Reboxetine mesylate

Absorption

Reboxetine is rapidly and extensively absorbed following oral administration.

Toxicity

Reports of seizures (rare) have been reported

The Uses of Reboxetine mesylate

Antidepressant (selective noradrenaline reuptake inhibitor).

The Uses of Reboxetine mesylate

Reboxetine can be used in biological study of the involvement of monoaminergic neurotransmission in the antidepressant-like action of scopolamine in the tail suspension test.

Background

Reboxetine is an antidepressant drug used in the treatment of clinical depression, panic disorder and ADD/ADHD. Its mesylate (i.e. methanesulfonate) salt is sold under tradenames including Edronax, Norebox, Prolift, Solvex, Davedax or Vestra. Reboxetine has two chiral centers, but it only exists as two enantiomers, (R,R)-(-)- and (S,S)-(+)-reboxetine.

Indications

For the treatment of clinical depression.

Definition

ChEBI: Reboxetine is an aromatic ether.

brand name

Edronax (Pharmacia & Upjohn).

Biological Activity

Potent and selective inhibitor of noradrenalin uptake (K i values are 1.1, 129 and > 10000 nM for rat NET, SERT and DAT respectively). Displays > 1000-fold selectivity over α -adrenoceptors, 5-HT, dopamine and muscarinic ACh receptors. Orally active, clinically used antidepressant.

Pharmacokinetics

Reboxetine is a selective noradrenaline reuptake inhibitor (NaRI), the first drug of new antidepressant class. Reboxetine is an a-ariloxybenzyl derivative of morpholine. Reboxetine is primarily used to treat depression but has also been found useful in the treatment of narcolepsy and panic disorders.

Metabolism

Reboxetine is metabolized by dealkylation, hydroxylation and oxidation followed by glucuronide or sulphate conjugation. It is metabolized by the cytochrome P450 CYP isoenzyme 3A4.