The most used drugs against schizophrenia

Schizophrenia is one of the most well-known mental disorders history, and even today receives a lot of attention. The presence of hallucinations, delusions and disorganized behaviors, together with a possible negative symptomatology such as alogia, has generated through the ages a deep suffering to those who suffer it, often being stigmatized and institutionalized.

It would not be until the appearance of the first psychotropic drugs that they would not begin to be able to control their symptoms effectively. Since then, a large number of substances have been investigated and synthesized whose main objective is to control the symptoms of schizophrenia. In fact, even today pharmacological treatment is a fundamental element. In this article we are going to do a little review of the most used drugs against schizophrenia, as well as its disadvantages and limitations.

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Antipsychotics: basic operation

Antipsychotics or neuroleptics are a group of drugs whose main objective is

treatment of psychotic symptomatology by chemical changes in the brain. Its mechanism of action is based on the regulation of dopamine levels in the brain.

Chief among them is the mesolimbic pathway, which in patients with schizophrenia presents an excess of dopamine that would end up generating the experimentation of positive symptoms such as hallucinations. At this point, all existing antipsychotics claim to reduce the amount of dopamine in this area in order to reduce psychotic symptoms, acting specifically on D2 receptors, which it blocks.

The first antipsychotics discovered worked very well in this regard, causing a great decrease in positive psychotic symptoms. However, there is another pathway that is also of great importance: the mesocortical pathway. This pathway has in subjects with schizophrenia a decrease in dopamine that causes the subject to manifest negative symptoms such as alogia or poverty of thought and other disturbances such as withdrawal and loss of skills.

Although typical antipsychotics have the function of reducing the level of dopamine in the mesolimbic pathway, the truth is that they exert its action in a non-specific way, causing said reduction to occur in other nerve pathways and even in other parts of the body. organism. Among the pathways affected would be the mesocortical.

Bearing in mind that the negative symptoms are caused by an absence or deficit of dopamine in it, the use of typical neuroleptics will not only have no effect but may actually harm and increase negative symptoms. And furthermore, other pathways that acted in a normative way are also negatively affected, being able to generate very annoying secondary symptoms that can interfere with daily life. For this reason, the investigation was directed to generate to look for alternatives, coming to elaborate with time those known as atypical neuroleptics.

These are known to also act as dopamine D2 receptor agonists, like typical ones, but also acting on the level of serotonin in the brain. Taking into account that serotonin has an inhibitory effect on dopamine secretion and that there is a much higher level of serotonergic receptors in the cortex than dopaminergic, reducing serotonin will mean that although the drug lowers dopamine in the cortex, the inhibition of an inhibitor ends up causing the levels to rise. keep. In this way, the level of dopamine in the mesolimbic pathway is reduced but not in the mesocortical pathway, while secondary symptoms from other pathways are also reduced.

The most widely used psychoactive drugs against schizophrenia

Although historically the typical antipsychotics have been more used, the truth is that in the currently, due to the lower number of secondary symptoms and its greater effect on the symptoms negative, In clinical practice, the most common is to find typical antipsychotics. Despite this, the typical ones are still used with some frequency. Below we can see some of the most commonly used drugs against schizophrenia, both atypical and typical.

The most currently used: atypical antipsychotics

Although at the level of controlling the positive symptoms they have a level comparable to the typical ones, the atypical antipsychotics have a series of great advantages over them. These include the existence of a certain effect on negative symptoms and the lower risk and frequency of undesirable secondary symptoms. Despite this, they can generate sexual effects, arrhythmias, extrapyramidal effects linked to movement such as akinesia or tardive dyskinesia, hyperglycemia, feeding and weight disturbances and others issues.

The most commercialized and used drugs against schizophrenia in Spain They are the following, although there are many more:

Clozapine

One of the best known atypical neuroleptics. Clozapine has a good effect even in subjects who do not respond to other neuroleptics. Also in those who with other drugs suffer from extrapyramidal symptoms due to the alteration dopaminergic in the nigrostriatal pathway (in fact it is considered the neuroleptic with the least effects extrapyramidal).

Aside from over dopamine and serotonin, acts at the level of adrenaline, histamine and acetylcholine. However, it also generates metabolic changes, overweight and there is also a risk of agranulocytosis, with which its use is more limited than that of the rest of atypicals and tends to be used as second option.

Risperidone

In addition to schizophrenia, risperidone is also used in the treatment of aggressive behavior in minors with severe conduct disorders. Also in bipolar disorder and in autism.

