Zipsydon20mg

Ziprasidone is an atypical (second-generation) antipsychotic thought to act through a combination of dopamine D2 and serotonin 5HT2 receptor antagonism. It is available in both capsule and intramuscular injection forms.

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.

Atypical neuroleptic drugs

Atypical antipsychotic (Benzothiazolylpiperazine derivative)

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.

The exact mechanism of action of ziprasidone is not fully known, but it is thought to be mediated through a combination of dopamine type 2 (D2) and serotonin type 2 (5HT2) receptor antagonism, which modulates dopaminergic and serotonergic signaling in the brain to reduce psychotic symptoms (hallucinations, delusions) and manic symptoms. It is metabolized primarily in the liver (via CYP3A4), with a mean terminal half-life of about 7 hours.

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.

Capsules should be administered orally with food - absorption is increased up to two-fold in the presence of food. Do not open, crush, or chew the capsule.

If a dose is missed, take it as soon as remembered. If it is close to the time of the next scheduled dose, skip the missed dose and resume the regular dosing schedule. Do not take a double dose to make up for a missed one.

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.

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.

Known history of QT prolongation Recent acute myocardial infarction Uncompensated heart failure Combination with other drugs that have demonstrated QT prolongation Known hypersensitivity to ziprasidone

Should not be used in combination with other drugs that have demonstrated QT prolongation. Lithium: Concomitant use did not affect the steady-state level or renal clearance of lithium. Oral contraceptives: Ziprasidone did not affect the pharmacokinetics of concomitant oral contraceptives. As it is metabolized via CYP3A4, use with caution with strong CYP3A4 inhibitors or inducers.

The absorption of ziprasidone is increased up to two-fold in the presence of food, so it should always be taken with food.

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.

There is insufficient data on the safety of ziprasidone use during breastfeeding, so breastfeeding mothers should consult a physician before use.

Safety and effectiveness in pediatric patients have not been established.

No overall differences in safety or effectiveness have been observed between elderly and younger subjects, but greater sensitivity in some older individuals cannot be ruled out. A lower starting dose, slower titration, and careful monitoring should be considered for elderly patients with multiple risk factors.

Renal: Dosage adjustment based on degree of renal impairment is not required; ziprasidone is not removed by hemodialysis. The cyclodextrin excipient in the intramuscular formulation is cleared by renal filtration, so caution is needed in renal impairment. Hepatic: Ziprasidone is cleared substantially by the liver, so hepatic impairment is expected to increase its AUC. A total daily dose reduction of at least 50% is recommended in moderate hepatic impairment.

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.

Chemically, ziprasidone hydrochloride monohydrate is 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one, monohydrochloride, monohydrate. Its molecular formula is C21H21ClN4OS.HCl.H2O, with a molecular weight of approximately 467.42. Ziprasidone is a benzothiazolylpiperazine derivative.

Q: What is Ziprasidone used for? A: It is used to treat schizophrenia and manic or mixed episodes associated with bipolar I disorder in adults. Q: Should this medicine be taken with food? A: Yes, absorption is increased up to two-fold with food, so it should always be taken with food. Q: Can I take this medicine if I have heart problems? A: No, it is contraindicated with a history of QT prolongation, recent heart attack, or uncompensated heart failure. Q: Is Ziprasidone safe during pregnancy? A: It is Pregnancy Category C. It should not be used during pregnancy without a doctor's advice. Q: Can this medicine be given to children? A: No, safety and effectiveness in pediatric patients have not been established.