Description

Simple

Clinical

Overview

Viloxazine is a selective norepinephrine reuptake inhibitor (NRI) that was used in some European countries as an antidepressant drug. It structurally differs from conventional tri- or tetra-cyclic antidepressants and it does not produce sedative anticholinergic or adrenergic effects in man [1]. While displaying amphetamine-like CNS stimulant effects, there is little evidence of drug dependence from viloxazine therapy. Viloxazine hydrochloride is a common active ingredient in drug formulation. It was discovered and brought to market in 1976 by Imperial Chemical Industries and in early 2000's, it was withdrawn from the market.

Pharmacology

Indication

Indicated for the treatment of clinical depression.

Pharmacodynamic

Viloxazine is a selective noradrenaline reuptake inhibitor (NRI) with minimal inhibitory effect on the reuptake of 5-HT. It is also shown to upregulate the levels of GABA-B receptors in the rat frontal cortex. It is shown to form a complex with the human norepinephrine transporter (hNET) [ Read more

Mechanism of action

Viloxazine inhibits noradrenaline uptake in rat and mouse heart tissue and has a weak effect on the uptake of 5-HT [ Read more

Absorption

Viloxazine is rapidly and almost completely absorbed following oral administration. The peak plasma concentration (Cmax) ranges between 540 and 1,600 ng/mL and the mean time to reach Cmax is approximately 86 minutes [ Read more

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

Elimination half life is approximately 3-4 hours [ Read more

Route of elimination

Viloxazine is rapidly eliminated via urine and about 2% of the administered dose is recovered in the feces. About 12-15% of the total drug is eliminated as unchanged parent drug [ Read more

Toxicity

Common adverse effects are nausea and vomiting. Other side effects are dry mouth, dizziness, headache, drowsiness, sleep disturbances, bad taste, anorexia, heartburn and indigestion, constipation, diarrhoea, ataxia, tremor, dyskinesia, paraesthesia, confusion, restlessness, irritability, hypomania a... Read more

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Viloxazine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The risk or severity of adverse effects can be increased when Viloxazine is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of adverse effects can be increased when Viloxazine is combined with (S)-Warfarin.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Viloxazine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Viloxazine.
4-hydroxycoumarin
The risk or severity of adverse effects can be increased when Viloxazine is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when 4-Methoxyamphetamine is combined with Viloxazine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Viloxazine is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Viloxazine.
7-Nitroindazole
The risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Viloxazine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Viloxazine.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Viloxazine.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Viloxazine.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Viloxazine.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Viloxazine.
Abacavir
Abacavir may decrease the excretion rate of Viloxazine which could result in a higher serum level.
Acarbose
Acarbose may decrease the excretion rate of Viloxazine which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Viloxazine which could result in a higher serum level.
Acefylline
The metabolism of Acefylline can be decreased when combined with Viloxazine.
Acemetacin
Acemetacin may decrease the excretion rate of Viloxazine which could result in a higher serum level.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Viloxazine.
9 References
  1. 1 . Pinder RM, Brogden RN, Speight TM, Avery GS: Viloxazine: a review of its pharmacological properties and therapeutic efficacy in depressive illness. Drugs. 1977 Jun;13(6):401-21.PubMed: 324751
  2. 2 . Lippman W, Pugsley TA: Effects of viloxazine, an antidepressant agent, on biogenic amine uptake mechanisms and related activities. Can J Physiol Pharmacol. 1976 Aug;54(4):494-509.PubMed: 974878
  3. 3 . Sebjanic V, Grombein S: Viloxazine (Vivalan ICI) in depression: results of a field trial of 276 patients in neuropsychiatric practice. Adv Biochem Psychopharmacol. 1982;32:113-20.PubMed: 7046360
  4. 4 . Case DE, Reeves PR: The disposition and metabolism of I.C.I. 58,834 (viloxazine) in humans. Xenobiotica. 1975 Feb;5(2):113-29.PubMed: 1154799
  5. 5 . Thomare P, Bourin M, Kergueris MF, Ortega A, Larousse C: Effects of administration route on pharmacokinetics of viloxazine in the rabbit. Methods Find Exp Clin Pharmacol. 1992 Mar;14(2):125-9.PubMed: 1598024
  6. 6 . Kergueris MF, Bourin M, Ribeyrol M, Beneroso N, Normand YL, Larousse C: Comparative pharmacokinetic study of conventional and sustained-release viloxazine in normal volunteers. Neuropsychobiology. 1989;20(3):136-40.PubMed: 2761683
  7. 7 . Vandel B, Vandel S, Jounet JM, Blum D: Pharmacokinetics of viloxazine hydrochloride in man. Eur J Drug Metab Pharmacokinet. 1982 Jan-Mar;7(1):65-8.PubMed: 7067726
  8. 8 . Zheng G, Xue W, Wang P, Yang F, Li B, Li X, Li Y, Yao X, Zhu F: Exploring the Inhibitory Mechanism of Approved Selective Norepinephrine Reuptake Inhibitors and Reboxetine Enantiomers by Molecular Dynamics Study. Sci Rep. 2016 May 27;6:26883. doi: 10.1038/srep26883.PubMed: 27230580
  9. 9 . Danchev ND, Rozhanets VV, Zhmurenko LA, Glozman OM, Zagorevskii VA: [Behavioral and radioreceptor analysis of viloxazine stereoisomers]. Biull Eksp Biol Med. 1984 May;97(5):576-8.PubMed: 6326891