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Home / Drugs / Starting with A / Aripiprazole
 
Aripiprazole
 

Aripiprazole is an atypical antipsychotic medication used 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. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole 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.
BrandsAbilify
Abilitat
CategoriesAntipsychotics
Antipsychotic Agents
ManufacturersOtsuka pharmaceutical co ltd
Otsuka pharmaceutical development and commercialization inc
Bristol-Myers Squibb Company
PackagersBristol-Myers Squibb Co.
Bryant Ranch Prepack
Cardinal Health
Comprehensive Consultant Services Inc.
DispenseXpress Inc.
E.R. Squibb and Sons LLC
Murfreesboro Pharmaceutical Nursing Supply
Otsuka America
PD-Rx Pharmaceuticals Inc.
Physician Partners Ltd.
Physicians Total Care Inc.
Quality Care
Rebel Distributors Corp.
Remedy Repack
Resource Optimization and Innovation LLC
Southwood Pharmaceuticals
Stat Rx Usa
SynonymsOPC 31
OPC-14597

indication

For the treatment of schizophrenia and related psychotic disorders.

pharmacology

Aripiprazole is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Aripiprazole is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Aripiprazole acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Aripiprazole. Aripiprazole's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Aripiprazole's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug.

mechanism of action

Aripiprazole's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia.

biotransformation

Hepatic.

half life

75-146 hours

route of elimination

Less than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces.

drug interactions

Carbamazepine: Carbamazepine, a strong CYP3A4 inducer, may decrease the serum concentration of aripiprazole by increasing its metabolism.

Dihydroquinidine barbiturate: Quinidine increases the effect and toxicity of aripiprazole

Itraconazole: Itraconazole may increase the effect of aripiprazole.

Ketoconazole: Ketoconazole may increase the effect of aripiprazole.

Quinidine: Quinidine increases the effect and toxicity of aripiprazole

Quinidine barbiturate: Quinidine increases the effect and toxicity of aripiprazole

Tacrine: Tacrine, a central acetylcholinesterase inhibitor, may augment the central neurotoxic effect of antipsychotics such as Aripiprazole. Monitor for extrapyramidal symptoms.

Telithromycin: Telithromycin may reduce clearance of Aripiprazole. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Aripiprazole if Telithromycin is initiated, discontinued or dose changed.

Terbinafine: Terbinafine may reduce the metabolism and clearance of Aripiprazole. Consider alternate therapy or monitor for therapeutic/adverse effects of Aripiprazole if Terbinafine is initiated, discontinued or dose changed.

Tetrabenazine: May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.

Triprolidine: The CNS depressants, Triprolidine and Aripiprazole, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.

Voriconazole: Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of aripiprazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of aripiprazole if voriconazole is initiated, discontinued or dose changed.