D. Marazziti - Volume 5, Settembre 1999, n.3
Testo Immagini Bibliografia Summary Riassunto Indice
Ruolo di un inibitore selettivo del
reuptake della noradrenalina, la reboxetina,
nella terapia della depressione
Role of a selective noradrenaline re-uptake
inhibitor, reboxetine
in the treatment of depression
Reboxetine, 2RS,aRS)-2—[a-(2-ethoxyphenoxy) benzyl)] mor-pholine methansulphonate, is the first non-tricyclic selective noradrenaline re-uptake inhibitor available in clinical practice. Reboxetine has no significant affinity for the serotonin or the dopamine transporter or adrenergic, cholinergic or histamine receptors; however, it down-regulates b-adrenoceptors earlier than other antidepressants, hence pointing at a shortened therapeutic latency, and increases acutely plasma normetanephrine, a noradrenaline metabolite. This drug, at an oral dose of 8-10 mg/die, proved to be more effective than placebo and comparable to 200 mg oral desipramine, 75-100 mg oral imipramine and 20-40 mg/die oral fluoxetine; however, side effects were less with reboxetine with respect to tricyclic antidepressants. Efficacy was shown in both short-term, 4-8 week trials, as well as in a 1-year follow-up study. Difficulty with urination, tachycardia, diaphoresis, dry mouth, sleep and erectile disturbances were observed with reboxetine more often than with placebo, whereas withdrawal effects were negligible. No interaction was shown with other antidepressants at the level of hepatic microsomal P450 isoenzymes. Reboxetine represents a safe and effective antidepressant testing on a modern basis the noradrenergic theory of depression.