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Ziprasidone (marketed as Geodon, Zeldox) was the fifth
atypical antipsychotic to gain FDA approval (February 2001).
Ziprasidone is Food and Drug Administration (FDA) approved
for the treatment of schizophrenia, and the intramuscular
injection form of ziprasidone is approved for acute agitation
in schizophrenic patients. Ziprasidone has also received
approval for acute treatment of mania associated with bipolar
disorder. The brand name Geodon has been suggested to bring
to mind the phrase 'down (don) to earth (geo)' referring
to the goals of the medication.
The oral form of ziprasidone is the hydrochloride salt,
ziprasidone hydrochloride. The intramuscular form, on the
other hand, is the mesylate salt, ziprasidone mesylate trihydrate,
and is provided as a lyophilized powder.

Pharmacology
Ziprasidone has a high affinity for dopamine, serotonin, and
alpha-adrenergic receptors and a medium affinity for histaminic
receptors. Ziprasidone also displays some inhibition of synaptic
reuptake of serotonin and norepinephrine, although the clinical
significance of this is unknown. The mechanism of action of
ziprasidone is unknown. However it has been theorized that
its antipsychotic activity is mediated primarily by antagonism
at dopamine receptors, specifically D2. Serotonin antagonism
may also play a role in the effectiveness of ziprasidone,
but the significance of 5-HT2A antagonism is debated among
researchers. Ziprasidone has perhaps the most selective affinity
for 5-HT2A receptors relative to D2 and 5-HT2C receptors of
any neuroleptic, even greater than that of risperidone. Antagonism
at histaminic and alpha adrenergic receptors likely explains
some of the side effects of ziprasidone, such as sedation
and orthostasis.
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