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CLINICAL POTENTIAL OF CARIPRAZINE IN THE TREATMENT OF ACUTE MANIA

Kürşat Altınbaş orcid id orcid.org/0000-0003-2899-0096 ; Department of Psychiatry, Çanakkale Onsekiz Mart University, Çanakkale, Turkey
Sinan Guloksuz ; Department of Psychiatry, Yale University School of Medicine, New Haven, Connecticut, USA, Department of Psychiatry and Psychology, Maastricht University Medical Centre, EURON, Maastricht, The Netherlands
Esat Timuçin Oral ; Department of Psychology, Istanbul Commerce University, Istanbul, Turkey


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Sažetak

Cariprazine (RGH-188, trans-4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexyl-amine
hydrochloride), is a novel antipsychotic with dopamine D2 and D3 receptors antagonist–partial agonist properties. Cariprazine has
also moderate affinity for serotonin 5-hydroxytryptophan (5-HT) 1A receptors, high affinity for 5-HT1B receptors with pure
antagonism and low affinity for 5-HT2A receptors. Randomized, double blind, placebo controlled, flexible-dose (3–12 mg/day)
studies have demonstrated cariprazine is effective in both schizophrenia and acute manic episodes associated with bipolar disorder.
The incidence of serious adverse events in cariprazine arm was no different than in placebo arm in these studies. The most common
adverse events were extrapyramidal symptoms, headache, akathisia, constipation, nausea, and dyspepsia which can be explained
with cariprazine’s partial dopamine agonism. Although cariprazine treatment was associated with a higher incidence of treatmentemergent
adverse events, particularly akathisia and tremor, common side effects of marketed second generation antipsychotics such
as weight gain, metabolic disturbances, prolactin increase or QTc prolongation were not associated with cariprazine, probably due
to its moderate to low binding affinity for histamine H1 and 5-HT2C receptors. Animal studies show that cariprazine may have
additional therapeutic benefit on impaired cognitive functioning with D3 receptor activity, however clinical data is still scarce. The
aim of this article is to review the potential use of cariprazine for the treatment of acute manic episodes in the light of the preclinical
and clinical trials reported to date.

Ključne riječi

cariprazine – antipsychotic – psychopharmacology - bipolar disorder - mania

Hrčak ID:

161186

URI

https://hrcak.srce.hr/161186

Datum izdavanja:

17.9.2013.

Posjeta: 930 *