Drug information of Ziprasidone

Ziprasidone

Drug group:

Ziprasidone is an atypical antipsychotic medication. It works by changing the effects of chemicals in the brain. Ziprasidone is used to treat schizophrenia and the manic symptoms of bipolar disorder (manic depression) in adults and children who are at least  10 years old. it’s Contain 20,40,60,80 mg capsules and 20mg vial

Mechanism of effect

Acts as antagonist at dopamine D2 and serotonin type 1 and 2 (5HT1D, 5HT2A) receptors; acts as agonist at serotonin 5HT1A receptor; moderately inhibits reuptake of norepinephrine and serotonin; has alpha-blocking and antihistaminic activity.

Pharmacodynamic

Ziprasidone is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Ziprasidone is a selective monoaminergic .

Pharmacokinetics

Absorption:

Peak plasma time: 6-8 hr (PO); ≤60 min (IM)

Distribution:

Protein bound: 99%

Metabolism:

Metabolized in liver

Elimination:

Half-life: 7 hr (PO); 2-5 hr (IM)

Excretion:Feces (66%), urine (20%)

Drug indications

Schizophrenia

Dosage

Schizophrenia:

20 mg PO q12hr with food initially; may be increased every other day PRN; not to exceed 80 mg q12hr

Periodically assess need for maintenance; clinical trials have documented no added benefit with doses above 20 mg q12hr

Acute Agitation With Schizophrenia:

IM: 10 mg q2hr or 20 mg q4hr; not to exceed 40 mg/day; use IM for up to 3 days, and switch to PO if continuing past this time

Bipolar I Disorder:

maintenance therapy as adjunct to lithium or valproate

Acute treatment: 40 mg PO q12hr with food initially; on day 2, may be increased if necessary to 60-80 mg PO q12hr; adjust dose according to tolerance and efficacy within range of 40-80 mg q12hr

Alerts

Atypical antipsychotics have been associated with metabolic changes (eg, hyperglycemia, dyslipidemia, and body weight gain) that may increase cardiovascular/cerebrovascular risk

Hyperglycemia may occur and in some cases may be extreme, resulting in ketoacidosis, hyperosmolar coma, or death; monitor blood glucose of high-risk patients. 

Neuroleptic malignant syndrome reported with antipsychotic drugs.

Tardive dyskinesia, acute dystonic reactions, pseudoparkinsonism, or akathisia may develop acutely or chronically. 

Discontinue if rash develops without an identified cause 

Drug reaction with eosinophilia and systemic symptoms (DRESS) reported; DRESS consists of combination of three or more of the following: cutaneous reaction (such as rash or exfoliative dermatitis), eosinophilia, fever, lymphadenopathy and one or more systemic complications such as hepatitis, nephritis, pneumonitis, myocarditis, and pericarditis; DRESS is sometimes fatal; discontinue therapy if DRESS suspected. 

Cutaneous adverse reactions, such as Stevens-Johnson syndrome, reported; severe cutaneous adverse reactions are sometimes fatal; discontinue therapy if suspected.

May cause orthostatic hypotension.

Suicide attempt is inherent in psychotic illness or bipolar disorder, close supervision of high-risk patients should accompany drug therapy 

Dopamine2 antagonists may elevate prolactin levels; long-standing hyperprolactinemia when associated with hypogonadism may lead to decreased bone density 

Leukopenia/neutropenia and agranulocytosis reported; possible risk factors for leukopenia/neutropenia include preexisting low white blood cell (WBC) count and history of drug-induced leukopenia/neutropenia 

If patient has history of clinically significant low WBC count or drug-induced leukopenia/neutropenia, monitor complete blood count (CBC) frequently during first few months of therapy; discontinue drug at first sign of clinically significant WBC decline <1000/μL in absence of other causative factors, and continue monitoring WBC count until recovery 

Antipsychotic agents have been associated with esophageal dysmotility and aspiration; use caution in patients at risk of pneumonia 

May cause QTc prolongation, which has been associated with development of malignant ventricular arrhythmias (torsade de pointes) and sudden death; discontinue therapy in patients with persistent QTc intervals >500 msec; avoid hypokalemia or hypomagnesemia 

Moderate to highly sedative; use caution when required to operate heavy machinery 

May cause core body temperature regulation impairment; use caution with heat exposure, strenuous exercise, dehydration, or taking medications with anticholinergic effects 

Make electrolyte imbalance corrections, especially hypomagnesemia or hypokalemia before and throughout therapy 

Use with caution in hepatic impairment

Seizure disorders; may cause hypotension, EPS, somnolence, and sensory instability.

Points of recommendation

You need to take the medicine exactly as prescribed by your doctor

Avoid working with dangerous equipment or driving until the effects of the medicine have been determined

Simultaneous use of drugs, diet, and herbal compounds and any co-morbidities (such as diabetes, seizure, dementia) should be reported to the doctor.

Avoid alcohol during treatment with Ziprasidone

Avoid increasing body heat or dehydration

You must inform your doctor if the patient is pregnant or intends to have a pregnancy or breastfeeding

Pregnancy level

C


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