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[[Image:aripiprazole.png|right|chemical structure of aripiprazole]]
'''Aripiprazole''' (brand name: '''Abilify<sup>&reg;</sup>''') is the sixth, and most recent, of the second generation [[antipsychotic]] (or [[atypical antipsychotic]]) medications to hit the market. Aripirazole is FDA approved for the treatment of [[schizophrenia]]. Additionally, there is some evidence from randomized, placebo controlled trials that aripirazole is effective for the treatment of acute [[mania]], although it is not FDA approved for this indication.
'''Aripiprazole''' (brand name: '''Abilify<sup>&reg;</sup>''') is the sixth, and most recent, of the second generation [[antipsychotic]] (or [[atypical antipsychotic]]) medications to hit the market. Aripirazole is FDA approved for the treatment of [[schizophrenia]]. Additionally, there is some evidence from randomized, placebo controlled trials that aripirazole is effective for the treatment of acute [[mania]], although it is not FDA approved for this indication.



Revision as of 22:21, 17 September 2004

chemical structure of aripiprazole
chemical structure of aripiprazole

Aripiprazole (brand name: Abilify®) is the sixth, and most recent, of the second generation antipsychotic (or atypical antipsychotic) medications to hit the market. Aripirazole is FDA approved for the treatment of schizophrenia. Additionally, there is some evidence from randomized, placebo controlled trials that aripirazole is effective for the treatment of acute mania, although it is not FDA approved for this indication.


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 scizophrenic 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 is achieved in 3-5 hours after oral dosing. The bioavailabilty of the oral tablets is about 90%.


Metabolism

Aripirazole is metabolized by the Cytochrome P450 isoenzymes 3A4 and 2D6. Accordingly, coadministration of aripirazole 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 risks of tardive dyskinesia with prolonged aripirazole use is unclear.


Dosage Forms

Aripirazole is available in 5mg, 10mg, 15mg, 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.

Aripiprazole was develeloped by Otsuka Pharmaceutical Co., Ltd and is manufactured by the Bristol Myers Squibb pharmaceutical company (NYSE: BMY).

Aripiprazole was approved by the FDA on November 15, 2002.