Cariprazine, a new antipsychotic

Cariprazine was approved by the United States Food and Drug Administration or FDA in 2015. Then, in 2018, it was authorized in Spain and It is marketed under the Reagila trademark..

Cariprazine is an atypical antipsychotic. Its effectiveness has been noted against the negative symptoms of schizophrenia, although it is also effective against positive symptoms. Likewise, it is useful to prevent the appearance of relapses in these patients.

Schizophrenia is one of the chronic diseases with the highest morbidity and mortality today.. It is estimated that it affects approximately 1% of the population. Nowadays, new drugs are being investigated, such as cariprazine, that can improve the course of the disease and the quality of life of patients.

What is cariprazine used for?

According to its technical sheet, cariprazine is indicated for the treatment of schizophrenia in adults. As it is a very new drug, other possible indications are still being tested and investigated.

In a study published by the journal The Lancet Its efficacy was compared to another atypical antipsychotic, such as risperidone. The results support its effectiveness in treating the negative symptoms of schizophrenia.

Likewise, cariprazine is used to treat episodes of depression, mania or mixed episodes in people with bipolar I disorder.

This medication is usually given by mouth once a day.. The recommended initial dose is 1.5 mg, although it can subsequently be increased up to 6 mg per day, depending on the intensity and damage of the side effects.

Mechanism of action

Its mechanism of action is not completely known.. It is considered a dopamine partial agonist, although it has affinity for various receptors with different actions on each of them:

partial agonist action on receptors: D2 and D3 for dopamine5-HT1A for serotoninAntagonist action on receptors:5-HT2A and 5-HT2B of serotoninH1 of histamine

This mechanism of action is similar to that of aripiprazole, another atypical antipsychotic. used in patients with schizophrenia, bipolar disorder and manic episodes. As the main difference with this, cariprazine has a more powerful affinity for the dopamine D3 receptor.

D3 receptors appear to be an important new therapeutic target in relation to negative symptoms of schizophrenia. Hence, this drug appears as a new reference and hope for the treatment of this disease.

For its part, cariprazine has two active metabolites, that is, with pharmacological activity:

DCAR: desmethyl cariprazine.DDCAR: didesmethyl cariprazine.

Cariprazine has a fairly long elimination half-life, as do its metabolites. Therefore, its effects can continue to manifest, even if treatment is suspended or the dosage is modified. In this sense, we must monitor any adverse effects that may appear. The lowest effective dose should be used.

Cariprazine Side Effects

The most frequent adverse reactions in treatment with cariprazine are the appearance of akathisia and parkinsonism.. Akathisia is a feeling of restlessness that doesn’t let you sit still. Regarding parkinsonism, the most common symptoms are reduced movement, muscle rigidity, slow thinking, etc.

Furthermore, according to Mayo Clinicmay appear other unwanted effectsas:

reduced appetiteconstipationdrowsinessstomach paindifficulty sleepinganxietyback painbelchingdry mouthheartburndigestionirritabilitypain in extremitiesweight gain

Many of these effects are dose dependent.. That is, they appear or worsen as the dose increases. Therefore, we must always communicate to the specialist any discomfort we detect during treatment. This way, he or she will be able to adjust the dose and avoid the appearance of unwanted reactions.

However, some side effects can be serious. Therefore, as indicated by the information services of the United States National Library of Medicine, If you experience any of these symptoms, contact your doctor immediately or seek emergency medical assistance:

seizuresinvoluntary body movementsinability to move or slow movementsfallsconfusionhyperventilationirregular heartbeatdifficulty to swallowtrouble breathinginflammation of the face, throat, tongue, lips, or eyes dark-colored urineinflammation of the extremitiesrash or itchy skin

According to the information of Mayo Clinic, that we have already mentioned previously, we can also observe the following side effects that require immediate medical attention, although their appearance is rare:

bladder painreduced urine productionburning urinationincreased thirstloss of consciousnessmuscle painssore throatstuffy nosetiredness or weaknessvomitingsuicidal thoughts or attempts

The following symptoms may also appear, but they are not a side effect, but rather as Signs of an overdose: sedation, lightheadedness, dizziness, and fainting. In these cases, you should also go to the doctor immediately to receive the care required for detoxification.

Special warnings and precautions for use

Research published in the Journal of Alzheimer’s disease reports and in JAMA psychiatry indicates that The use of antipsychotics in people with dementia increases their chances of dying. Therefore, cariprazine should not be used in psychotic patients with dementia. We recommend that you consult with a specialist if any of your family members diagnosed with dementia are receiving treatment with antipsychotics.

On the other hand, it is also necessary to highlight that the emergence of suicidal behavior (suicidal ideas, suicide attempts and suicide) is inherent to psychotic illnesses and, in general, this usually appears at the beginning or before any modification of antipsychotic treatment.

In this sense, antipsychotic treatment should be accompanied by close supervision in high risk patients. Especially at the beginning of treatment and any time your dose is increased or decreased.

Before using cariprazine

The health portal MedlinePlus, which we have already mentioned, suggests that you tell your doctor if: you are allergic to cariprazine; you take other prescription and over-the-counter medications (including supplements and vitamins); you consume herbal products (especially St. John’s wort); you have or have had low levels of red blood cells; have had seizures, a stroke, a mini-stroke, or heart failure; you are pregnant or plan to become pregnant.

For its part, Mayo Clinic, It also recommends that you should notify them if you suffer from:

circulation problemsdehydrationheart problemsdiabeteshyperglycemiahypotensionleukopenianeuroleptic malignant syndrome (NMS)seizurestardive dyskinesiadifficulties swallowingkidney diseasesliver diseases

If you have had some of these problems in the past, but you no longer have them, you should also tell your doctor. This background can help you a lot when evaluating your case and choosing the intervention route.

Final considerations

Cariprazine is a new antipsychotic drug effective against the negative symptoms of schizophrenia. It is the result of research that is still continuing to face the challenges that diseases of this nature pose. currently.

Therefore, it should be used with caution and only under the supervision of a doctor. Under no circumstances should you self-medicate with an antipsychotic (or any other type of drug). Consult a professional to determine the best treatment option for you.

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