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Cariprazine: uses and side effects of this psychopharmaceutical

Cariprazine: uses and side effects of this psychopharmaceutical

August 10, 2022

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

Finding a treatment that palliates the symptoms and maintains stability in these subjects has been the goal of a large amount of research from different disciplines. Pharmacology is one of them, having synthesized different substances that diminish or temporarily eliminate the psychotic symptomatology. We are talking about antipsychotics. One of them, approved in 2015, is Cariprazine .

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Cariprazine as an antipsychotic

Cariprazine is a substance made and approved by the FDA in 2015, classified as an atypical antipsychotic . It is a substance with great effectiveness and developed for the purpose of suppressing or reducing psychotic symptoms, both at the level of symptoms that increase activity or add elements to the patient's usual functionality (called positive symptoms), such as hallucinations, delusions, restlessness or destructuring of thought.

However, this drug seems to be more effective than other drugs such as risperidone in the treatment of negative symptoms. A) Yes, has greater effect on those symptoms that reduce the level of activation of the patient , such as the poverty of thought or the apathy and anhedonia or inability to motivate or feel pleasure.

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Mechanism of action

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

Also, at the level of serotonin we find that it exerts different roles depending on the recipient 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 acting 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). Also also affects, although in a rather minor way, the noradrenergic and histaminergic system , something that can influence when generating 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 common in other disorders of the psychotic type, especially in those with delusions, agitation and hallucinations.

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

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

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Side effects and contraindications

Although very 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 population types.

Regarding side effects, It is usual to generate drowsiness and weight gain , being the most frequent and known symptoms. However, it can also cause agitation, dizziness, problems urinating or defecating, stomach problems such as indigestion, hypersalivation or blurred vision. In addition to this other more serious problems that may require medical attention is the possible experimentation of convulsions, muscular weakness, dark coloration of the urine (due to the problems of urination), loss of facial expression, falls, hyperthermia or alterations of consciousness, tachycardias , hyperglycemia and hypotension.

Some motor symptoms such as tremors and involuntary movements (such as those of dyskinesia) are also possible. As with the rest of antipsychotics or neuroleptics also we must be careful with the possible appearance of neuroleptic malignant syndrome , with deadly potential.

Regarding contraindications, as with many other antipsychotics, people with other pharmacological treatments should be especially careful with this medication, especially in the case of antidepressants, since there are a large number of medicinal substances that can interact with cariprazine. . Diabetic people should be especially careful, as it is common for this drug to generate elevations of blood sugar leading to hyperglycemia.

Likewise should be avoided by patients with cardiovascular disorders , who have suffered some type of stroke or who have dementia (multiplying the risk of mortality in this case). It should also be avoided during pregnancy, requiring a consultation with the doctor to assess alternatives, as it can 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 predominantly negative symptoms in patients with schizophrenia: a randomized, double-blind, controlled trial. Lancet.

Antipsychotics: Classification and Side Effects – Psychiatry | Lecturio (August 2022).

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