Molindone: uses and side effects of this drug

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

The treatment of schizophrenia has been and continues to be an area of great relevance worldwide, having generated a great deal of research in this regard. One of the most explored elements is the creation of different substances with psychoactive effects. 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 substances, 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 molindonewhich we are going to talk about in this article.

What is molindone?

Molindone is a psychotropic drug classified as a within the group of antipsychoticsIt is an antipsychotic, a drug that helps to combat the symptoms of disorders such as schizophrenia and chronic delusional disorder. Its action contributes to reduce perceptual disturbances such as hallucinations or delusions, as well as to cause a decrease in the level of brain activation of the subject and even to reduce his level of aggressiveness.

It is a phenylbutylpiperidine, like pimozide, and although it is considered to have a profile similar to that of antipsychotics, it is also considered to have a profile similar to that of pimozide. Although it is considered to have a profile similar to atypical antipsychotics such as quetiapine or clozapine, it is generally considered an atypical antipsychotic.It is generally considered a typical or first generation antipsychotic (although some studies consider it an atypical, there is no evidence that its action corresponds to this class of neuroleptic).

This drug was withdrawn from the market by its creators in 2010.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

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 acts 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, it also has cholinergic and adrenergic effects.

However, this action is not only limited to the mesolimbic dopaminergic pathway (where there is an excess of dopamine in subjects with schizophrenia) but also acts non-specifically in the brain. acts in a non-specific way in the brain.. This causes other brain areas whose dopamine levels were within normal or even low to also suffer a decrease in dopamine levels, which can lead to unpleasant secondary symptoms. This is what happens with the nigrostriatal and tuberoinfundibular pathways, as well as the mesocortical.

Main applications in disorders

Molindone is a drug that once had utility 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. In addition to this has been seen to be of some use in the treatment of behavioral disorders linked to aggressiveness, as well as hyperactivity. linked to aggressiveness, as well as hyperactivity.

Side effects

Molindone is a psychotropic drug that was once considered useful and effective. However, in some cases can lead to a number of aversive and undesirable side effects..

The most common is the presence of drowsiness and sedation, as with most neuroleptics.. It also causes a significant weight loss (something unusual in antipsychotics), urinary retention, hyperactivity, dry mouth, facial expressionlessness, sleep problems such as insomnia, urination problems, depression or agitation.

It is important to emphasize that we are dealing with a typical neuroleptic, so that its effect on dopamine is non-specific over the whole brain.. In this sense it is especially frequent that it can generate severe motor symptoms such as agitation, dyskinesia or convulsions.

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

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

Contraindications

The main contraindications are its use with alcoholic beverages and depressants should be avoided. and depressant substances. Neither subjects with epilepsy or with low leukocyte levels and urinary problems, nor with breast Cancer (which it can stimulate).

Also subjects with renal and hepatic failure should be especially cautious with this drug. People with dementia should not take 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 these types of conditions. Children under 12 years of age, pregnant and lactating women should avoid its 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.