Olanzapine

Another of the best-known drugs against schizophrenia, olanzapain is used especially to combat both positive and negative psychotic symptoms. Like some of the above, it has also been used for the treatment of bipolar disorder, and in some cases for borderline personality disorder. It is one of the most effective antipsychotics, similar to clozapine but with greater serotonergic affinity (which will generate a greater effect on negative symptoms).

As with the rest secondary symptoms include appetite and weight disturbances, sexual problems (decreased libido and possible galactorrhea and gynecomastia), tachycardia and hypotension among many others.

• Related article: "Olanzapine: operation and effects of this psychoactive drug"

Aripiprazole

This type of atypical antipsychotic has been used for schizophrenia, but also for other alterations in which there is great agitation as in some cases of autism and for the disorder major depressive. It is a relatively new drug, synthesized in 2002. It stands out for being a partial agonist of D2 receptors (acting only depending on the dopamine levels of the pathway in question). It is effective in the treatment of positive, negative and affective symptoms. It does not cause sexual problems.

The most frequent typical neuroleptics

Although they are currently much less used than atypicals because they tend to generate more and more powerful side effects, it is frequent to find that some classic neuroleptics continue to be used in drug-resistant cases in which the atypical ones do not work or well and under certain conditions. In this sense, although there are many more, two stand out as the best known and most frequent.

haloperidol

The best known of all antipsychotics, it has been the most used until the birth of atypical neuroleptics and in fact it continues to be used as a treatment for schizophrenia. Its injected use is frequent to treat acute crises and stabilize the patient, even if you later switch to another type of medication.

In addition to schizophrenia, it is used in other psychotic disorders (being very effective in the treatment of positive symptoms), or other disorders that generate psychomotor agitation: disorders by ticks and Tourette's syndrome, manic episodes or delirium tremens among others. Occasionally it has been used as an analgesic and antiemetic.

• Related article: "Haloperidol (antipsychotic): uses, effects and risks"

Chlorpromazine

Another of the most common and well-known antipsychotics, it is in fact the first antipsychotic that was found. Effects and indications similar to haloperidol. Occasionally it has also been used for the treatment of tetanus and porphyria, or as a last option in the case of OCD.

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Antiparkinsonians

Due to the probability of extrapyramidal effects typical of neuroleptics (especially the typical ones), anti-Parkinsonian medication is often added to antipsychotic medication. In this sense, the use of elements such as Levodopa is frequent.

Reflection on its disadvantages and limitations

The pharmacological treatment of schizophrenia is essential and must be given continuously throughout the life cycle in order to prevent the occurrence of flare-ups. However, it is relatively common to find cases in which patients have suffered a flare-up after deciding to quit.

The truth is The consumption of psychoactive drugs on a continuous basis presents a series of disadvantages and limitations. In the first place, the continued consumption of a certain substance will cause the body to end up taking a certain degree of tolerance towards it, with which the effects may become less. This is one of the reasons why it is not uncommon for dose changes or direct medication changes (using other active ingredients).

Another great limitation of neuroleptics is that although they have a great effect on positive symptoms (highlighting hallucinations, delusions, agitation and disorganized behavior and speech) the effectiveness on negative symptoms (poverty of speech and thought) still leaves little to be desired. want. In fact, typical antipsychotics either have an effect on the latter and can even make them worse. Fortunately, the atypicals do have an effect on this symptomatology, although they still have a wide margin for improvement.

In addition to this, the great disadvantage generated by the presence of possible secondary symptoms stands out. The most common (not in vain another name of the first antipsychotics was that of major tranquilizers) is excessive sleepiness and sedation, which can limit the creativity and cognitive ability of the subject. This can affect, for example, their performance at work or academics.. Alterations at the motor level may also appear, some of them affecting the extrapyramidal pathways. (although this is more frequent in the typical ones), and in some cases they also have an effect in the field sexual. In addition, weight gain, hypercholesterolemia and hyperglycemia are also favored.

They may be a risk factor for some diseases, and could be a risk for patients with some metabolic problems such as diabetes (its use is contraindicated in diabetic patients, with liver problems and heart). They are also not recommended during pregnancy and lactation or in subjects with dementia.

Finally, a limitation of the use of psychoactive drugs is the fact that in acute phases or people who do not accept their diagnosis there may be a high level of resistance or even forgetfulness of consumption. Fortunately in this regard some drugs have depot presentations, which are injected intramuscularly and are gradually released into the bloodstream over time.

Thus, although the use of antipsychotics is essential to prevent flare-ups and maintain symptoms under control, we must take into account that it has its limitations and can generate some problematic. This should lead to further research to find and synthesize new drugs that allow a much more specific action and produce fewer effects. side effects, as well as to assess and measure with great precision the type of medicine and the doses that we use in each case in order to produce the greatest possible well-being of the patient. patient.