Ziprone

Ziprone Uses, Dosage, Side Effects, Food Interaction and all others data.

Ziprone, a benzylisothiazolylpiperazine is an atypical antipsychotic which may produce antischizophrenic effect by the antagonism of central dopamine D2 receptors and central type 2 serotonergic (5-HT2) receptors.

Ziprone is classified as a "second generation" or "atypical" antipsychotic and is a dopamine and 5HT2A receptor antagonist with a unique receptor binding profile. As previously mentioned, ziprasidone has a very high 5-HT2A/D2 affinity ratio, binds to multiple serotonin receptors in addition to 5-HT2A, and blocks monoamine transporters which prevents 5HT and NE reuptake. On the other hand, ziprasidone has a low affinity for muscarinic cholinergic M1, histamine H1, and alpha1-adrenergic receptors.

Trade Name Ziprone
Availability Prescription only
Generic Ziprasidone
Ziprasidone Other Names Ziprasidona, Ziprasidone, Ziprasidonum
Related Drugs Vraylar, fluoxetine, venlafaxine, quetiapine, lamotrigine, Abilify, Prozac, Seroquel, aripiprazole, olanzapine
Weight 20mg, 40mg, 60mg, 80mg
Type Capsule
Formula C21H21ClN4OS
Weight Average: 412.936
Monoisotopic: 412.112459711
Protein binding

Ziprasidone is extensively protein bound with over 99% of the drug bound to plasma proteins, primarily albumin and alpha1-acid glycoprotein.

Groups Approved
Therapeutic Class Atypical neuroleptic drugs
Manufacturer S,j, & G, Fazul Ellahie (pvt) Ltd,
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Ziprone
Ziprone

Uses

Ziprone is used for the treatment of schizophrenia, as monotherapy for the acute treatment of bipolar manic or mixed episodes, and as an adjunct to lithium or valproate for the maintenance treatment of bipolar disorder. Ziprone intramuscular is used for acute agitation in schizophrenic patients. When deciding among the alternative treatments available for the condition needing treatment, the prescriber should consider the finding of ziprasidone's greater capacity to prolong the QT/QTc interval compared to several other antipsychotic drugs. Prolongation of the QTc interval is associated in some other drugs with the ability to cause torsade de pointes-type arrhythmia, a potentially fatal polymorphic ventricular tachycardia, and sudden death. In many cases this would lead to the conclusion that other drugs should be tried first. Whether ziprasidone will cause torsade de pointes or increase the rate of sudden death is not yet known

Ziprone is also used to associated treatment for these conditions: Acute Agitation, Agitation, Bipolar 1 Disorder, Psychosis, Schizophrenia, Treatment Resistant Major Depressive Disorder, Acute Manic episode, Acute Mixed manic depressive episode

How Ziprone works

The effects of ziprasidone are differentiated from other antispychotics based on its preference and affinity for certain receptors. Ziprone binds to serotonin-2A (5-HT2A) and dopamine D2 receptors in a similar fashion to other atypical antipsychotics; however, one key difference is that ziprasidone has a higher 5-HT2A/D2 receptor affinity ratio when compared to other antipsychotics such as olanzapine, quetiapine, risperidone, and aripiprazole. Ziprone offers enhanced modulation of mood, notable negative symptom relief, overall cognitive improvement and reduced motor dysfunction which is linked to it's potent interaction with 5-HT2C, 5-HT1D, and 5-HT1A receptors in brain tissue. Ziprone can bind moderately to norepinephrine and serotonin reuptake sites which may contribute to its antidepressant and anxiolytic activity. Patient's taking ziprasidone will likely experience a lower incidence of orthostatic hypotension, cognitive disturbance, sedation, weight gain, and disruption in prolactin levels since ziprasidone has a lower affinity for histamine H1, muscarinic M1, and alpha1-adrenoceptors.

Dosage

Ziprone dosage

Schizophrenia:

  • Adult: Initially, 20 mg bid, increase if necessary at intervals of not
  • Elderly: Lower initial dose and slower titration.

Acute mixed or manic episodes in bipolar disorder:

  • Adult: Initially, 40 mg bid, increased to 60 mg or 80 mg bid on the 2nd day. Adjust subsequent doses according to patient's response and tolerance level. Maintenance treatment of bipolar I disorder (adjunctive therapy to either lithium or valproate): Continue at the same dosage on which the patient was initially stabilised within 40-80 mg bid.
  • Elderly: Lower initial dose and slower titration.

Should be taken with food.

Side Effects

Somnolence, rash or urticaria, GI disturbances, dizziness, flu-like symptoms, HTN, headache, agitation, confusion, dyspnoea, orthostatic hypotension, increased prolactin levels, wt gain, sexual dysfunction, extrapyramidal symptoms, tardive dyskinesia, hyperglycaemia. Rarely, cholestatic jaundice, hepatitis, seizures, leucopenia, neutropenia, thrombocytopenia, hyperlipidaemia.

Toxicity

The most common adverse reactions reported with ziprasidone include somnolence, respiratory tract infections, extrapyramidal symptoms, dizziness, akathisia, abnormal vision, asthenia, vomiting, headache and nausea.

Precaution

Patient with history of seizures or conditions that lower the seizure threshold, CV or cerebrovascular disease, conditions which predispose to hypotension. Renal impairment. Elderly with dementia-related psychosis. Pregnancy and lactation.

