These Are The Most Used Drugs Against Schizophrenia

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Schizophrenia is one of the best known mental disorders of history, and even today it receives a lot of attention. The presence of hallucinations, delusions and disorganized behavior, together with possible negative symptoms such as alogia, has generated deep suffering over time for those who suffer from it, often being stigmatized and institutionalized.

It would not be until the appearance of the first psychotropic drugs that their symptoms would begin to be controlled effectively. Since that time, 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 short review of the most used drugs against schizophrenia as well as its disadvantages and limitations.

Antipsychotics: basic operation

Antipsychotics or neuroleptics are a group of drugs whose main objective is to the treatment of psychotic symptoms through chemical changes in the brain Its mechanism of action is based on the regulation of dopamine levels in the brain.

The main one is the mesolimbic pathway, which in patients with schizophrenia presents an excess of dopamine that would end up generating the experience of positive symptoms such as hallucinations. At this point, all existing antipsychotics aim to reduce the amount of dopamine existing 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 sense, causing a great decrease in positive psychotic symptoms. However, there is another pathway that is also of great importance: the mesocortical. In subjects with schizophrenia, this pathway has a decrease in dopamine that causes the subject to manifest negative symptoms such as alogia or poverty of thought and other alterations such as withdrawal and loss of abilities.

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

Taking into account that negative symptoms are caused by an absence or deficiency of dopamine in it, The use of typical neuroleptics will not only have no effect but may actually harm and increase negative symptoms. And in addition, other pathways that acted in a normative manner are also negatively affected, potentially generating very annoying secondary symptoms that can interfere with daily life. For this reason, research was aimed at generating alternatives, eventually developing those known as atypical neuroleptics.

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

The most used psychotropic drugs against schizophrenia

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

The most used currently: atypical antipsychotics

Although they have a comparable level of controlling positive symptoms to typical antipsychotics, atypical antipsychotics have a series of great advantages over them. Among them, the existence of a certain effect on negative symptoms and the lower risk and frequency of undesirable secondary symptoms stand out. Despite this, they can generate sexual effects, arrhythmias, extrapyramidal effects linked to movement such as akinesia or tardive dyskinesia, hyperglycemia, eating and weight alterations, and other problems.

The most marketed and used anti-schizophrenia drugs 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 extrapyramidal symptoms due to the dopaminergic alteration in the nigrostriatal pathway (in fact it is considered the neuroleptic with the least extrapyramidal effects).

Apart from 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, so its use is more limited than that of the rest of the atypicals and it tends to be used as a second option.

Risperidone

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

Olanzapine

Another of the best-known drugs against schizophrenia, olanzapaine is used especially to combat both positive and negative psychotic symptoms. Like some of the previous ones, 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 although with greater serotonergic affinity (which will generate a greater effect on negative symptoms).

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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.

Aripiprazole

This type of atypical antipsychotic has been used for schizophrenia, but also for other disorders in which there is great agitation, such as in some cases of autism and for major depressive disorder. 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 generate sexual problems.

The most common typical neuroleptics

Although they are currently much less used than the atypical ones because They tend to generate more and more powerful side effects, it is common to find that some classic neuroleptics continue to be used in drug-resistant cases in which atypical ones do not work or under certain conditions. In this sense, although there are many more, two stand out as the most well-known and 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. It is frequently used injected to treat acute crises and stabilize the patient even if you subsequently 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: tic disorders and Tourette syndrome, manic episodes or delirium tremens, among others. It has occasionally been used as an analgesic and antiemetic.

Chlorpromazine

Another of the most common and well-known antipsychotics, It is in fact the first antipsychotic found With 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.

Antiparkinsonian

Due to the probability of extrapyramidal effects typical of neuroleptics (especially typical ones), Antiparkinsonian 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

Pharmacological treatment of schizophrenia is essential and must be given continuously throughout the entire life cycle in order to prevent the presence of outbreaks. However, it is relatively common to find cases in which patients have suffered an outbreak after having decided to stop.

The truth is The continuous consumption of psychotropic drugs presents a series of disadvantages and limitations Firstly, the continued consumption of a certain substance will cause the body to end up gaining a certain degree of tolerance towards it, so the effects may become minor. This is one of the reasons why it is not uncommon for changes in dosage or medication directly (using other active ingredients).

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Another major limitation of neuroleptics is that although they have a great effect on positive symptoms (highlighting hallucinations, delusions, agitation, and disorganized behavior and speech), their effectiveness on negative symptoms (poverty of speech and thought) still leaves something to be desired. In fact, typical antipsychotics do not have an effect on the latter and they can even make them worse. Fortunately, the atypical ones do have an effect on this symptomatology, although they still have a wide margin for improvement.

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

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

Finally, a limitation of the use of psychotropic drugs is the fact that in acute phases or in people who do not accept their diagnosis there may be high resistance or even forgetting to use them. Fortunately in this sense Some drugs have depot presentations, which are injected intramuscularly and are released little by little into the bloodstream over time.

Thus, although the use of antipsychotics is essential to prevent outbreaks and keep symptoms under control, we must keep in mind that they have their limitations and can cause some problems. This should lead to greater research to find and synthesize new drugs that allow a much more specific action and produce fewer adverse effects, as well as to assess and measure with great precision the type of medication and the doses we use in each case. in order to produce the greatest possible well-being of the patient.