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.

Read more at Wikipedia.org


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FDA drug approvals
From Geriatrics, 12/1/04

New indication:

Abilify[R]

Bristol-Meyers Squibb and Otsuka Pharmaceutical

Aripiprazole

Atypical antipsychotic indicated for treatment of acute bipolar mania, including manic and mixed episodes associated with bipolar disorder.

Aripiprazole is believed to exert its effect through a combination of partial agonist activity at D2 and 5-HT1A receptors and antagonist activity at 5-HT2A receptors.

Dosing. For acute bipolar mania, administer at a dose of 30 mg/d. Dose may be decreased to 15 mg/d based on individual patient tolerability. The dose of aripiprazole should be reduced to one-half the usual dose when administered concomitantly with potential CYP3A4 and CYP2D6 inhibitors.

Geriatric dosage adjustments. None recommended.

Pharmacokinetics. Of the 7,951 patients treated with aripiprazole in premarketing clinical trials, 991 (12%) were [greater than or equal to]65 and 789 (10%) were [greater than or equal to]75. There was no effect of age on the pharmacokinetics of a single 15-mg dose of aripiprazole. Aripiprazole clearance was decreased by 20% in elderly subjects ([greater than or equal to]65 years) compared to younger adult subjects (18 to 64 years).

Drugs used concomitantly with aripiprazole that induce CYP3A4 could cause an increase in aripiprazole clearance and lower blood levels. Drugs used that are inhibitors of CYP3A4 or CYP2D6 could inhibit aripiprazole elimination and cause increased blood levels.

Safety. NMS has been reported in association with the administration of antipsychotic drugs.

Aripiprazole may be associated with orthostatic hypotension.

Tardive dyskinesia, a syndrome of involuntary dyskinetic movements, may develop in patients treated with aripiprazole.

Antipsychotics have been associated with seizures, cognitive and motor impairment, disruption of body temperature regulation, and dysphagia.

Hyperglycemia, associated with ketoacidosis or hyperosmolar coma or death, may occur with the use of aripiprazole.

Adverse events. Commonly observed adverse events associated with aripiprazole include accidental injury, akathisia, headache, nausea, dyspepsia, vomiting, orthostatic hypotension, tremors, and constipation.

Patients who use ariprazole for extended periods should be periodically re-evaluated.

COPYRIGHT 2004 Advanstar Communications, Inc.
COPYRIGHT 2005 Gale Group

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