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Ziprasidone information from DrugsUpdate  

See Available Brands of Ziprasidone in India

P - Caution when used during pregnancy
L - Contraindicated in Lactation
FI - Food *

Ziprasidone (marketed as Geodon, Zeldox by Pfizer) was the fifth atypical antipsychotic to gain FDA approval (February 2001). In the United States, Ziprasidone is Food and Drug Administration (FDA) approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients. Ziprasidone has also received approval for acute treatment of mania and mixed states associated with bipolar disorder. The brand name Geodon has been suggested to bring to mind the phrase 'down (don) to earth (geo)' referring to the goals of the medication.

The oral form of ziprasidone is the hydrochloride salt, ziprasidone hydrochloride. The intramuscular form, on the other hand, is the mesylate salt, ziprasidone mesylate trihydrate, and is provided as a lyophilized powder.

Geodon was one of four drugs which Pfizer in 2009 pleaded guilty to misbranding "with the intent to defraud or mislead". Pfizer agreed to pay $2.3 billion (£1.4 billion) in settlement, and entered a corporate integrity agreement. Pfizer was found to have illegally promoted four of its drugs for use in conditions that had not been approved by the FDA.

Pharmacodynamics

Pharmacokinetics

Ziprasidone, an atypical antipsychotic, produces antischizophrenic effect through a combination of dopamine D2 and serotonin 5H2 receptor antagonism.

Absorption
Well absorbed from the GI tract. Peak plasma concentrations: 6-8 hr (oral); 1 hr (IM). Bioavailability: 100% (IM). Food increases absorption.

Distribution
Protein-binding: 99%.

Metabolism
Extensively hepatic by aldehyde oxidase (66% of a dose) and by the cytochrome P450 isoenzyme CYP3A4.

Excretion
Excreted mainly as metabolites via faeces (66%) and urine (20%); <5% as unchanged drug. Mean terminal elimination half-life: 7 hr (oral); 2-5 hours (IM).

Ziprasidone Indications / Ziprasidone Uses

Information Not Available

Ziprasidone Adverse Reactions / Ziprasidone Side Effects

Somnolence, respiratory tract infections, akathisia, extrapyramidal syndrome, tardive dyskinesia, hyperglycaemia, dizziness, dystonia, headache, GI disturbances, asthenia, agitation, rash, urticaria, visual disturbances, prolonged QT interval, orthostatic hypotension, increased prolactin levels, weight gain, sexual dysfunction, hyperlipidaemia, seizures.

Potentially Fatal: Blood dyscrasias, neuroleptic malignant syndrome.

Precautions

Warnings
Increased mortality
Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death compared with placebo. Over the course of a 10-wk controlled trial, the rate of death in drug-treated patients was about 4.5% compared with 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either CV (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature.

Monitor
Ensure that patients at risk of electrolyte disturbances have baseline serum potassium and magnesium measurements. Correct low levels before proceeding with treatment. Periodically monitor potassium and magnesium in patients started on diuretic treatment during ziprasidone therapy. Discontinue treatment in patients who have persistent QTc measurements more than 500 msec.

Special Precautions

Patients predisposed to significant electrolyte disturbances, esp hypokalaemia, should have a baseline serum potassium and magnesium screening performed and corrected before treatment. CNS depression; cerebrovascular disease and significant CV illness; history of seizures; conditions that decrease seizue threshold; predisposition to hypotension; patients at risk of aspiration pneumonia; Parkinson's disease; renal impairment (IM); hepatic impairment; pregnancy. Discontinue if persistent QTc measurements >500 msec. May impair ability to drive or operate machinery. Monitor ECG in patients who shows symptoms of torsades de pointes (e.g. syncope, dizziness, palpitations). Monitor serum electrolytes if on concurrent diuretic therapy. Monitor glucose levels in DM or patient at risk of developing DM.

Other Drug Interactions

Antagonistic effect with levodopa and dopamine antagonists. Additive hypotensive effect with antihypertensives. Additive sedative effects with other CNS agents, alcohol.

Potentially Fatal: Increased risk of torsades de pointes with drugs that prolong QT interval e.g. dofetilide, quinidine, sotalol, and other Class Ia and III antiarrhythmics, moxifloxacin, pimozide, sparfloxacin, thioridazine.

Other Interactions

Food Interaction


Grapefruit juice may increase serum concentration. Increased CNS depression with kava kava, chamomile. Possible decrease of ziprasidone concentration with St John's Wort.

Dosage

Oral
Schizophrenia
Adult: As hydrochloride: ≥18 yr: Initially 20 mg bid, increase if necessary at intervals of not < 2 days, up to 80 mg bid. Maintenance: 20 mg bid.
Elderly: Lower initial dose with slow titration and close monitoring.
Hepatic impairment: Dose reductions may be needed.

Oral
Mania
Adult: Initially, 40 mg bid, increased to 60-80 mg bid on the 2nd day. Adjust subsequent doses according to patient's response and tolerance level.
Elderly: Lower initial dose with slow titration and close monitoring.
Hepatic impairment: Dose reductions may be needed.

Intramuscular

Acute agitation in patients with schizophrenia
Adult: As mesilate: ≥18 yr: 10-20 mg as needed; doses of 10 mg may be repeated every 2 hr and doses of 20 mg may be repeated every 4 hr. Max: 40 mg daily for 3 consecutive days. Switch to oral therapy as soon as possible.
Elderly: Lower initial dose with slow titration and close monitoring.
Renal impairment: Use with caution due to cyclodextrin excipient.
Hepatic impairment: Dose reductions may be needed.

Reconstitution
Add 1.2 ml of sterile water to the vial to obtain a solution containing 20 mg/ml.

Food(before/after)

Should be taken with food

List of Contraindications

Ziprasidone and Pregnancy

Caution when used during 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.

Ziprasidone and Lactation

Contraindicated in lactation

Ziprasidone and Children

Safety and efficacy not established

Ziprasidone and Geriatic

Use with caution

Ziprasidone and Other Contraindications

Concomitant use of oral and IM ziprasidone. Recent acute MI, decompensated heart failure, cardiac arrhythmias, conditions that may increase QT interval eg, QT-interval prolongation or history of QT prolongation; prolactin dependent tumours. Lactation. Not for treatment of behavioural disorders in elderly with dementia.

Storage

Intramuscular
Store at 15-30°C (59-86°F). Once reconstituted, store at 15-30°C for up to 24 hr or 2-8°C (36-46°F) for up to 7 days. Protect from light.

Oral
Store at 15-30°C (59-86°F).

Lab interference

Intramuscular
Store at 15-30°C (59-86°F). Once reconstituted, store at 15-30°C for up to 24 hr or 2-8°C (36-46°F) for up to 7 days. Protect from light.

Oral
Store at 15-30°C (59-86°F).

Ziprasidone brands in India:

Azona Zipris Zipsydon

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