CLINICAL POTENTIAL OF CARIPRAZINE IN THE TREATMENT OF ACUTE MANIAReportar como inadecuado




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Psychiatria Danubina, Vol.25 No.3 September 2013. -

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.

cariprazine – antipsychotic – psychopharmacology - bipolar disorder - mania



Autor: Kürşat Altınbaş - ; Department of Psychiatry, Çanakkale Onsekiz Mart University, Çanakkale, Turkey Sinan Guloksuz - ; Depar

Fuente: http://hrcak.srce.hr/



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