Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Austria: Zeldox; Bulgaria: Zeldox; Czech Republic: Zeldox; Denmark: Zeldox; Estonia: Zeldox; Finland: Zeldox; Germany: Zeldox; Greece: Geodon; Hungary: Zeldox; Ireland: Geodon, Zeldox; Luxembourg: Zeldox; Poland: Zeldox; Portugal: Zeldox; Romania: Zeldox; Slovakia: Zeldox; Slovenia: Zeldox; Spain: Zeldox; Sweden: Geodon, Zeldox, Ziprasidon.

North America

Canada: Zeldox; USA: Geodon.

Latin America

Argentina: Zeldox; Brazil: Geodon; Mexico: Geodón.

Drug combinations


Ziprasidone Hydrochloride: C~21~H~21~ClN~4~OS HCl H~2~O. Mw: 467.41. 2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, monohydrochloride, monohydrate. CAS-138982-67-9; CAS-146939-27-7 (ziprasidone)(1994).

Ziprasidone Mesylate: C~21~H~21~ClN~4~OS CH~4~O~3~S 3H~2~O. Mw: 563.09. (1) 2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, monomethanesulfonate, trihydrate; (2) 5-[2-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-2-indolinone monomethanesulfonate, trihydrate. CAS-199191-69-0 (1999).

Pharmacologic Category

Atypical Antipsychotics. (ATC-Code: N05AE04).

Mechanism of action

A benzylisothiazolylpiperazine antipsychotic. Exact mechanism of action unknown. Has high affinity for D~2~, D~3~, 5-HT~2A~, 5-HT~1A~, 5-HT~2C~, 5-HT~1D~, and α~1~-adrenergic, and moderate affinity for histamine H~1~ receptors. Ziprasidone functions as antagonist at D~2~, 5-HT~2A~, and 5-HT~1D~ receptors and as agonist at 5-HT~1A~ receptor. Ziprasidone moderately inhibits reuptake of serotonin and norepinephrine.

Therapeutic use

Treatment of schizophrenia. Treatment of acute manic or mixed episodes associated with bipolar disorder with or without psychosis. Acute agitation in schizophrenia.

Pregnancy and lactiation implications

Developmental toxicity demonstrated in animals. There are no adequate, well-controlled studies in pregnant women. Use only if potential benefit justifies risk to fetus. Excretion in breast milk unknown (not recommended during lactation).

Unlabeled use

Tourette’s syndrome. Psychosis/agitation related to Alzheimer’s dementia.


Hypersensitivity to ziprasidone or any component of the formulation. History of (or current) prolonged QT. Congenital long QT syndrome. Recent MI. History of arrhythmias. Uncompensated heart failure. Concurrent use of other QTc-prolonging agents including amiodarone, arsenic trioxide, bretylium, chlorpromazine, cisapride, class Ia antiarrhythmics (quinidine, procainamide), dofetilide, dolasetron, droperidol, ibutilide, levomethadyl, mefloquine, mesoridazine, pentamidine, pimozide, probucol, some quinolone antibiotics (moxifloxacin), sotalol, tacrolimus, and thioridazine.

Warnings and precautions

Antipsychotic use associated with esophageal dysmotility and aspiration (use with caution in risk of pneumonia (e.g. Alzheimer’s disease)). May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia. Atypical antipsychotics associated with development of hyperglycemia (may be extreme and associated with ketoacidosis, hyperosmolar coma, or death). Use with caution in diabetes or other glucose regulation disorders. Use may be associated with neuroleptic malignant syndrome. May cause orthostatic hypotension (use with caution in cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia). May result in QTc prolongation, associated with development of malignant ventricular arrhythmias (torsade de pointes) and sudden death. Avoid hypokalemia, hypomagnesemia. Use caution in bradycardia. Use associated with fairly high incidence of rash. Moderately to highly sedating. Possibility of suicide attempt inherent in psychotic illness or bipolar disorder (use with caution in high-risk patients). Impaired core body temperature regulation may occur (caution with strenuous exercise, heat exposure, dehydration, and concomitant medication possessing anticholinergic effects). Significant weight gain observed with antipsychotic therapy. Ziprasidone not approved for dementia-related psychosis in elderly patients (increased incidence of cerebrovascular adverse events (including fatalities) reported). Use with caution in hepatic disease or impairment, in Parkinson’s disease, and in breast cancer or other prolactin-dependent tumors (elevates prolactin levels). Use with caution in renal impairment, and in risk of seizures, including patients with history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. Elderly patients may be at increased risk of seizures due to increased prevalence of predisposing factors.



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