Zipradon

Treatment of schizophrenia in adults. Acute treatment as monotherapy of manic or mixed episodes associated with bipolar I disorder. Maintenance treatment of bipolar I disorder as an adjunct to lithium or valproate in adults.

Ziprasidone binds with relatively high affinity to dopamine D2 and D3, serotonin 5HT2A, 5HT2C, 5HT1A, 5HT1D, and alpha1-adrenergic receptors, and with moderate affinity to the histamine H1 receptor. It is an antagonist at D2, 5HT2A, and 5HT1D receptors, and an agonist at the 5HT1A receptor. It also inhibits synaptic reuptake of serotonin and norepinephrine. It shows no appreciable affinity for the cholinergic muscarinic receptor.

Schizophrenia: Initiate at 20 mg twice daily. Daily dosage may be adjusted up to 80 mg twice daily. Dose adjustments should occur at intervals of not less than 2 days. The lowest effective dose should be used. Acute treatment of manic/mixed episodes of bipolar I disorder: Initiate at 40 mg twice daily. Increase to 60 mg or 80 mg twice daily on day 2. Subsequent adjustments should be based on tolerability and efficacy within the range of 40-80 mg twice daily. Maintenance treatment of bipolar I disorder as an adjunct to lithium or valproate: Continue at the same dose on which the patient was initially stabilized, within the range of 40-80 mg twice daily. Acute treatment of agitation associated with schizophrenia (intramuscular): 10-20 mg, up to a maximum of 40 mg per day. 10 mg doses may be given every 2 hours; 20 mg doses every 4 hours.

Schizophrenia: Somnolence, respiratory tract infection. Manic and Mixed Episodes Associated with Bipolar Disorder: Somnolence, extrapyramidal symptoms, dizziness, akathisia, abnormal vision, asthenia, vomiting. Intramuscular administration: Headache, nausea, somnolence.

Pregnancy Category C. Should be used during pregnancy only if the potential benefit justifies the potential risk, and under a physician's advice.

Pregnancy Category: C — always consult a doctor before taking during pregnancy.

Increased incidence of cerebrovascular adverse reactions (stroke, TIA) in elderly patients with dementia-related psychosis. May prolong the QT interval - avoid in patients with bradycardia, hypokalemia, hypomagnesemia, congenital QT prolongation, or in combination with other QT-prolonging drugs. Neuroleptic Malignant Syndrome (NMS) - a potentially fatal complex; discontinue immediately and monitor closely if it occurs. Severe cutaneous adverse reactions such as DRESS and Stevens-Johnson syndrome have been reported - discontinue if suspected. Tardive dyskinesia may develop acutely or chronically. Metabolic changes - hyperglycemia, dyslipidemia, and weight gain may occur; monitor regularly. Patients with diabetes risk factors should undergo blood glucose testing before and during treatment. Discontinue in patients who develop a rash without an identified cause. Orthostatic hypotension - use with caution in patients with cardiovascular disease. Leukopenia, neutropenia, and agranulocytosis may occur - patients with pre-existing low WBC should have frequent CBC monitoring during the first few months. Use cautiously in patients with a history of seizures. May impair cognitive and motor function - caution with operating machinery. Closely supervise high-risk suicidal patients.

Clinical experience with ziprasidone overdose is limited. Symptoms may include extrapyramidal symptoms, somnolence, slurred speech, and hypotension. Given the risk of QT prolongation, cardiac monitoring (ECG) is important in cases of overdose. There is no specific antidote to ziprasidone; treatment is generally supportive - maintaining airway, ensuring oxygenation, and monitoring cardiovascular function. Seek emergency medical care immediately if overdose is suspected.

Keep below 30C, away from light and moisture. Keep out of the reach of children.