Used to treat schizophrenia and acute manic or mixed episodes associated with bipolar disorder.
Also used as maintenance treatment of bipolar disorder when added to lithium or valproate.
An atypical antipsychotic agent,
Intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients.
The oral form of ziprasidone is the hydrochloride salt, ziprasidone hydrochloride.
The intramuscular form is the mesylate salt, ziprasidone mesylate trihydrate, and is provided as a lyophilized powder.
Has a high affinity for dopamine, serotonin, and alpha-adrenergic receptors.
Has a moderate affinity for histamine receptors, where it is believed to act as an antagonist.
Mechanism of action is unknown.
Bioavailability of ziprasidone administered intramuscularly is 100%, and 60% when administered orally.
Intramuscular administration results in peak serum concentration at about 60 minutes.
The mean half-life ranges from two to five hours.
Absorption is not optimally achieved when administered without food.
Metabolizedin the liver by primarily by aldehyde oxidase.
Lesser metabolism occurs via cytochrome P450 3A4 (CYP3A4).
May slightly increases the QTc interval in some patients and increases the risk of a potentially lethal torsades de pointes.
Should be used cautiously in patients taking other medications likely to interact with ziprasidone or increase the QTc interval.
May cause activation into mania in some bipolar patients.
Adverse events include: chest pain, sedation, insomnia, orthostasis, neuroleptic malignant syndrome, akathisia, tardive dyskinesia, speech disorders, and impaired erectile function.
May cause hyperglycemia and insulin resistance.
Elderly patients with dementia-related psychosis treated with agent are at an increased risk of death, and is not approved for treating these patients.
In short-term schizophrenia clinical trials, 10% of treated patients experienced a weight gain of >7% of body weight vs 4% for placebo.
In short-term bipolar mania clinical trials, 4.9% of treated patients experienced a weight gain of >7% of body weight vs 3.3% for placebo.