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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Ziprasidone Mesylate
Generic Name
Ziprasidone Mesylate
Active Ingredient
ZiprasidoneCategory
Atypical Antipsychotic [EPC]
Salt Form
Hydrochloride
Variants
8
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Ziprasidone Mesylate, you must consult a qualified healthcare professional.
| 68083-340 |
| 20 mg/mL | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | INTRAMUSCULAR | 43598-061 |
| 20 mg/mL | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | INTRAMUSCULAR | 51662-1564 |
| 20 mg/mL | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | INTRAMUSCULAR | 72205-205 |
| 20 mg/mL | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | INTRAMUSCULAR | 72266-160 |
Detailed information about Ziprasidone Mesylate
Ziprasidone is an atypical antipsychotic used to treat schizophrenia and bipolar I disorder. It works by balancing dopamine and serotonin levels in the brain to improve mood, thinking, and behavior.
Dosage for Ziprasidone is highly individualized and depends on the condition being treated and the patient's response to the medication.
For the treatment of schizophrenia, the typical starting dose is 20 mg taken twice daily with food. Depending on the clinical response, your doctor may increase the dose up to a maximum of 80 mg twice daily. Dose adjustments should generally occur at intervals of no less than two days, as it takes time for the body to reach a steady state. The effective range is usually between 40 mg and 80 mg twice daily.
The recommended starting dose for bipolar mania is 40 mg twice daily taken with food. The dose may be increased to 60 mg or 80 mg twice daily on the second day of treatment. Subsequent adjustments should be based on tolerance and efficacy, with the goal of maintaining the patient on the lowest effective dose within the 40-80 mg twice-daily range.
For acute agitation in schizophrenia, the recommended dose is 10 mg to 20 mg administered via IM injection. A dose of 10 mg may be given every two hours, or 20 mg every four hours, up to a maximum of 40 mg per day. IM use is generally restricted to three consecutive days.
Ziprasidone is FDA-approved for the treatment of manic or mixed episodes associated with Bipolar I Disorder in pediatric patients aged 10 to 17 years.
Ziprasidone is not currently FDA-approved for the treatment of schizophrenia in pediatric patients.
No dosage adjustment is required for patients taking the oral capsules who have kidney disease. However, the intramuscular (IM) injection contains an excipient called sulfobutylether β-cyclodextrin sodium (SBECD), which is cleared by the kidneys. Therefore, the IM form should be used with caution in patients with significant renal impairment.
Since Ziprasidone is cleared by the liver, patients with mild to moderate hepatic impairment should be monitored closely. However, specific dosage adjustment guidelines are not strictly defined in the labeling. Use in severe hepatic impairment is not well-studied and requires extreme caution.
Elderly patients (65 years and older) do not typically require a lower starting dose based on age alone. However, because this population is more prone to orthostatic hypotension (dizziness upon standing) and decreased hepatic or cardiac function, a slower titration (dose increase) may be appropriate.
If you miss a dose, take it as soon as you remember, provided it is taken with food. However, if it is almost time for your next scheduled dose, skip the missed dose and continue with your regular schedule. Do not 'double up' or take two doses at once to make up for a missed one.
Signs of a Ziprasidone overdose may include extreme drowsiness, tremors, anxiety, and most dangerously, heart rhythm changes (prolonged QT interval) which can lead to fainting or seizures. If an overdose is suspected, contact your local poison control center or seek emergency medical attention immediately. There is no specific antidote for Ziprasidone; treatment is supportive and focused on maintaining airway and cardiac monitoring.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop the medication without medical guidance, as this can lead to a relapse of symptoms.
Most patients taking Ziprasidone will experience some side effects, particularly during the first few weeks of treatment as the body adjusts. Common side effects include:
Ziprasidone is a powerful medication that requires careful clinical monitoring. Before starting treatment, patients must undergo a thorough cardiovascular assessment. Because Ziprasidone has a greater capacity to prolong the QT interval than many other antipsychotics, it is generally reserved for patients who do not have a history of significant heart disease.
Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Analyses of seventeen placebo-controlled trials (modal duration of 10 weeks), largely in patients taking atypical antipsychotic drugs, revealed a risk of death in drug-treated patients of between 1.6 to 1.7 times the risk of death in placebo-treated patients. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was about 4.5%, compared to a rate of about 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. Ziprasidone is not approved for the treatment of patients with dementia-related psychosis.
Ziprasidone must NEVER be used with medications that are known to significantly prolong the QT interval. Combining these drugs increases the risk of sudden cardiac death. Contraindicated drugs include:
There are several conditions where Ziprasidone is strictly prohibited due to the risk of life-threatening complications:
Ziprasidone is classified under the older FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Animal studies have shown developmental toxicity, including increased fetal structural abnormalities, when exposed to doses several times the human equivalent.
Neonatal Abstinence Syndrome: Neonates exposed to antipsychotic drugs during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery. These symptoms can include agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, and feeding disorder. Ziprasidone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Limited data suggest that Ziprasidone is excreted into human breast milk in very small amounts. The milk-to-plasma ratio is estimated to be low. However, because of the potential for serious adverse reactions in nursing infants (such as sedation or movement disorders), a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Ziprasidone's therapeutic efficacy is primarily attributed to its high-affinity antagonism at Dopamine D2 and Serotonin 5-HT2A receptors. It also functions as a 5-HT1A receptor agonist, which may enhance its cognitive and antidepressant properties. Unique among many antipsychotics, Ziprasidone also inhibits the synaptic reuptake of serotonin and norepinephrine by binding to their respective transporters. This 'triple-hit' mechanism (D2/5-HT2A antagonism plus SRI/NRI activity) provides a broad spectrum of activity against both positive and negative symptoms of schizophrenia.
The binding profile of Ziprasidone is characterized by high affinity for D2, D3, 5-HT2A, 5-HT2C, 5-HT1A, 5-HT1D, and α1-adrenergic receptors, and moderate affinity for histamine H1 receptors. Its lack of significant affinity for muscarinic cholinergic receptors explains its low incidence of anticholinergic side effects (like constipation or dry eyes). The onset of action for acute symptoms can occur within hours (IM) or days (oral), but full antipsychotic effects often take 4 to 6 weeks of consistent dosing.
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Common questions about Ziprasidone Mesylate
Ziprasidone is primarily used to treat schizophrenia and manic or mixed episodes associated with bipolar I disorder. In schizophrenia, it helps manage symptoms such as hallucinations, delusions, and disorganized thinking. For bipolar disorder, it works to stabilize mood during acute manic phases characterized by excessive energy or agitation. It is also used as a long-term maintenance therapy in bipolar disorder when combined with other mood stabilizers. Your doctor may also use the injectable form for emergency control of acute agitation.
The most common side effects reported by patients include drowsiness (somnolence), nausea, and a feeling of restlessness known as akathisia. Many patients also experience dizziness, especially when standing up quickly, and some may notice mild muscle stiffness or tremors. Because Ziprasidone must be taken with food, stomach upset is common if the meal is too small. Most of these side effects are most prominent when first starting the medication or during a dose increase. If these symptoms become severe or persistent, you should consult your healthcare provider.
It is strongly advised that you do not drink alcohol while taking Ziprasidone. Alcohol is a central nervous system depressant that can significantly worsen the drowsiness and dizziness caused by the medication. This combination can lead to dangerous levels of sedation, impaired judgment, and a higher risk of falls or accidents. Furthermore, alcohol can interfere with the stability of the psychiatric conditions Ziprasidone is meant to treat. Always discuss your lifestyle habits with your doctor before beginning antipsychotic therapy.
