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NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Indole derivatives
ziprasidone
N05AE04
Forms & Strengths
- Capsules: 20 mg, 40 mg, 60 mg, 80 mg
- Intramuscular injection: 20 mg/mL
Adult Dosing
- Schizophrenia: 20 mg twice daily with food, titrating up to 40-80 mg twice daily; maximum 160 mg/day
- Acute Bipolar Mania: 40 mg twice daily on day 1, then 40-80 mg twice daily on subsequent days; maximum 80 mg twice daily
- Acute Agitation (IM): 10 mg to 20 mg as a single dose; max 40 mg/day (10 mg every 2 hours or 20 mg every 4 hours)
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of schizophrenia
- Acute treatment of manic or mixed episodes associated with bipolar disorder (monotherapy)
- Acute agitation in schizophrenia (intramuscular)
Mechanism of Action
- Atypical antipsychotic agent
- High affinity antagonism at dopamine D2 and serotonin 5-HT2A receptors
- Moderate antagonism at serotonin 5-HT1D and 5-HT2C receptors
- Moderate agonist activity at serotonin 5-HT1A receptors
- Moderate inhibition of serotonin and norepinephrine reuptake
Contraindications
- Known history of QT prolongation or congenital long QT syndrome
- Recent acute myocardial infarction or uncompensated heart failure
- Concurrent administration of other drugs that prolong the QT interval
- Known hypersensitivity to ziprasidone
Adverse Reactions
- Somnolence
- Extrapyramidal symptoms
- Dizziness
- Nausea
- Respiratory tract infection
- QTc interval prolongation
- Orthostatic hypotension
- Weight gain
- Neuroleptic malignant syndrome
Drug Interactions
- Class IA and III antiarrhythmics (contraindicated due to additive QT prolongation)
- CYP3A4 inhibitors (e.g., ketoconazole) may increase ziprasidone concentration
- CYP3A4 inducers (e.g., carbamazepine) may decrease ziprasidone concentration
- CNS depressants and alcohol (additive sedation and impairment)
- Levodopa and dopamine agonists (pharmacodynamic antagonism)
Curated Content: Needs Vetting Before Put to Clinical Use