloxazine stereoisomers]". Biulleten' Eksperimental'noi Biologii i Meditsiny 97 (5): 576-8. [Article in Russian] PMID 6326891 List of Library Holdings Worldwide
  9. ^  Biam (1999) see Biam, 1999.
  10. ^  AstraZeneca Slovensko (2000). VIVALAN tbl obd. Retrieved on 2005-11-05.
  11. ^  AstraZeneca International (2003). Vivalan (viloxazine hydrochloride). Retrieved on 2005-11-06.
  12. ^  Attenburrow AA, Stanley TV, Holland RP (1984). "Nocturnal enuresis: a study.". The Practitioner 228 (1387): 99-102. PMID 6364124. List of Library Holdings Worldwide
  13. ^  Yurdakok M, Kinik E, Guvenc H, Beduk Y (1987). "Viloxazine versus imipramine in the treatment of enuresis.". The Turkish Journal of Pediatrics 29 (4): 227-30. PMID 3332732. List of Library Holdings Worldwide
  14. ^  Libert MH (1990). "[The use of viloxazine in the treatment of primary enuresis]". Acta Urologica Belgica 58 (1): 117-22. [Article in French] PMID 2371930 List of Library Holdings Worldwide
  15. ^  Guilleminault C, Mancuso J, Salva MA, Hayes B, Mitler M, Poirier G, Montplaisir J (1986). "Viloxazine hydrochloride in narcolepsy: a preliminary report.". Sleep 9 (1 Pt 2): 275-9. PMID 3704453. List of Library Holdings Worldwide
  16. ^  Mitler MM, Hajdukovic R, Erman M, Koziol JA (1990). "Narcolepsy.". Journal of Clinical Neurophysiology 7 (1): 93-118. PMID 1968069. List of Library Holdings Worldwide
  17. ^  Altamura AC, Mauri MC, Girardi T, Panetta B (1990). "Alcoholism and depression: a placebo controlled study with viloxazine.". International journal of clinical pharmacology research 10 (5): 293-8. PMID 2079386. List of Library Holdings Worldwide
  18. ^  Leon CA, Vigoya J, Conde S, Campo G, Castrillon E, Leon A (1994). "[Comparison of the effect of amisulpride and viloxazine in the treatment of dysthymia]". Acta Psiquiatrica y Psicologica de America Latina 40 (1): 41-9. [Article in Spanish] PMID 8053353 List of Library Holdings Worldwide
  19. ^  Lippman W, Pugsley TA. (1976). "Effects of viloxazine, an antidepressant agent, on biogenic amine uptake mechanisms and related activities.". Canadian Journal of Physiology and Pharmacology 54 (4): 494-509. PMID 974878. List of Library Holdings Worldwide
  20. ^  see Lippman and Pugsley, 1976.
  21. ^  Lloyd KG, Thuret F, Pilc A (1985). "Upregulation of gamma-aminobutyric acid (GABA) B binding sites in rat frontal cortex: a common action of repeated administration of different classes of antidepressants and electroshock". Journal of Pharmacology & Experimental Therapeutics 235 (1): 191-9. PMID 2995646. List of Library Holdings Worldwide
  22. ^  see Biam, 1999.
  23. ^  Edwards JG, Glen-Bott M (1984). "Does viloxazine have epileptogenic properties?". Journal of Neurology, Neurosurgery, and Psychiatry 47 (9): 960-4. PMID 6434699. List of Library Holdings Worldwide
  24. ^  Chebili S, Abaoub A, Mezouane B, Le Goff JF (1998). "[Antidepressants and sexual stimulation: the correlation]". L'Encephale 24 (3): 180-4. [Article in French] PMID 9696909 List of Library Holdings Worldwide
  25. ^  F Pisani, A Fazio, C Artesi, M Russo, R Trio, G Oteri, E Perucca and R Di Perri (1992). "Elevation of plasma phenytoin by viloxazine in epileptic patients: a clinically significant drug interaction". Journal of Neurology, Neurosurgery, and Psychiatry 55 (2): 126-127. PMID 1538217. List of Library Holdings Worldwide
  26. ^  Perault MC, Griesemann E, Bouquet S, Lavoisy J, Vandel B (1989). "A study of the interaction of viloxazine with theophylline.". Therapeutic Drug Monitoring 11 (5): 520-2. PMID 2815226. List of Library Holdings Worldwide
  27. ^  Laaban JP, Dupeyron JP, Lafay M, Sofeir M, Rochemaure J, Fabiani P (1986). "Theophylline intoxication following viloxazine induced decrease in clearance.". European Journal of Clinical Pharmacology 30 (3): 351-3. PMID 3732375. List of Library Holdings Worldwide


v • d • e
Psychoanaleptics: RIs
S RI Trazodone)
A RI Maprotiline)
D RI Amineptine)
SN RI Venlafaxine
ND RI Bupropion
SND RI Nomifensine
Mirtazapine)
 
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