Drug Guide
Ziprasidone Mesylate
Classification
Therapeutic: Antipsychotic, atypical
Pharmacological: Serotonin-dopamine antagonist, 5-HT2A receptor antagonist
FDA Approved Indications
- Schizophrenia
- Bipolar disorder (manic or mixed episodes)
Mechanism of Action
Ziprasidone works by antagonizing dopamine D2 and serotonin 5-HT2A receptors, which helps to balance neurotransmitters in the brain, reducing psychotic symptoms and mood swings.
Dosage and Administration
Adult: Initially 20 mg twice daily with food. Dose may be titrated based on response, up to 40-80 mg twice daily.
Pediatric: Not approved for pediatric use.
Geriatric: Start at lower doses due to increased sensitivity to side effects.
Renal Impairment: Adjust dosage based on clinical response and tolerability.
Hepatic Impairment: Use with caution; no specific dose adjustment recommended.
Pharmacokinetics
Absorption: Rapidly absorbed with food; bioavailability is enhanced when taken with food.
Distribution: Widely distributed; protein binding approximately 51%.
Metabolism: Primarily hepatic via aldehyde oxidase and CYP3A4 enzymes.
Excretion: Primarily fecal and urinary excretion.
Half Life: Approximately 7 hours.
Contraindications
- Hypersensitivity to ziprasidone or any component of the formulation.
- History of QT prolongation or congenital long QT syndrome.
Precautions
- Risk of QT prolongation, ventricular arrhythmias, or sudden death; use with caution in patients with cardiovascular disease, electrolyte disturbances, or those taking other QT-prolonging drugs.
- Pregnancy and lactation: Use only if clearly needed, weigh the benefits against risks.
Adverse Reactions - Common
- Drowsiness (Frequent)
- Dizziness (Frequent)
- Nausea (Frequent)
- Akathisia (Frequent)
Adverse Reactions - Serious
- QT prolongation, Torsades de Pointes (Rare)
- Neuroleptic Malignant Syndrome (Rare)
- Anaphylactic reactions (Rare)
Drug-Drug Interactions
- Other QT-prolonging agents (e.g., some antidepressants, antiarrhythmics)
- CYP3A4 inhibitors or inducers
- CNS depressants
Drug-Food Interactions
- Alcohol, which can increase sedative effects and impair cognition.
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor baseline and periodic EKGs, especially QT interval, electrolyte levels, mental status, and cardiovascular status.
Diagnoses:
- Risk for cardiac arrhythmias
- Impaired sensory perception
- Risk for falls
Implementation: Administer with food, monitor for signs of arrhythmia, educate patient on reporting symptoms such as palpitations or dizziness.
Evaluation: Assess for improvement in psychotic symptoms, mood stabilization, and absence of adverse cardiac effects.
Patient/Family Teaching
- Take medication with food to improve absorption.
- Do not discontinue abruptly.
- Be aware of symptoms like dizziness, fainting, or palpitations and report promptly.
- Avoid alcohol and other CNS depressants unless approved by healthcare provider.
Special Considerations
Black Box Warnings:
- Increased mortality in elderly patients with dementia-related psychosis.
Genetic Factors: No specific genetic testing required.
Lab Test Interference: May affect blood glucose measurements slightly due to hyperglycemia report.
Overdose Management
Signs/Symptoms: Somnolence, hypotension, QT prolongation, seizures.
Treatment: Supportive care, cardiac monitoring, activated charcoal if ingestion is recent, and magnesium sulfate or other measures for QT prolongation as needed.
Storage and Handling
Storage: Store at room temperature (20°C to 25°C), away from moisture, heat, and light.
Stability: Stable for up to 2 years in original container.