Ziprasidone is a novel antipsychotic drug. It has high affinity for se
rotonin 5-HT2 and dopamine D-2 receptors in vitro, with an Ii-fold hig
her affinity for 5-HT2 than for D-2 receptors, suggestive of a low pot
ential for inducing motor disturbance [including extrapyramidal sympto
ms (EPS)]. The effects of ziprasidone in receptor binding studies refl
ected its in vitro pharmacology, with more potent effects against 5-HT
2 receptor-than against D-2 receptor-mediated behaviour. Because zipra
sidone inhibits serotonin (5-hydroxytryptamine; 5-HT) and noradrenalin
e (norepinephrine) reuptake, it may have anxiolytic and antidepressant
effects. Data from phase II and III clinical trials have shown zipras
idone to be effective in reducing the positive and negative symptoms o
f, and depression associated with, schizophrenia, and in reducing anxi
ety in patients about to undergo dental surgery. Ziprasidone was gener
ally well tolerated in phase II and III clinical trials, with somnolen
ce and nausea being the most frequently reported adverse events in pla
cebo-controlled studies. Motor disturbances, including EPS, were infre
quently observed.