Sertindole: Characteristics And Side Effects Of This Drug

Sertindole

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 a rupture or split occurs 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 in order to treat this problem we find sertindole, which we will talk about throughout this article

What is sertindole?

It is called sertindole. a psychotropic drug belonging to the group of antipsychotics or neuroleptics which are substances that act on the body by modifying brain chemistry in such a way that they reduce or eliminate psychotic symptoms while they have an effect, especially at the level of symptoms such as hallucinations, delusions and agitation.

Is about an effective drug derived from phenylindole, which also compared to other neuroleptics has the advantage that it does not generate, or at least not as frequently, either the same level of sedation as other drugs of the same type or as many extrapyramidal or motor symptoms. It is available in pharmacies in the form of film-coated tablets, for oral administration.

Among antipsychotics, sertindole is classified as atypical or second generation. This group of drugs was designed with the purpose of being effective not only against the so-called positive symptoms of schizophrenia and other psychotic disorders, that is, symptoms that add some element to the patient’s activity, such as the aforementioned hallucinations and delusions (something for which first-generation antipsychotics were already effective); It was also wanted that they have a therapeutic effect on negative symptoms, which entails the loss or decrease of the subject’s capabilities.

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Likewise, it is also sought that they do so safely and generating the fewest possible side effects (the first generation generated a large number of possible annoying side effects and in some cases could be dangerous).

Sertindole was withdrawn from sale in Spain during 1998 due to the existence of indications of a possible relationship between the consumption of the drug and some cases of heart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 withdraw the ban as no increase in the risk of mortality in the general population was observed. However, to do so, it was decided to incorporate the population with heart ailments among the group of people who are contraindicated for the drug, and 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, that is, the way in which it affects the body, is based on its action on certain neurotransmitters.

Specifically, Sertindole acts as a dopamine antagonist at its D2 receptors, that is, it blocks and hinders its action and decreases its concentration in the brain. This action would be what generates a decrease in positive symptoms, since an excess of dopamine has been observed in the mesolimbic pathway of people with this type of symptoms.

In addition to that It is also an antagonist of serotonin 5-HT2 and alpha1 adrenergic receptors In this sense it has a long-lasting effect.

Being an antagonist of serotonin, which itself inhibits dopamine synthesis, makes it effective in the treatment of negative symptoms and generates fewer side effects than classic neuroleptics. The reason for this is that while positive symptoms are generated by an excess of dopamine in the mesolimbic pathway, negative symptoms have been associated with a deficit of dopamine in the mesocortical pathway.

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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 go down where they have to, in the mesolimbic pathway).

For what 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 currently it is only used when there is no response or one is intolerant to other antipsychotic drugs and as long as there are no acute and emergency symptoms. In case of use, it is necessary to monitor and perform periodic checks on the patient.

Possible side effects

Although sertindole is a useful drug in the treatment of schizophrenia, The administration of this substance can cause 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, seizures, tardive dyskinesia, ejaculation difficulties (the volume of ejaculated fluid is reduced) and/or erectile dysfunction, peripheral edema may occur.

Among the frequent ones, one of the most dangerous, and the reason why it was removed, is found in increased risk of cardiac events: The QT interval is prolonged, something that facilitates the possible appearance of arrhythmias in the at-risk population.

Torsade de Pointes arrhythmias may also appear, in which there is ventricular tachycardia and a drop in blood pressure (it can cause fainting and, in complex cases, even death). Another possibility is the appearance of thrombosis and venous or pulmonary embolisms, although this is not common. Finally, the risk of neuroleptic malignant syndrome, also with fatal potential, stands out.

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Contraindications

Although this drug can be beneficial for the treatment of certain pathologies, the truth is that it must also be taken into account that the effect of sertindole on the body can be dangerous for some sectors of the population. In this sense, we can find that some people have this drug contraindicated.

Sertindole should not be taken by those who are allergic to this medication. Due to the cardiovascular risk, this drug is contraindicated those who have suffered some type of coronary or cerebrovascular event It is also contraindicated in people with severe liver failure.

Pregnant and lactating women They should avoid its consumption, and in the case of the latter, if there is no other option, breastfeeding should be stopped. It is also not indicated in the childhood stage.

Those who have diabetes or 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 (you should the appropriateness and possible interaction between drugs should be medically evaluated).