Sertindole: characteristics and side effects of this drug.
A summary of the characteristics of this antipsychotic drug used against schizophrenia.
Among the different mental disorders and alterations, schizophrenia is probably one of those that generates the greatest alteration in the person who suffers from it, since it produces a rupture or split between the psyche and reality.
Although there is currently no treatment that eliminates and cures this condition, fortunately we do have different methods and treatments that allow us to prevent and control the symptoms. One of the pillars of these treatments are neuroleptic or antipsychotic psychotropic drugs, of which there is a wide variety.
Among these drugs developed to treat this problem we find sertindole, which will be discussed in this article..
What is sertindole?
It receives the name of sertindole a psychopharmaceutical belonging to the group of the antipsychotics or neurolepticsThese are substances that act on the organism by modifying brain chemistry in such a way that they reduce or eliminate psychotic symptoms while they are in effect, especially at the level of symptoms such as hallucinations, delirium and agitation.
It is an effective an effective drug derived from phenylindoleIt has the advantage over other neuroleptics in that it does not generate, or at least not as frequently, the same level of sedation as other drugs of the same type, nor as many extrapyramidal or motor symptoms. It is available in pharmacy in the form of film-coated tablets, for oral administration.
Among the antipsychotics sertindole is classified as atypical or second generation. This group of drugs was designed to be effective not only against the so-called positive symptomatology of schizophrenia and other psychotic disorders, i.e., symptoms that add some element to the patient's activity, such as hallucinations and delusions (something for which the first-generation antipsychotics were already effective); they were also intended to have a therapeutic effect on the negative symptomatology, which involves the loss or reduction of the subject's capacities.
It was also sought that they should do so in a safe manner and generate the least number of side effects. and generate as few side effects as possible (the first generation (first generation drugs generated a large number of possible side effects that were bothersome and in some cases could be dangerous).
Sertindole was withdrawn from sale in Spain in 1998 due to the existence of indications of a possible relationship between consumption of the drug and some cases of heart problems and deaths in the United Kingdom, but after eight years of analysis and clinical studies it was decided to lift the ban as no increase in the risk of mortality in the general population was observed. However, it was decided to include people with heart disease in the group of people contraindicated for the drug, and it is necessary to maintain medical monitoring of the drug. it is necessary to maintain medical monitoring of the patient's condition and evolution..
Mechanism of action of this substance
The mechanism of action of sertindole, i.e. the way in which it affects the organism, is based on its action on certain neurotransmitters.
Specifically, sertindole acts as a neurotransmitter, sertindole acts as a dopamine antagonist at its D2 receptors.This action would generate a decrease in positive symptomatology, since an excess of dopamine has been observed in the mesolimbic pathway of people with this type of symptomatology. This action would be the one that generates a decrease of the positive symptomatology, since an excess of dopamine has been observed in the mesolimbic pathway of people with this type of symptomatology.
In addition, it is also an antagonist it is also an antagonist of serotonin 5-HT2 and alpha1-adrenergic receptors.. In this sense, it has a long-lasting effect.
Being a serotonin antagonist, which itself inhibits dopamine synthesis, makes it effective in the treatment of negative symptomatology and generates fewer side effects than classical neuroleptics. The reason for this is that while positive symptoms are generated by an excess of dopamine in the mesolimbic pathway, negative symptomatology has been associated with a deficit of dopamine in the mesocortical pathway.
Serotonin is a dopamine inhibitor and its receptors are found in a high proportion in the cortex, so by inhibiting the inhibitor the dopamine levels in this area do not decrease and even increase (while they do decrease where they have to, in the mesolimbic pathway).
For which disorders is it indicated?
Sertindole is a useful drug, and as an antipsychotic or neuroleptic its main therapeutic indication is in the treatment of schizophrenia..
However, due to the existence of cardiovascular risk, it is not a treatment of choice, and at present it is only used when there is no response or intolerance to other antipsychotic drugs, and only when there is no acute and emergency symptomatology. In case of use, it is necessary to monitor and make periodic controls to the patient.
Possible side effects
Although sertindole is a useful drug in the treatment of schizophrenia, the administration of this substance can generate annoying and even dangerous side effects..
Among the most frequent we can find dizziness, nasal congestion, hypotension, tingling or paresthesia, weight gain, or dry mouth..
In addition, although less common, hyperglycemia, loss of consciousness, convulsive crises, tardive dyskinesia, ejaculation difficulties (the volume of ejaculated liquid is reduced) and/or erectile dysfunction, peripheral edema may also appear.
Among the frequent ones, one of the most dangerous, and the reason why it was withdrawn, is found in increased risk of cardiac eventsThe QT interval is prolonged, which facilitates the possible occurrence of arrhythmias in at-risk populations.
Torsade de Pointes arrhythmias may also appear, in which there is ventricular tachycardia and a drop in blood pressure (may cause fainting and, in complex cases, even death). Another possibility is the occurrence of venous or pulmonary thrombosis and embolism, although this is not common. Finally, there is a risk of neuroleptic malignant syndrome, also potentially fatal.
Contraindications
Although this drug can be beneficial for the treatment of certain pathologies, it should also be taken into account that the effect of sertindole on the organism can be dangerous for some sectors of the population. In this sense, we can find that some people have contraindications for this drug.
People who are allergic to this drug should not take sertindole. Due to the cardiovascular risk, this drug is contraindicated in the following cases those who have suffered any type of coronary or cerebrovascular event.. It is also contraindicated in people with severe hepatic insufficiency.
Pregnant and lactating women should avoid its consumption, and in the case of the latter, if there is no other option, breastfeeding should be interrupted. It is also not indicated in children.
People with diabetes or who have had seizures should avoid it or at least maximize medical control, as well as those who are taking other drugs among which we can find examples of some antidepressants, antiarrhythmics, other antipsychotics or even Antibiotics and antihistamines (the suitability and possible interaction between drugs should be medically evaluated).
(Updated at Apr 13 / 2024)