Drug reference

Ziprasidone

Atypical Antipsychotic · Antipsychotic

Atypical AntipsychoticAntipsychotic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

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Mechanism

Ziprasidone, like other antipsychotic agents, reduces dopaminergic neurotransmission primarily through D2 receptor blockade. It also acts on D2 autoreceptors. This D2 blockade is considered the primary therapeutic mechanism for its antipsychotic activity.

Indications

Acute agitation in agitated and minimally cooperative patients (IM administration)Acute maniaSchizophreniaPsychotic symptoms of delirium or dementia (off-label, with warning regarding increased mortality)Agitation and psychosis in AD (BPSD)Withdrawn patients with schizophreniaApathetic patients with schizophreniaNegative symptoms of schizophreniaElderly patients with psychosis

Dosing

Adult: For acute mania, doses are titrated rapidly to the maximum recommended dose over the first 24-72 hours of treatment; acute mania patients with psychosis often require doses close to or at the maximum FDA-approved dose. Intramuscular administration is an option for agitated and minimally cooperative patients.
Pediatric: Not specified
Geriatric: Lower doses are generally recommended for psychotic symptoms in delirium or dementia patients. Extrapyramidal neurological symptoms (EPS), orthostasis, and sedation are particularly problematic in this patient population.

Pharmacokinetics

Peak effect

6–8 h

Half-life

7.5 h

Bioavailability

60% (when given with food)

Protein binding

99.9 ± 0.08%

Metabolism

Aldehyde oxidase (66%), CYP3A4 (34%)

Excretion

<1%

Contraindications

Use in elderly dementia patients (increased mortality risk)

Side effects

Common

Extrapyramidal neurological symptoms (EPS) (less risk than haloperidol for IM form)OrthostasisSedationLow risk of metabolic adverse effectsparkinsonismfalls

Serious

Increased mortality in dementia-related psychosis (general warning for all antipsychotics)
Neuroleptic malignant syndrome
increased mortality in elderly dementia patients
higher risk of stroke and overall mortality in elderly patients with dementia-related psychosis