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 allows alleviating symptoms and maintaining stability in these subjects has been the objective of a large amount of research from different disciplines. Pharmacology is one of them, having synthesized different substances that temporarily reduce or 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 made with 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 disorganization of thought.
However, this drug seems to be more effective than other drugs such as risperidone in terms of treating negative symptoms. So, has the greatest effect on those symptoms that reduce the patient’s level of activation such as alogia or poverty of thought or abulia and anhedonia or inability to motivate or feel pleasure.
Mechanism of action
Cariprazine is considered an atypical or second-generation antipsychotic. As such, it affects brain neurochemistry, altering the dopaminergic and serotonergic systems. Unlike most antipsychotics, which block brain dopamine, cariprazine is considered a partial agonist of said neurotransmitter (that is, they generate an effect similar to that of endogenous dopamine), something that has been seen to be associated with the improvement in the negative symptoms generated by the deficiency of this hormone at the mesocortical level.
Likewise, at the level of serotonin 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). Likewise also affects, although in a much 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. Its use is also common in other psychotic disorders, especially in those that present 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, helping to reduce the level of current hyperarousal and excessively expansive mood.
Although it does not yet have this action, The possible application of this drug in cases of depression remains to be investigated (both unipolar and in depressive episodes of bipolar disorder) or even in autism, in a similar way to what happens with aripiprazole and risperidone.
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.
As far as side effects are concerned, It is common to cause drowsiness and weight gain, being the most frequent and well-known symptoms. However, in addition to this, it can 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 are the possible experience of seizures, muscle weakness, dark coloring of urine (due to urination problems), loss of facial expressiveness, falls, hyperthermia or alterations in consciousness, tachycardia. , 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, Care must be taken with the possible appearance of neuroleptic malignant syndrome with deadly potential.
Regarding contraindications, as with many other antipsychotics, people who receive other pharmacological treatments should take special caution 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, since it is common for this drug to generate elevations in blood sugar that lead to hyperglycemia.
In addition patients with cardiovascular disorders should avoid it, 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 doctor to evaluate alternatives, since it may be a risk for the appearance of malformations or alterations in the fetus.