Affiliation:
1. Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology, CHARUSAT-Campus,
Changa-388421, Anand, Gujarat, India
2. North Carolina State University, North Carolina, USA
Abstract
Abstract:
Cariprazine is a piperazine derivative approved by the USFDA in 2015 as a novel atypical
antipsychotic drug (APD) to treat adults with schizophrenia and bipolar manic or mixed episodes in
adults. However, due to the partial agonist action on dopamine D2, D3 receptors, and serotonin 5-HT1A
receptors as well as the antagonist effect on 5-HT2A, 5-HT2B, and H1 receptors, cariprazine differs
pharmacologically from other APDs, both typical and atypical. Moreover, cariprazine also has a
unique pharmacokinetic profile due to the formation of two clinically significant metabolites:
desmethyl-cariprazine (DCAR) and desmethyl-cariprazine (DDCAR). They are eliminated by
CYP3A4 and also, to a lesser extent, by CYP2D6. Here, we also review the effectiveness, safety, as
well as current clinical update of cariprazine in bipolar I disorder associated with/without mania and
schizophrenia through randomized and post-hoc analysis. The potential benefits of cariprazine as a
promising therapeutic alternative in addressing major clinical requirements for better therapy of such
severe neuropsychiatric conditions were demonstrated in this summarized review study.
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology,General Neuroscience
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