Using Cariprazine to Ameliorate Negative Symptoms and Metabolic Side Effects of Clozapine and Paliperidone – Clinical Cases

Abstract

Introduction Cariprazine is a third-generation antipsychotic approved in Europe in 2017 for the treatment of schizophrenia. It presents distinct pharmacodynamic properties, such as D3/D2 partial agonism, preferential binding to D3 receptors, antagonism at the serotonin 5-HT2A and 5-HT2B receptors, partial agonism at 5-HT1A receptors, and low affinity to other receptors (including noradrenergic, histaminergic, and cholinergic). It has demonstrated efficacy in the treatment of positive and negative symptoms of schizophrenia with a safe side effect and metabolic profile. Methods Here, we describe one clinical case of a patient that benefited from an add-on of cariprazine to a regimen of clozapine; and two clinical cases of patients that benefited from the switch from clozapine and paliperidone long-acting injectable to cariprazine. Results and Discussion Those cases illustrate how cariprazine can be used in patients with schizophrenia in the treatment of both positive and negative symptoms, and when aiming to ameliorate the metabolic burden associated with other treatments. However, further studies are needed to consubstantiate those findings.

Cariprazine: An Antipsychotic Medication with High Therapeutic Potential

“…In patients who have undergone ineffective antipsychotic treatment trials, the addition of cariprazine to clozapine resulted in observable improvements in patient functioning, reductions in the severity of positive, 9 negative, depressive, and anxiety symptoms [28,29,30]. There are cases of patients with clozapine-resistant schizophrenia, who show improvement after the use of cariprazine alone with significantly fewer side effects [14,31,32]. Cariprazine may be useful, when aiming to ameliorate the metabolic burden associated with clozapine or other antipsychotic treatment, as it is noted for low potential for weight gain and metabolic side effects [18,33,34].…”

A review on the pharmacology of cariprazine and its role in the treatment of negative symptoms of schizophrenia

“…Steady state of paranoid delusions and aggressiveness was achieved with 2 weeks of cariprazine treatment (79). Cariprazine as adjunctive or monotherapy also resulted in remission of negative symptoms (5,25,64,74).…”