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Ziprasidone
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Ziprasidone is a prescription drug used for the treatment of schizophrenia and bipolar disorder. It belongs to a family of psychiatric drugs known as atypical antipsychotics. Other members of this family include clozapine (Clozaril) and risperidone (Risperdal). Ziprasidone is marketed by Pfizer and received FDA approval in February 2001.
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Other Names
Ziprasidone is marketed in the U.S. as Geodon.
Uses
Ziprasidone is specifically indicated for the treatment of:
- Schizophrenia
- Mania in bipolar disorder
- Acute agitation in schizophrenia
How Ziprasidone is Taken
Ziprasidone is available as intramuscular (IM) injection or in oral capsules containing 20, 40, 60, or 80 mg of active ingredient.
For schizophrenia
Ziprasidone is taken initially as 20 mg twice daily with food. Daily dosage may subsequently be adjusted as needed to improve symptoms, up to a maximum of 80 mg twice daily. A once-daily formulation is under active development.
For bipolar mania
Ziprasidone is initially taken as 40 mg twice daily with food. The dosing can subsequently be adjusted on the basis of tolerability and effectiveness within the range 40-80 mg twice daily.
For agitation
The recommended dose is 10-20 mg administered by intramuscular injection up to a maximum dose of 40 mg per day. Doses of 10 mg may be administered every two hours. Doses of 20 mg may be administered every four hours up to a maximum of 40 mg per day. In clinical trials, patients given IM ziprasidone showed significant and rapid (within 15-30 minutes) reduction in agitation and hostility to an extent greater than that attained with [haloperidol].[1]
How Ziprasidone Works
The precise mechanism of action of ziprasidone is unknown. However, it has been proposed that this drug's efficacy in schizophrenia and bipolar disorder is mediated through the inhibition of dopamine type 2 (D2) and serotonin type 2 (5HT2) receptors in the brain.
How the Body Affects Ziprasidone
Ziprasidone is well absorbed, reaching peak circulating levels in 6-8 hours.
Lab studies show that the liver enzyme CYP3A4 is the major enzyme involved in the metabolism of ziprasidone. The liver enzyme CYP1A2 contributes to a much lesser extent.
Approximately 20% of the original dose is excreted in the urine, with approximately 66% being eliminated in the feces.
Side Effects
The most common side effects associated with ziprasidone use:
- Somnolence (sleepiness)
- Extrapyramidal symptoms
- Dizziness
- Akathisia (restlessness)
- Abnormal vision
- Asthenia (feelings of weakness)
- Vomiting
Risks and Precautions
- Elderly patients with a diagnosis of psychosis related to dementia who are treated with atypical antipsychotics like ziprasidone are at an increased risk of death.
- The risk of heart arrhythmias (irregular heartbeat) is increased if certain other medicines are taken with ziprasidone and if there are preexisting certain abnormal heart conditions.
- A potentially fatal condition called Neuroleptic Malignant Syndrome (NMS) can occur with antipsychotic medications like ziprasidone. Signs of NMS include very high fever, rigid muscles, shaking, confusion, sweating, or increased heart rate and blood pressure.
- People treated with atypical antipsychotics like ziprasidone need to be monitored for symptoms of hyperglycemia (high blood sugar).
- Dizziness caused by a fall in blood pressure may occur with ziprasidone use.
- Pregnancy and breastfeeding are not advised while using ziprasidone.
- Ziprasidone can cause sleepiness; so driving and operating machinery is not advised.
- Heat regulation in the body is affected by ziprasidone so avoidance of high temperature or humidity is advised.
- Consuming alcoholic beverages is not recommended while taking ziprasidone.
Drug Interactions
The following medications are known or likely to produce significant drug interactions with ziprasidone use:
- Dofetilide
- Sotalol
- Quinidine and other Class Ia and III anti-arrhythmics
- Mesoridazine
- Thioridazine
- Chlorpromazine
- Droperidol
- Pimozide
- Sparfloxacin
- Gatifloxacin
- Moxifloxacin
- Halofantrine
- Mefloquine
- Pentamidine
- Arsenic trioxide
- Levomethadyl acetate
- Dolasetron mesylate
- Probucol
- Tacrolimus
Effectiveness
Four out of five short-term controlled studies showed ziprasidone to be more effective than placebo in treating schizophrenia.[2]
Another trial demonstrated that ziprasidone is significantly superior to placebo in reducing symptoms of acute mania in people with bipolar disorder.[3]
References
- ↑ Zimbroff DL, Allen MH, Battaglia J, et al. Best clinical practice with ziprasidone IM: update after 2 years of experience. CNS Spectr. 2005 Sep;10(9):1-15. Abstract | Full Text
- ↑ Crutchfiled DB, Ziprasidone: A New Atypical Antipsychotic. Geriatric Times II(5), September/October 2001.
- ↑ Keck PE Jr, Versiani M, Potkin S, et al. Ziprasidone in the treatment of acute bipolar mania: a three-week, placebo-controlled, double-blind, randomized trial. Am J Psychiatry. 2003 Apr;160(4):741-8. Abstract | Full Text | PDF
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