Viloxazine

Viloxazine (Emovit®, Vivalan®, Vivarint®, Vicilan®) is a bicyclic antidepressant morpholine derivative that inhibits the reuptake of norepinephrine. It is a racemic compound with two isomers, the S(-)-isomer being five times as pharmacologically active as the R(+)-isomer.

Uses

Approved

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

Unapproved/off-Label/investigational

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

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

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

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.

Mechanism of action

In 1976, Lippman and Pugsley reported that viloxazine, like imipramine, inhibited norepinephrine reuptake in the hearts of rats and mice; unlike imipramine, (or desipramine or amitriptyline, for that matter) it did not block reuptake of norepinephrine in neither the medullae nor the hypothalami of rats. As for 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. Unlike any of the other drugs tested, it did not exhibit any anticholinergic effects.

It is also known to up-regulate GABA_B receptors in the frontal cortex.

Side effects

Side effects include nausea, vomiting, insomnia, loss of appetite, increased erythrocyte sedimentation, EKG and EEG anomalies, epigastric pain, diarrhea, constipation, vertigo, orthostatic hypotension, edema of the lower extremities, dysarthria, tremor, psychomotor agitation, mental confusion, inappropriate secretion of antidiuretic hormone, increased transaminases, seizure, (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), and increased libido.

Drug interactions

Viloxazine is known to increase plasma levels of phenytoin by an average of 37%. It is also known to significantly increase plasma levels of theophylline and decrease its clearance from the body, sometimes resulting in accidental overdose of theophylline.

References

Biam (1999) VILOXAZINE CHLORHYDRATE, MORPHOLINES ^* Available from: http://www.biam2.org/www/Sub3399.html Accessed on 5 November 2005. (French)
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【合法】個人輸入代行薬【未認可】 (The relevant section is English)
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
in Russian PMID 6326891 List of Library Holdings Worldwide
Biam (1999) see Biam, 1999.
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in French PMID 2371930 List of Library Holdings Worldwide
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in Spanish PMID 8053353 List of Library Holdings Worldwide
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see Lippman and Pugsley, 1976.
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see Biam, 1999.
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in French PMID 9696909 List of Library Holdings Worldwide
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Bicyclic antidepressants

Viloxazin | Viloxacina | Viloxazina | 维洛沙秦