Intramuscular Acute agitation in patients with schizophrenia
Adult: As ziprasidone mesilate: 10-20 mg as needed, to max 40 mg daily for 3 consecutive days. Doses of 10 mg may be given 2 hrly and doses of 20 mg may be repeated 4 hrly. Switch to oral therapy as soon as possible. Elderly: Lower initial dose and slower titration.
Oral Schizophrenia
Adult: As ziprasidone HCl: 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 and slower titration.
Oral Acute manic episodes of bipolar disorder, Acute mixed episodes of bipolar disorder
Adult: As ziprasidone HCl: 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 w/in 40-80 mg bid. Elderly: Lower initial dose and slower titration.
Administration
Should be taken with food.
Reconstitution
Add 1.2 mL of sterile water for inj to the vial to obtain a soln containing 20 mg/mL.
Contraindications
Patient w/ history of QT prolongation or cardiac arrhythmias, recent acute MI or decompensated heart failure. Concurrent use w/ other drugs known to prolong the QT interval.
Special Precautions
Patient w/ history of seizures or conditions that lower the seizure threshold, CV or cerebrovascular disease, conditions which predispose to hypotension. Renal impairment. Elderly w/ dementia-related psychosis. Pregnancy and lactation.
Adverse Reactions
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. Potentially Fatal: Life-threatening arrhythmias e.g. torsades de pointes and sudden death, neuroleptic malignant syndrome, agranulocytosis, drug reaction w/ eosinophilia and systemic symptoms (DRESS).
This drug may cause somnolence, impairment of judgment, thinking or motor skills, if affected, do not drive, operate machinery or perform hazardous tasks. Avoid alcohol.
Monitoring Parameters
Monitor serum electrolytes if on concurrent diuretic therapy. Monitor ECG in patients who show symptoms of torsades de pointes (e.g. syncope, dizziness, palpitations); wt gain. Closely monitor worsening of glucose control in patients w/ pre-existing DM. Frequently monitor CBC during 1st few mth of therapy in patients w/ pre-existing low leucocyte count or history of drug-induced leucopenia or neutropenia.
Overdosage
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 w/ a laxative, gastric lavage (after intubation for unconscious patient); established IV access. Treat hypotension and circulatory collapse w/ IV fluids. In case of severe extrapyramidal symptoms, anticholinergic medication should be given.
Drug Interactions
May antagonise effects of levodopa and dopaminergics. May enhance effects of other CNS depressants and certain antihypertensives. Altered metabolism w/ CYP3A4 inducers (e.g. carbamazepine), and inhibitors (e.g. ketoconazole). Potentially Fatal: Increased risk of arrhythmias w/ drugs known to prolong QT interval (e.g. dofetilide, quinidine, sotalol, other class Ia and III antiarrhythmics, moxifloxacin, pimozide, sparfloxacin, thioridazine).
Food Interaction
Absorption is increased up to 2-fold in the presence of food. Additive CNS effects w/ alcohol.
Action
Description: Ziprasidone, 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. Pharmacokinetics: Absorption: Well absorbed from the GI tract. Food may double the absorption. Time to peak plasma concentration: 6-8 hr (oral); w/in 1 hr (IM). Distribution: Volume of distribution: 1.5 L/kg. Plasma protein binding: Approx 99%. Metabolism: Extensively hepatic by aldehyde oxidase (approx 66% of a dose) and by the CYP3A4 isoenzyme. Excretion: Mainly as metabolites via faeces (approx 66%) and urine (approx 20%); <5% as unchanged drug. Mean terminal elimination half-life: Approx 7 hr (oral); approx 2-5 hr (IM).
Chemical Structure
Ziprasidone Source: National Center for Biotechnology Information. PubChem Database. Ziprasidone, CID=60854, https://pubchem.ncbi.nlm.nih.gov/compound/Ziprasidone (accessed on Jan. 24, 2020)
Storage
Store between 15-30°C. Reconstituted soln: Store between 15-30°C for up to 24 hr or 2-8°C for up to 7 days. Protect from light.
N05AE04 - ziprasidone ; Belongs to the class of indole derivatives antipsychotics.
References
Anon. Ziprasidone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/01/2015.Buckingham R (ed). Ziprasidone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/01/2015.Geodon Capsule, Injection, Powder, Lyophilized for Solution (Roerig). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 30/01/2015.McEvoy GK, Snow EK, Miller J et al (eds). Ziprasidone. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 30/01/2015.Ziprasidone (Marketed as Geodon and Generics): Drug Safety Communication - Rare But Potentially Fatal Skin Reactions. U.S. FDA. https://www.fda.gov/. Accessed 30/01/2015.
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