Molindone: uses and side effects of this drug

The treatment of schizophrenia has been and continues to be an area of ​​great relevance worldwide, having 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. Although it is not one of the best known and in fact in 2010 its sale was suspended, one of the typical or first generation antipsychotics is molindone, which we are going to talk about in this article.

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What is the grinder?

Molindone is a classified psychoactive drug within the group of antipsychotics, medicines that help fight the symptoms of disorders such as schizophrenia and chronic delusional disorder. Its action contributes to reduce alterations of perception such as hallucinations or delusions, as well as to cause a decrease in the level of brain activation of the subject and even decrease their level of aggressiveness.

It is a phenylbutylpiperidine, like pimozide, and although it is considered to be It has a profile similar to atypical antipsychotics such as quetiapine or clozapine., is generally considered a typical or first-generation antipsychotic (although some studies do considered an outlier, there is no evidence to show that their action corresponds to this class of neuroleptic).

This drug was withdrawn from the market by its creators in 2010. And it is that although in different studies molindone was shown to be practically as effective as other antipsychotics, including both typical and atypical, however can generate a large number of symptoms secondary. Its use was not widespread and it is no longer marketed, although some generic derivative can still be found in some places.

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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 dopamine D2 and D1 receptors. However, its effect and affinity for these receptors is 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 (point at which there is an excess of dopamine in subjects with schizophrenia) but rather acts nonspecifically in the brain. This generates that other brain areas whose dopamine levels were within normal or even low also suffer from decreased dopamine levels, which can lead to secondary symptoms nasty. This is what happens with the nigrostriatal and tuberoinfundibular pathways, as well as the mesocortical pathways.

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, together with other psychotic disorders. In this sense, it was effective in reducing the level of activation and hallucinations. Besides it It has been seen to be of some use in the treatment of conduct disorders. linked to aggressiveness, as well as hyperactivity.

Side effects

Molindone is a psychoactive drug that at the time was considered useful and effective. 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 to this, it generates a significant drop in weight (something unusual in antipsychotics), urinary retention, hyperactivity, dry mouth, facial expressionlessness, sleep problems such as insomnia, problems urinating, depression or agitation.

It is important to note that we are dealing with a typical neuroleptic, with which its effect on dopamine occurs nonspecifically throughout the brain. In this sense, it is especially frequent that it can generate severe motor symptoms such as agitation, dyskinesia or convulsions.

Akathisia is relatively common or inability to keep still. Sexual symptoms may also appear and those linked to the production of prolactin (when dopamine is reduced in the tuberoinfundibular pathway, production of prolactin is released) such as emission of milk from the breast or galactorrhea (in both sexes), decreased libido or alterations in the cycle menstrual.

Some rare but more serious secondary symptoms are the aforementioned possibility of having seizures, the presence of visual disturbances, fever, disturbances of consciousness, rashes, tachycardia or bradycardia or respiratory problems, among others. There is also the risk of developing neuroleptic malignant syndrome, a potentially fatal syndrome that makes it essential to control the dosage of the drug.

contraindications

As main contraindications, Its consumption together with alcoholic beverages should be avoided. and depressant substances. Neither are 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 Special caution should be exercised with this drug. People with dementia should not take this medicine (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 conditions. Children under 12 years of age, pregnant women and lactating women should avoid their consumption.

Bibliographic references:

• Bagnall, A.M.; Fenton, M.; Kleijnen, J. & Lewis, R. (2007). Molindone for schizophrenia and severe mental illness. Cochrane Database of Systematic Reviews, 1. Art. No.: CD002083. DOI: 10.1002/14651858.CD002083.pub2
• Imming, P.; Sinning, C. & Meyer, A. (2006). Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov.;5(10):821-34.