Ziprasidone should only be used during pregnancy if the potential benefits to the mother outweigh the potential risks to the fetus. There is limited data on its safety in human pregnancy, but animal studies have suggested some risks to fetal development. Additionally, babies born to mothers who take antipsychotics in the third trimester may experience withdrawal symptoms or movement disorders after birth. If you are pregnant or planning to become pregnant, it is vital to discuss a management plan with your psychiatrist. Never stop taking your medication suddenly during pregnancy without medical advice.
The timeline for Ziprasidone's effects varies depending on the symptoms being treated. For acute agitation using the injection, effects can be felt within 15 to 30 minutes. When taking the oral capsules for schizophrenia or mania, some improvement in sleep and agitation may be noticed within the first week. However, the full antipsychotic effects on hallucinations and delusions typically take 4 to 6 weeks of consistent use. It is important to continue taking the medication exactly as prescribed even if you do not feel better immediately.
No, you should never stop taking Ziprasidone suddenly unless instructed by your doctor in an emergency. Abruptly stopping an antipsychotic can lead to a rapid return of psychotic symptoms or a 'rebound' manic episode. It can also cause physical withdrawal symptoms such as nausea, sweating, insomnia, and tremors. If you and your doctor decide to stop the medication, they will provide a tapering schedule to slowly lower your dose over several weeks. This allows your brain chemistry to adjust safely.
If you miss a dose of Ziprasidone, take it as soon as you remember, but only if you can take it with a meal of at least 500 calories. If it is nearly time for your next scheduled dose, skip the missed dose entirely and return to your normal routine. Do not take two doses at the same time to compensate for the one you missed. Consistency is key with Ziprasidone because its absorption is so dependent on food. Setting a regular schedule with your morning and evening meals can help prevent missed doses.
Ziprasidone is considered one of the most 'weight-neutral' atypical antipsychotics available. Clinical trials have shown that patients taking Ziprasidone generally experience much less weight gain than those taking medications like Olanzapine or Clozapine. In some cases, patients switching from other antipsychotics to Ziprasidone actually lose weight. However, weight gain is still possible, and it is important to monitor your weight and metabolic health regularly. A healthy diet and exercise remain important components of your overall treatment plan.
Ziprasidone can interact with many other medications, some of which can be dangerous. It should never be taken with drugs that affect heart rhythm (QT-prolonging drugs) like certain antibiotics or antiarrhythmics. It can also interact with medications processed by the CYP3A4 liver enzyme, such as certain antifungals or seizure medications. Always provide your doctor with a complete list of all prescriptions, over-the-counter drugs, and herbal supplements you use. Your doctor will check for these interactions to ensure your treatment combination is safe.
Yes, Ziprasidone is available as a generic medication in the form of ziprasidone hydrochloride capsules. The generic version is bioequivalent to the brand-name drug Geodon, meaning it contains the same active ingredient and works the same way in the body. Generic Ziprasidone is typically much more affordable than the brand-name version and is covered by most insurance plans. When filling your prescription, your pharmacist may provide the generic version unless your doctor specifically requests the brand name.
Other drugs with the same active ingredient (Ziprasidone)
> Warning: Stop taking Ziprasidone and call your doctor or emergency services immediately if you experience any of the following:
With prolonged use, Ziprasidone may lead to certain metabolic changes, although the risk is lower than with drugs like Clozapine or Olanzapine. These include:
Ziprasidone carries a Boxed Warning regarding its use in elderly patients with dementia-related psychosis. Clinical trials have shown that elderly patients treated with antipsychotic drugs for dementia-related symptoms are at an increased risk of death, primarily from cardiovascular (heart failure, sudden death) or infectious (pneumonia) causes. Ziprasidone is not approved for the treatment of patients with dementia-related psychosis.
Report any unusual symptoms or changes in mood/behavior to your healthcare provider immediately. Regular monitoring of your physical health is a vital part of antipsychotic therapy.
