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Chlorpromazine: effects and uses of this psychopharmaceutical

Chlorpromazine: effects and uses of this psychopharmaceutical

July 19, 2024

In antiquity, schizophrenia and psychotic disorders had a treatment that allowed to fight the different symptoms and perceptive and cognitive alterations.

This would change with the discovery of the first antipsychotics, and for the first time patients with these disorders can receive outpatient treatment without requiring hospitalization. One of the first and best known is chlorpromazine .

  • Related article: "Types of antipsychotics (or neuroleptics)"

Chlorpromazine: description and a little history

Chlorpromazine is a substance belonging to the group of antipsychotics or neuroleptics , which have a great effect in the control of psychotic symptoms such as hallucinations, agitation and delirium.

It is one of the first antipsychotics, and is part of the group of classic or typical neuroleptics. Structurally it is a phenothiazine. Although it is true that although currently chlorpromazine continues to be used in the treatment of psychopathologies such as schizophrenia, the use of other types of antipsychotics is usually preferred due to the risks and side effects that the classics can generate, at the time they were a revolution and they have served (and continue to serve in many cases) to greatly improve the quality of life of patients with various mental disorders.

This substance was discovered and synthesized by chance by Paul Charpentier in 1950 while looking for a remedy against malaria. However, some time later Henri Laborit, after observing its tranquilizing effects without necessarily causing sedation, would begin to recommend and establish its use in psychiatry. It would be used for the first time in the treatment of psychotic psychopathologies in 1951, with a remarkable success that would lead to the discovery to be called the fourth revolution in psychiatry.

And is that previously the methods used to treat psychotic patients were usually ineffective, risky and highly aversive and painful for the patient (for example induce insulin coma or the use of electroshock). The fact that chlorpromazine was effective allowed a more biologicist view of psychotic disorders and would begin to allow outpatient treatment instead of requiring hospitalization in most cases.

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Mechanism of action

As we have mentioned, chlorpromazine is one of the classic or typical antipsychotics. This type of antipsychotic acts by blocking the dopamine receptors in the brain, especially the D2 receptor.

The fact that this blockade is a benefit is due to the fact that in schizophrenia, positive symptoms such as hallucinations, disturbances of thought and language, distraction, agitation and restlessness tend to be due to the presence of an excess of dopamine in the pathway. mesolimbic By blocking its emission there is a great improvement of the psychotic symptomatology of this type.

However both chlorpromazine and the rest of classical antipsychotics affect dopamine receptors non-specifically, that is, throughout the brain. In this way not only the pathway that presents an excess of dopamine is affected, but other pathways that had adequate or even low levels are seen to be in excess of their levels of this neurotransmitter. It also has an effect on acetylcholine and other neurotransmitters. This causes secondary symptoms of varying severity to appear.

In addition, in schizophrenia, other symptoms also appear in which there is a flattening, slowing down or reduction of functions and processes, especially at the cognitive level. The most classic example of these symptoms (called negative) is the alogia or poverty of thought. These symptoms are linked to a dopaminergic deficit in the mesocortical pathway , so that the effect of chlorpromazine not only does not prove positive in these symptoms but could also lead to some worsening.

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Side effects and risks of chlorpromazine

As with other psychotropic drugs, the use of chlorpromazine can have a number of side effects and risks to be taken into consideration. As mentioned above, by exerting an antagonistic effect on dopamine in all pathways it is possible that problems arising from it arise.

One of the main problems derived from the decrease of dopamine, specifically when it occurs in the nigrostriatal pathway, are the appearance of motor disorders such as slowing, akathisia, dystonia, stiffness and tremors both by themselves and in what is called parkinsonian syndrome. Another of the frequent symptoms is tardive dyskinesia or emission of repetitive and involuntary movements of the face and sometimes of the trunk and extremities.

In the tuberoinfundibular pathway, the blockade of dopamine can cause the presence of alterations such as galactorrhea or emission of milk through the breasts (regardless of sex), gynecomastia or breast growth (also in both sexes) and alterations in sexual response.

It has also been commented that chlorpromazine and other typical antipsychotics can cause side effects from their interaction with acetylcholine . Among them we find mental dullness, constipation, blurred vision or ocular hypertension.

Other side effects referred to with certain frequency are a high level of sedation and a remarkable weight gain , there must be caution in cases of food or metabolic problems. It can also cause problems such as high blood pressure or dizziness, having effects on the cardiovascular system.

Finally one of the most serious syndromes and may end with patient's death (although it is very unusual) is the neuroleptic malignant syndrome, in which fever, cyanosis, tachycardia and in some cases coma and even death appear. It is in prevention of this syndrome and other problems by which the dosage of this type of substances is done with extreme care.

Situations and disorders for which it is indicated

One of the most widespread uses of chlorpromazine is even today (although there is a preference for the use of atypical neuroleptics such as olanzapine due to its greater safety and its effects on negative symptoms) the treatment of schizophrenia and other psychotic disorders .

However, chlorpromazine has also been shown to be effective in treating manic states. In general, it is effective in all situations where there are positive psychotic symptoms or states of intense motor agitation. This includes the presence of delirium and in some withdrawal syndromes. It has been used successfully at the time of reduce choreic symptoms in Huntington's Korea , and sometimes it can be used as a last option in cases of OCD.

At a more physiological level, we observe that it is sometimes used to treat intestinal problems such as nausea and vomiting (since it is antiemetic), tetanus or porphyria.

Also, given its tranquilizing potential, sometimes it has also been used in situations where there are problems with sleep (not in vain, at first antipsychotics were called the major tranquilizers). Also in situations that deal with high pain .

Bibliographic references:

  • Gómez, M. (2012). Psychobiology CEDE Preparation Manual PIR.12. CEDE: Madrid.
  • Mazana, J.S .; Pereira, J. and Cabrera, R. (2002). Fifty years of chlorpromazine. Spanish Journal of Penitentiary Health, vol.4 (3). CP Tenerife II. Medical services.
  • Salazar, M .; Peralta, C .; Pastor, J. (2006). Manual of Psychopharmacology. Madrid, Panamericana Medical Publishing House.

The Evidence for Chlorpromazine (July 2024).

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