Butriptyline (Evadene, Evadyne, Evasidol, Centrolese) is a tricyclic antidepressant (TCA) which has been used in Europe since 1974. It is the isobutyl side chain homologue of amitriptyline and produces similar effects to it, but with less marked side effects like sedation and interactions with adrenergic drugs.
In vitro, butriptyline is a strong antihistamine and anticholinergic, moderate 5-HT2 and α1-adrenergic receptor antagonist, and weak serotonin reuptake inhibitor, with negligible affinity for the norepinephrine and dopamine transporters. These actions appear to confer a profile similar to that of iprindole and trimipramine with serotonin-blocking effects as the predominant mediator of mood-lifting efficacy.
However, in clinical trials, using similar doses, butriptyline was found to be even more effective than amitriptyline as an antidepressant, despite the fact that amitriptyline is much, much stronger as both a 5-HT2 antagonist and serotonin-norepinephrine reuptake inhibitor. As a result, it may be that butriptyline, in vivo, functions as a prodrug to a metabolite with more appreciable pharmacodynamics.
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