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Contraindications and side effects of Molindone

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Discover the Contraindications and side effects of Molindone.

This antipsychotic is used against the symptoms of schizophrenia, such as hallucinations.

Contraindications and side effects of Molindone

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The treatment of schizophrenia has been and continues to be an area of great relevance worldwide, has generated a large amount of research in this regard.

One of the most explored elements is the creation of different substances with psychoactive effects that allow a reduction and control of symptoms, the main ones being those classified as antipsychotics or neuroleptics.

In this group, we can find different types of substance, classified in turn into two large groups: first-generation or typical and second-generation or atypical.

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Although it is not one of the best known and its sale was suspended in 2010, one of the typical or first-generation antipsychotics is molindone, which we are going to talk about in this article.

What is molindone?

Molindone is a psychotropic drug classified within the group of antipsychotics, medicines that help fight the symptoms of disorders such as schizophrenia and chronic delusional disorder.

Its action contributes to reducing perceptual alterations such as hallucinations or delusions, as well as causing a decrease in the level of brain activation of the subject and even reducing their level of aggressiveness.

It is a phenyl butyl piperidine, like pimozide, and although it is considered to have a profile similar to atypical antipsychotics such as quetiapine or clozapine, it is generally considered atypical or first-generation antipsychotics (although some studies consider it an atypical, there is no evidence to show that its action corresponds to this class of neuroleptics).

This drug was withdrawn from the market by its creators in 2010.

And although in different studies molindone was shown to be practically as effective as other antipsychotics, including both typical and atypical, it can nevertheless generate a large number of secondary symptoms.

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Its use was not very widespread and it is no longer commercialized, although in some places a generic derivative can still be found.

Mechanism of action

As a typical antipsychotic, the main mechanism of action of molindone is based on the interaction at the dopaminergic level that it generates in the brain.

Specifically, it works by blocking the dopamine D2 and D1 receptors. However, its effect and affinity for these receptors are much lower than that of other antipsychotic drugs. In addition to this, it also has cholinergic and adrenergic effects.

However, this action is not limited solely to the mesolimbic dopaminergic pathway (the point at which there is an excess of dopamine in subjects with schizophrenia) but it acts in a nonspecific way in the brain.

This causes that other brain areas whose dopamine levels were within the usual or even low also suffer a decrease in dopamine levels, which can lead to unpleasant secondary symptoms.

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This is what happens with the nigrostriatal and tuberoinfundibular pathways, as well as the mesocortical pathway.

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Main applications in disorders

Molindone is a drug that at the time was useful in different disorders.

The main indication for which it was approved is schizophrenia, along with other psychotic disorders. In this sense, it was effective in reducing the level of activation and hallucinations.

In addition, it has been seen as of certain users for the treatment of behavior disorders linked to aggressiveness, as well as hyperactivity.

Side effects of Molindone

Molindone is a psychotropic drug that was considered useful and effective at the time. However, in some cases, it can cause a series of aversive and undesirable side effects.

The most common is the presence of drowsiness and sedation, like most neuroleptics.

In addition, it generates a significant decrease in weight (something unusual in antipsychotics), urinary retention, hyperactivity, dry mouth, facial expressionlessness, sleep problems such as insomnia, urination problems, depression, or agitation.

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It is important to note that we are dealing with a typical neuroleptic, with which its effect on dopamine occurs in a nonspecific way over the entire brain.

In this sense, it is especially frequent that it can generate severe motor symptoms such as agitation, dyskinesia, or seizures.

Akathisia, or the inability to keep still, is relatively common. Sexual symptoms related to prolactin production may also appear (as dopamine in the tuberoinfundibular pathway decreases, prolactin production increases), such as emission of milk from the breast or galactorrhea (in both sexes), decreased libido, or abnormalities. of the menstrual cycle.

Some rare but more serious secondary symptoms are the aforementioned possibility of having seizures, the presence of visual disturbances, fever, altered consciousness, rashes, tachycardia or bradycardia, or respiratory problems, among others.

There is also the risk of the neuroleptic malignant syndrome, a life-threatening syndrome that makes drug dosage control essential.

Contraindications of Molindone

As the main contraindications, its joint consumption with alcoholic beverages and depressant substances should be avoided.

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Neither subjects with epilepsy or with low levels of leukocytes and urinary problems, nor with breast cancer (which it can stimulate).

Also, subjects with renal and hepatic insufficiency should be especially cautious with this drug.

People with dementia should not consume this drug (in fact the Food and Drug Administration (FDA) has not authorized its use in these cases), since it increases the probability of death during treatment in elderly subjects with this type of condition.

Children under 12 years of age, pregnant and lactating women should avoid its consumption.

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