Aripiprazole chemical structure
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Aripiprazole

Aripiprazole (produced by Bristol-Myers Squibb and sold as Abilify®) is the sixth and most recent of the atypical antipsychotic medications to be approved by the FDA for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. more...

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Pharmacology

Aripirazole possesses a novel mechanism of action when compared to the other FDA approved atypical antipsychotics (i.e. clozapine, olanzapine, quetiapine, ziprasidone, and risperidone). Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. Partial agonism at D2 receptors has been shown to modulate dopaminergic activity in areas where dopamine activity may be high or low, such as the mesolimbic and mesocortical areas of the schizophrenic brain, respectively. In addition to partial agonist activity at the D2 receptor, aripirazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.

Pharmacokinetics

Aripiprazole displays linear kinetics with an elimination half-life of approximately 75 hours. Accordingly, steady state plasma concentrations are achieved in about 14 days. Cmax (maximum plasma concentration) is achieved in 3-5 hours after oral dosing. The bioavailabilty of the oral tablets is about 90%. The drug undergoes extensive hepatic metabolization (dehydrogenation, hydroxylation, and N-dealkylation). The active major metabolite is dehydro-aripiprazole with an elemination half-life of about 94 hours. The parent drug is excreted only in traces and the metabolites, whether active or not, are excreted via feces and urine.

Metabolism

Aripiprazole is metabolized by the Cytochrome P450 isoenzymes 3A4 and 2D6. Accordingly, coadministration of aripiprazole with medications that may inhibit (e.g. paroxetine, fluoxetine) or induce (e.g. carbamazepine) these metabolic enzymes may increase or decrease, respectively, plasma concentrations of aripiprazole.

Adverse Events

Adverse events reported in the package insert for aripiprazole include headache, nausea, vomiting, somnolence, insomnia, and akathisia. It appears that aripirazole has a low incidence of EPS (extrapyramidal side effects). The risk of tardive dyskinesia with prolonged aripirazole use is unclear.

Dosage Forms

Aripirazole is available in 5mg, 10mg, 15mg, 20mg, and 30mg tablets.

Warnings About Medications with Similar Names

A warning has gone out recently because of this drug's name. The '-prazole' ending of this drug name makes this drug sound like it is one of the proton pump inhibitors (such as omeprazole, pantoprazole, lansoprazole) which are used in treating peptic ulcer disease. However, aripiprazole and these drugs are in an entirely different class of drugs altogether and confusing the two can lead to some unnecessary side effects.

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Zyprexa Warning
From Maine Nurse, 5/1/04

Eli Lilly and Company would like to inform you of important labeling changes regarding Zyprexa (olanzapine). The Food and Drug Administration (FDA) has asked all manufacturers of atypical antipsychotic medications, including Lilly, to add a Warning statement describing the increased risk of hyperglycemia and diabetes in patients taking these medications, including Zyprexa. In addition to Zyprexa, the atypical antipsychotic class includes Clozaril® (clozapine, Novartis), Risperdal® (risperidone, Janssen), Seroquel® (quetiapine, AstraZeneca), Geodon® (ziprasidone, Pfizer), and Abilify® (aripiprazole, Bristol Myers Squibb and Otsuka American Pharmaceutical). Accordingly, the Zyprexa prescribing information has been updated with the following information:

WARNINGS

Hyperglycemia and Diabetes Mellitus

Hyperglycemia, in some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, has been reported in patients treated with atypical antipsychotics including Zyprexa. Assessment of the relationship between atypical antipsychotic use and glucose abnormalities is complicated by the possibility of an increased background risk of diabetes mellitus in patients with schizophrenia and the increasing incidence of diabetes mellitus in the general population. Given these confounders, the relationship between atypical antipsychotic use and hyperglycemia-related adverse events is not completely understood. However, epidemiological studies suggest an increased risk of treatment-emergent hyperglycemia-related adverse events in patients treated with the atypical antipsychotics. Precise risk estimates for hyperglycemia related adverse events in patients treated with atypical antipsychotics are not available.

Patients with an established diagnosis of diabetes mellitus who are started on atypical antipsychotics should be monitored regularly for worsening of glucose control. Patients with risk factors for diabetes mellitus (e.g., obesity, family history of diabetes) who are starting treatment with atypical antipsychotics should undergo fasting blood glucose testing at the beginning of treatment and periodically during treatment. Any patient treated with atypical antipsychotics should be monitored for symptoms of hyperglycemia including polydipsia, polyuria, polyphagia and weakness. Patients who develop symptoms of hyperglycemia during treatment with atypical antipsychotics should undergo fasting blood glucose testing. In some cases, hyperglycemia has resolved when the atypical antipsychotic was discontinued; however, some patients required continuation of anti-diabetic treatment despite discontinuation of the suspect drug.

Should you have any questions or concerns regarding this important safety information, please contact your Eli Lilly and Company sales representative or contact the Lilly medical department at 1-800-Lilly-RX. Please refer to the full prescribing information for Zyprexa included with this letter. As always, we request that serious adverse events be reported to Lilly at 1-800-Lilly-Rx or to the FDA MedWatch program by phone (1-800-FDA-1088), by fax (1-800-FDA-0178) or by e-mail (www.fda.gov/medwatch).

Copyright Main State Nurses' Association May-Jul 2004
Provided by ProQuest Information and Learning Company. All rights Reserved

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