Levosulpiride is the levorotatory enantiomer of
sulpiride, a substituted
benzamide indicated as an
antipsychotic,
antidepressant,
antiemetic and antidyspeptic
drug, as well as for the treatment of
somatoform disorders. In vivo
sulpiride displays a number of
neuroleptic properties which it shares with all typical
neuroleptic drugs; however, it has also a number of divergent characteristics that set it apart as the principal compound of the so-called 'atypical
neuroleptic agents'. The main mechanism of action of
levosulpiride consists of blocking the D2 dopaminergic receptors, preferentially located on the presynaptic membranes in the dopaminergic pathways of the brain; this means that
sulpiride is a selective
autoreceptor blocker. The results of series of experimental trials conducted to evaluate the toxicologic characteristics of
levosulpiride are presented. Both the acute, subacute, chronic and local toxicity trials, and the studies on reproduction toxicity, mutagenic potential and oncogenic/carcinogenic potential, demonstrate that
levosulpiride is well tolerated by the animals tested (rats, mice, rabbits and dogs) at doses higher than those effective in human
therapy. Moreover, the findings from the experimental studies on
levosulpiride lead to exclude the toxicity from accumulation, tolerance, dependence or withdrawal syndrome. In conclusion, according to the evaluated preclinical studies,
levosulpiride shows pharmacotoxicologic properties which make it suitable for the management of diseases for which the
drug is indicated.