Interaction

May antagonise effects of levodopa and dopaminergics. May enhance effects of other CNS depressants and certain antihypertensives. Altered metabolism with CYP3A4 inducers (e.g. carbamazepine), and inhibitors (e.g. ketoconazole).

Food Interaction

  • Avoid alcohol.
  • Take with food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Ziprone Cholesterol interaction

[Moderate] Atypical antipsychotic drugs have been associated with undesirable alterations in lipid levels.

While all agents in the class have been shown to produce some changes, each drug has its own specific risk profile.

Before or soon after initiation of antipsychotic medication, obtain a fasting lipid profile at baseline and monitor periodically during treatment.

Volume of Distribution

The mean apparent volume of distribution of Ziprone is 1.5 L/kg.

Elimination Route

In the absence of food, ziprasidone's oral bioavailability is 60%, and absorption may reach 100% if ziprasidone is taken with a meal containing at least 500 kcal. The difference in bioavailability has little to do with the fat content of the food and appears to be related to the bulk of the meal since more absorption occurs the longer ziprasidone remains in the stomach.

Half Life

The half life of ziprasidone is 6-7 hours.

Clearance

The mean apparent systemic clearance is 7.5 mL/min/kg.

Elimination Route

Ziprone is extensively metabolized after oral administration with only a small amount excreted in the urine (<1%) or feces (<4%) as unchanged drug.

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Patient with history of QT prolongation or cardiac arrhythmias, recent acute MI or decompensated heart failure. Concurrent use with other drugs known to prolong the QT interval.

Acute Overdose

Symptoms: Minimal sedation, slurred speech, transitory HTN, extrapyramidal symptoms, somnolence, tremor, anxiety. Management: Establish and maintain an airway, ensure adequate oxygenation and ventilation. Consider admin of activated charcoal together with a laxative, gastric lavage (after intubation for unconscious patient); established IV access. Treat hypotension and circulatory collapse with IV fluids. In case of severe extrapyramidal symptoms, anticholinergic medication should be given.

Storage Condition

Store between 15-30° C.

Innovators Monograph

You find simplified version here Ziprone

Ziprone contains Ziprasidone see full prescribing information from innovator Ziprone Monograph, Ziprone MSDS, Ziprone FDA label

FAQ

What is Ziprone used for?

Ziprone is a medication that works in the brain to treat schizophrenia.Ziprone rebalances dopamine and serotonin to improve thinking, mood, and behavior.Ziprone is an antipsychotic medicine.

What are the side effects for Ziprone?

Common side effects may include:

  • dizziness, drowsiness, weakness;
  • headache;
  • nausea, vomiting;
  • trouble swallowing;
  • weight gain;
  • feeling restless or being unable to sit still;
  • tremors, involuntary muscle movements;
  • vision problems; or
  • runny nose, new or worsening cough.

How should I take Ziprone?

Ziprone oral is taken by mouth.Ziprone injection is injected into a muscle. A healthcare provider will give you this injection if you are unable to take the medicine by mouth.

Is Ziprone safe during pregnancy?

Taking antipsychotic medicine in the last 3 months of pregnancy may cause breathing problems, feeding problems, or withdrawal symptoms in the newborn. If you get pregnant, tell your doctor right away. Do not stop taking btrand without your doctor's advice.

Can I take Ziprone while breastfeeding?

You should not breastfeed while using this medicine.

Can I drink alcohol with Ziprone?

Avoid drinking alcohol. Dangerous side effects could occur.

What time should I take Ziprone?

It is usually taken twice a day with food. Take Ziprone at around the same times every day.

How long does it take for Ziprone to work?

Some improvements may be seen in as little as 1 to 2 weeks.it can sometimes take up to 6 weeks to see the full benefits of the medication. 

Is Ziprone used for depression?

Ziprone augmentation was equally efficacious in treating depression in patients with versus without anxious depression.The observed anxiolytic effect for patients with higher anxiety was not clinically significant.

How does Ziprone make I feel?

Ziprone can cause uncontrollable movements involving your face, tongue, and other body parts. Symptoms also include shaking, muscle stiffness, or feeling like you can't sit still.

Does Ziprone make me gain weight?

Ziprone is not associated with weight gain.

Can I drive after taking Ziprone?

Avoid driving or hazardous activity until you know how this medicine will affect you. Dizziness or drowsiness can cause falls, accidents, or severe injuries.

Can Ziprone cause heart problems?

Ziprone can cause a serious heart problem. Your risk may be higher if you also use certain other medicines for infections, asthma, heart problems, high blood pressure, depression, mental illness, cancer, malaria, or HIV.

Can I using Ziprone with other drugs?

Using Ziprone with other drugs that make you drowsy can worsen this effect. Ask your doctor before using opioid medication, a sleeping pill, a muscle relaxer, or medicine for anxiety or seizures.

What happens if I take Ziprone overdose?

Previously reported pediatric Ziprone overdoses describe a syndrome of sedation, tachycardia, hypotonia, and coma consistent with that of the patient described in this paper. In pediatric Ziprone overdose, QTc prolongation and hypotension have also been illustrated, but seizures have not been reported.

What should I avoid while taking Ziprone?

While you are taking Ziprone, you may be more sensitive to extreme temperatures, such as very hot or cold conditions. Avoid getting too cold, or becoming overheated or dehydrated. Drink plenty of fluids, especially in hot weather and during exercise. It is easier to become dangerously overheated and dehydrated while you are taking Ziprone.

*** Taking medicines without doctor's advice can cause long-term problems.
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