Ziprasidone causes a dose-related prolongation of the QT interval. A prolonged QT interval can lead to a life-threatening heart rhythm called Torsades de Pointes. You should not take Ziprasidone if you have a history of 'long QT syndrome,' a recent heart attack, uncompensated heart failure, or if you take other medications that also prolong the QT interval. Your doctor may perform an Electrocardiogram (ECG) before and during treatment.
A potentially fatal symptom complex sometimes referred to as NMS has been reported in association with antipsychotic drugs. Clinical manifestations of NMS are hyperpyrexia (high fever), muscle rigidity, altered mental status, and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmia).
This is a syndrome of potentially irreversible, involuntary, dyskinetic movements that may develop in patients treated with antipsychotic drugs. The risk is believed to increase with the duration of treatment and the total cumulative dose.
Atypical antipsychotic drugs have been associated with metabolic changes that may increase cardiovascular/cerebrovascular risk. These changes include hyperglycemia (high blood sugar), dyslipidemia, and weight gain. While Ziprasidone's risk is lower than others, monitoring is still required.
Patients on Ziprasidone should have the following monitored regularly:
Ziprasidone may cause significant somnolence (drowsiness) and impair judgment, thinking, or motor skills. You should not drive a car or operate dangerous machinery until you are reasonably certain that Ziprasidone therapy does not affect you adversely.
Alcohol can increase the sedative effects of Ziprasidone. Combining the two can lead to dangerous levels of respiratory depression or extreme drowsiness. It is strongly recommended to avoid alcohol while taking this medication.
Do not stop taking Ziprasidone abruptly. Sudden discontinuation can lead to a 'rebound' of psychotic symptoms or withdrawal-like effects such as insomnia, tremors, or sweating. If the medication needs to be stopped, your doctor will provide a tapering schedule to gradually reduce the dose.
> Important: Discuss all your medical conditions, especially heart problems or electrolyte imbalances, with your healthcare provider before starting Ziprasidone.
Ziprasidone is not known to cause significant interference with common laboratory tests, such as urine drug screens for amphetamines or opioids. However, it can cause elevations in serum prolactin levels, which should be considered if testing for hormonal imbalances.
If an interaction is unavoidable, your doctor may:
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter cold or allergy medicines.
These conditions require a careful risk-benefit analysis by a specialist:
While there is no documented cross-sensitivity with other atypical antipsychotics (like Risperidone), patients who have had severe skin reactions (like DRESS syndrome) to other medications should be monitored with extreme caution, as Ziprasidone has a specific association with severe cutaneous adverse reactions.
> Important: Your healthcare provider will evaluate your complete medical history, including a baseline ECG, before prescribing Ziprasidone.
Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, the Boxed Warning regarding increased mortality in elderly patients with dementia-related psychosis is the primary concern. Elderly patients are also more sensitive to orthostatic hypotension and may require slower dose titration.
For oral administration, no dose adjustment is necessary for patients with renal failure. However, the IM injection contains sulfobutylether β-cyclodextrin sodium (SBECD), which can accumulate in patients with impaired renal function. In patients with a GFR < 10 mL/min, the IM form should be avoided if possible.
Ziprasidone is extensively metabolized by the liver. While specific adjustments for the Child-Pugh classification are not provided in the manufacturer's labeling, patients with cirrhosis or significant liver dysfunction should be monitored for signs of toxicity, as the half-life of the drug may be prolonged.
> Important: Special populations require individualized medical assessment and frequent follow-up appointments.
| Bioavailability | 60% (with food) / 30% (fasted) |
| Protein Binding | 99% (Albumin and AAG) |
| Half-life | 7 hours (Oral) / 2-5 hours (IM) |
| Tmax | 6-8 hours (Oral) |
| Metabolism | Aldehyde Oxidase (66%), CYP3A4 (33%) |
| Excretion | Renal 20%, Fecal 66% (as metabolites) |
Ziprasidone is a Second-Generation (Atypical) Antipsychotic. It is chemically distinct from other atypicals like the thienobenzodiazepines (Olanzapine) or dibenzothiazepines (Quetiapine).