norfluoxetine

Norfluoxetine is the principal active metabolite of fluoxetine, a widely used selective serotonin reuptake inhibitor (SSRI) antidepressant. It is formed in the liver via demethylation of fluoxetine primarily by CYP2D6. Norfluoxetine retains significant pharmacological activity and, like its parent compound, acts primarily by inhibiting the serotonin transporter and thereby increasing synaptic serotonin concentrations. Its prolonged elimination half-life (typically 4 to 16 days) contributes to the long duration of effect for fluoxetine therapy. Norfluoxetine is pharmacologically active, with both antidepressant and serotonergic effects, but is not marketed as a stand-alone drug. It is relevant primarily as a metabolite observed in fluoxetine therapy, and is responsible for sustained SSRI activity after discontinuation of fluoxetine. Norfluoxetine can also act as a weak norepinephrine reuptake inhibitor and may have antagonist activity at the 5-HT2C receptor[5][6][7].

Other names

demethylfluoxetine