viloxazine

237.29

237.29

256-281-7

DTXSID6057900

Colorless to light yellow

N - Nervous system

1.0942 (rough estimate)

176-179 °C

379.83°C (rough estimate)

1.5000 (estimate)

pKa 8.1 (Uncertain)

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 and mania, sweating, palpitation, tachycardia, increased and decreased blood pressure, pruritus and skin rashes.

In four placebo-controlled trials of viloxazine in children with ADHD, minor serum aminotransferase elevations occurred in 5% to 10% of recipients but were more than 2 times the upper limit of normal in less than 1%. In the preregistration trials, there were no instances of clinically apparent liver injury or serum aminotransferase elevations with jaundice attributable to viloxazine. Since its approval as therapy for depression in Europe more than 30 years ago and as therapy of ADHD in the United States in 2021, there have been no publications describing clinically apparent liver injury due to viloxazine. Furthermore, summaries of the efficacy and safety of viloxazine do not mention hepatic adverse events. Nevertheless, long term clinical experience with viloxazine in children is limited, and other SNRIs (such as atomoxetine) have been linked to rare instances of clinically apparent liver injury.

Indicated for the treatment of clinical depression.

Viloxazine is a selective norepinephrine reuptake inhibitor that is used in the therapy of attention deficit/hyperactivity disorder in children. Viloxazine has been associated with uncommon and mild serum enzyme elevations during therapy but not with occurrence of clinically apparent liver injury.

Drugs for ADHD

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). The S(-)-stereoisomer of viloxazine exhibits more potent pharmacological actions.

A structurally and mechanistically diverse group of drugs that are not tricyclics or monoamine oxidase inhibitors. The most clinically important appear to act selectively on serotonergic systems, especially by inhibiting serotonin reuptake. (See all compounds classified as Antidepressive Agents, Second-Generation.)|Drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. The tricyclic antidepressants (ANTIDEPRESSIVE AGENTS, TRICYCLIC) and amphetamines are among the therapeutically important drugs that may act via inhibition of adrenergic transport. Many of these drugs also block transport of serotonin. (See all compounds classified as Adrenergic Uptake Inhibitors.)

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. Increase in plasma drug concentration is dose-proportional.|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.

Viloxazine is thought to be extensively metabolized into 5-hydroxy derivative and glucuronidated phenol. Other detected metabolites include 4-hydroxy isomer and its glucuronide, together with the sulphate conjugates of the phenolic metabolites.

Elimination half life is approximately 3-4 hours.

Viloxazine inhibits noradrenaline uptake in rat and mouse heart tissue and has a weak effect on the uptake of 5-HT. In a docking study, the amino group of viloxazine points towards Asp75 in the drug binding pocket of the transporter and forms hydrogen bonds with Phe72, Asp75 and Phe317. The rest of the drug molecule forms hydrophobic interactions with other key residues in the binding pocket.

Emovit

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals