Sibutramin udøver hovedsagelig sin terapeutiske effekt via dets aktive sekundære og primære aminmetabolitter (metabolit 1 og metabolit 2), som hæmmer reabsorption af noradrenalin, serotonin (5- hydroxytryptamin, 5- HT) og dopamin.
Treatment should consist of the general measures employed in the management of overdosing, such as keeping airways unobstructed, monitoring of cardiovascular functions and general symptomatic and supportive measures.