Objective: Aripiprazole, a synthetic compound, obtained by chemical modification of the
structure of quinolinone is considered as an atypical antipsychotic drug. The present review is an attempt
to summarize the updated information related to reported chemistry and pharmacology of Aripiprazole.
Development: Aripiprazole, under development by Otsuka Pharmaceutical, was approved by the U.S.
Food and Drug Administration (USFDA) by the end of 2002 with an aim to treat patients with schizophrenia.
This drug got approved by European Commission in February 2013 to treat the patients having
severe manic episodes in bipolar I disorder Additionally, it got approval in Japan in January 2006 and in
Canada in 2014.
Pharmacology: Aripiprazole shows high specificity for dopamine receptor especially D2 and D3, serotonin
5-HT1A and serotonin 5-HT2A receptors, reasonable specificity for dopamine D4, serotonin 5-
HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors. It also shows moderate specificity for
the serotonin reuptake. The major side effects include headache, agitation, akithesia, anxiety, tachycardia,
insomnia, postural hypotension, constipation, vomiting, dizziness, nervousness and somnolence.
Conclusion: The present article embarks the available information on Aripiprazole with emphasis on its
clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism and