Psychotic disorders, with schizophrenia as the main and most recognized representative, are one of the types of mental disorders that generate the greatest amount of suffering and functional disturbance in the lives of people who suffer from it.

Finding a treatment that allows for the alleviation of symptoms and the maintenance of stability in these subjects has been the objective of a great deal of research from different disciplines. Pharmacology is one of them, having synthesized different substances that decrease or temporarily eliminate psychotic symptoms. We are talking about antipsychotics. One of them, approved in 2015, is cariprazine .

Cariprazine as an antipsychotic

Cariprazine is a substance developed and approved by the FDA in 2015, classified as an atypical antipsychotic . It is a highly effective substance designed to suppress or reduce psychotic symptoms, both at the level of symptoms that increase activity or add to a patient’s usual functioning (called positive symptoms), such as hallucinations, delusions, restlessness or impaired thinking.

However, this drug appears to be more effective than other drugs such as risperidone in treating negative symptoms. Thus, has a greater effect on those symptoms that reduce the level of activation of the patient , such as alogia or poverty of thought or abulia and anhedonia or inability to be motivated or feel pleasure.

Mechanism of action

Cariprazine is considered an atypical or second generation antipsychotic. As such, it generates an affectation in the brain neurochemistry by altering the dopaminergic and serotoninergic systems. Unlike most antipsychotics, which block brain dopamine, cariprazine is considered a partial agonist of this neurotransmitter (i.e., it generates an effect similar to that of endogenous dopamine), something that has been associated with the improvement in negative symptoms generated by the deficit of this hormone at the mesocortical level.

Likewise, at the serotonin level we find that it plays different roles depending on the receptor in question. It acts as a partial agonist of the 5-HT1a receptor, which influences the reduction of dopamine synthesis in some brain areas, while it acts as an antagonist of the 5-HT2a and 5-HT2b receptors (which on the other hand generates an increase in dopamine levels in the mesocortical pathway). It also affects, albeit to a much lesser extent, the noradrenergic and histaminergic system , which may influence the generation of side effects.

Main uses

The main indication that cariprazine has is schizophrenia , in which it seems to have a high level of effectiveness in the treatment of both positive and negative symptoms. It is also commonly used in other psychotic disorders, especially those with delusions, agitation and hallucinations.

It has also been indicated for some cases of bipolar disorder. Specifically, it has been approved for use in the presence of acute manic or mixed episodes, helping to reduce the current level of hyperactivity and excessively expansive mood.

Although it does not yet have such an action, the possible application of this drug in cases of depression (both unipolar and in the depressive episodes of bipolar disorder) or even in autism, similar to what happens with aripiprazole and risperidone, has yet to be investigated.

Side effects and contraindications

Although highly effective in the treatment of different conditions and mental disorders, cariprazine is a substance that can also generate different side effects and even be totally contraindicated (or require extreme regulation) for some specific types of population.

In terms of side effects, is common to generate drowsiness and weight gain , being the most frequent and known symptoms. However, in addition to this it can cause agitation, dizziness, problems with urination or defecation, stomach problems such as indigestion, hypersalivation or blurred vision. In addition to this, other more serious problems that may require medical attention are the possible experience of convulsions, muscle weakness, dark coloring of the urine (due to urination problems), loss of facial expression, falls, hyperthermia or alterations of consciousness, tachycardia, hyperglycemia and hypotension.

Some motor symptoms such as tremors and involuntary movements (like those of dyskinesia) are also possible. As with other antipsychotics or neuroleptics as well , care must be taken with the possible appearance of neuroleptic malignant syndrome , with the potential for death.

As for contraindications, as with many other antipsychotics, special caution should be exercised with this drug by people receiving other drug treatments, especially in the case of antidepressants, as there are a large number of medicinal substances that can interact with cariprazine. People with diabetes should be especially careful, since it is common for this drug to generate elevations in blood sugar that lead to hyperglycemia.

Likewise should be avoided by patients with cardiovascular disorders , who have suffered some type of stroke or who present dementia (in this case multiplying the risk of mortality). Its consumption should also be avoided during pregnancy, requiring a consultation with the physician to assess alternatives, since it may be a risk for the appearance of malformations or alterations in the fetus.

Bibliographic references

  • Németh, G.; Laszlovsky, I.; Czobor, P. et al (2017). Cariprazine versus risperidone monotherapy for treatment of predominant negative symptoms in patients with schizophrenia: a randomized, double-blind, controlled trial. Lancet.