The suffering of different mental disorders by the population has made that throughout history different mechanisms and measures have been sought to be applied in order to treat these affections. Even in ancestral and prehistoric cultures, rituals such as trepanning have been carried out for this purpose. However, over the years, different methodologies have been refined which are very effective in the treatment of these disorders.

Among them we find the synthesis of substances that eliminate or reduce the symptoms: psychopharmaceuticals. As far as schizophrenia is concerned, drug treatment is now considered to be of great importance for the maintenance and stabilization of patients. And among the many existing psychopharmaceuticals we can find aripiprazole , which we will discuss in this article.

Aripiprazole: what is it?

Aripiprazole is a psychoactive drug classified as an antipsychotic or neuroleptic, specially designed to have a positive effect on the reduction and elimination of the symptoms of schizophrenia and psychotic disorders , such as delusions and hallucinations and psychomotor agitation.

Within antipsychotics it is classified as atypical , because its creation is based on the attempt to develop effective drugs in the treatment of these symptoms without producing the level of side effects that the typical or classic ones have, as well as to increase the effectiveness in the treatment of a type of symptomatology, the negative one (those symptoms that reduce the functionality of the skills present in the patient, such as impoverishment of thinking and abulia), which the typical antipsychotics do not treat or even may harm.

And in this task it is especially efficient, contributing to fight both positive and negative symptoms. In addition, it has the advantage of having a possible administration in the form of an intramuscular injection in depot format (slow release) at a monthly level, and in these cases it is not necessary to take the drug orally on a continuous basis.

Mechanism of action

Aripiprazole is, as we said, an atypical antipsychotic. As with most of these neuroleptics, its effects are due to its action on two neurotransmission systems: dopamine and serotonin . However, their mechanism of action is somewhat different from that of other atypicals with regard to dopamine.

While most antipsychotics, both typical and atypical, often work by blocking the brain’s D2 dopamine receptors, this is not the case with aripiprazole. This drug is in fact a partial agonist of the D2 receptors, favouring in principle their presence in the brain . This would, in principle, allow an increase in positive psychotic symptoms, but it does, however, reduce them.

This reduction is explained by the performance on serotonin. The rest of the atypicals decrease cerebral serotonin in such a way that it stops inhibiting dopamine in the areas that do not need a reduction of it, so that the blocking action they generally produce has an effect on the mesolimbic pathway (positive symptoms such as hallucinations are produced by an excess in this pathway) but in the cortex this blocking effect is reduced and compensated for by the inhibition of an inhibitor (serotonin).

In the case of aripiprazole, this effect occurs in part in some types of serotonin receptors, being blocked by the drug, while on the other hand it stimulates its synthesis as a partial agonist of the 5-HT1a receptors. This contributes to a decrease in the level of dopamine in some areas while it increases in others.

Indications

The main indication for aripiprazole is the treatment of schizophrenia and other psychotic disorders. In this sense contributes to reduce or eliminate positive symptoms , either in the form of hallucinations, agitation or behavioral disorders, while having positive effects on negative ones (abulia, thought poverty and emotional flattening among others). It is also used to keep those suffering from these disorders stable, from the age of fifteen onwards.

It has also been used effectively in the treatment of manic episodes in the context of bipolar disorder, from the age of thirteen. Not only in the treatment of acute crises, but also in the prevention of further episodes. However, in some subjects it is possible that the consumption of this drug triggers manic episodes .

In addition to the above indications, this drug is also sometimes used in the treatment of problems such as Tourette’s disorder or autism, usually to control their clinical manifestations.

Side effects

Although useful in many disorders, aripiprazole is a psychoactive drug that can cause many side effects of varying severity.

Among the most frequent we can find the presence of drowsiness and fatigue, weight gain, headache, increased appetite, nervousness , hypersalivation, muscle pain, gastrointestinal disorders, diarrhea or constipation and balance problems. Insomnia and anxiety are common. More serious ones would include alterations of consciousness, hyperglycemia, respiratory distress, muscle stiffness, visual disturbances, arrhythmias and dyskinesias, as well as thoughts of suicide. Unlike other antipsychotics, sexual or motor disorders are not common.

In addition, it has been observed in recent years how the administration of this drug has been associated in some cases (although it is not common) with an increase in impulsivity, gambling, hyperphagia, increased libido and the pursuit of sexual relations and the existence of compulsive behaviours such as shopping. In short, it has been associated in some people with the existence of loss of impulse control, something that can have various consequences for the person in question.

Contraindications and risks

Aripiprazole is a very powerful drug that can generate various effects in the body, and can pose a considerable risk and is contraindicated in different types of population.

Among those who should not consume this drug we can find those people with allergy to it or to some of its components. This drug is also highly contraindicated for people suffering from dementia, increasing the risk of death in these cases. The presence of cardiopathies or cardiovascular and cerebrovascular diseases also make this drug somewhat contraindicated.

People with diabetes should avoid this drug, as its use can raise blood sugar levels greatly and lead to dangerous hyperglycemia. Those with liver or kidney disease should not use aripiprazole if their condition is severe, or at least should discuss the doses taken with their doctor. Also, people with epilepsy are at risk for severe seizures if they take this drug. Another of its contraindications is in pregnant and lactating women, since it increases the risk for the fetus and the drug is transmitted through the placenta and through breast milk.

Aripiprazole can interact with different medications, an interaction that can be harmful. These drugs include some of those used in the treatment of HIV, as well as antidepressants, antihypertensive drugs and some anticonvulsants. It should also not be taken with alcohol or other drugs .

With regard to the loss of impulse control, special caution should be taken by those who already suffer from such a disorder, subject to substance dependence (whether or not they are already uninhabited), bipolarity (despite the fact that it is a possible drug to use for treatment) and obsessive-compulsive disorder.

Bibliographic references

  • Salazar, M.; Peralta, C.; Pastor, J. (2011). Manual of Psychopharmacology. Madrid, Editorial Médica Panamericana.