Moperone: Uses And Side Effects Of This Psychotropic Drug
Antipsychotics are drugs used to treat psychosis, delirium, Obsessive-Compulsive Disorder (severe), agitation and violent behavior, among others. In psychiatry, mental health and primary care, its use is widespread.
In this article We will talk about moperone, an antipsychotic from the butyrophenone group It is a drug of high potency (it has great affinity with the receptors on which it acts) and low toxicity (very safe).
Moperone is a first-generation antipsychotic drug, marketed as Luvatren This drug originates from Japan, belongs to the group of butyrophenones and is mainly used to treat schizophrenia, as well as other psychotic disorders or with psychotic symptoms.
It is a high-potency antipsychotic, that is, it has a great affinity to bind with its receptor and exert its effect. At a biochemical level and as a mechanism of action, Moperone’s affinity is greater for dopamine D2 receptors, closely related to schizophrenia (where there is an excess of this substance). It also has affinity for serotonin 5-HT2 receptors, although to a lesser degree, and for sigma receptors.
Their efects
The Moperone acts by inhibiting aggression and reducing psychotic symptoms At a chemical level it does so through an antagonistic effect on apomorphine, adrenaline and norepinephrine.
Another of its effects is that it increases plasma and adrenal concentrations of adrenal corticosterone.
Dopamine and its presence in the brain
As we have seen, moperone acts, among others, on dopamine D2 receptors. But… what else do we know about this substance, dopamine, so related to psychosis?
Dopamine is a brain neurotransmitter that has various locations and functions: It is found in the nigrostriatal system, in the mesolimbic system, in the mesocortical system and in the tuberoinfundibular system. In the nigrostriatum it is related to movement, in the mesolimbic, with reinforcement and emotion, in the mesocortical with executive functions and in the tuberoinfundibular with the inhibition of prolactin.
Its receptors, in addition to being D2, are also D1 and D5 (postsynaptic receptors). D2, along with D3 and D4, can be both pre- and postsynaptic. D2 receptors are altered in schizophrenia (due to excess). These receptors are involved in reinforcement and addictions.
antipsychotics
Moperone is a type of antipsychotic; Antipsychotics generally act by blocking D2 (dopaminergic) receptors.
Regarding your instructions, They are mainly used for psychoses, confusion and delirium, agitation and violent behavior movement disorders (tics, Gilles de Tourette,…), severe OCD (Obsessive-Compulsive Disorder), alcohol deprivation and chronic pain.
In addition to these indications, second-generation (atypical) antipsychotics are also used for bipolar disorder, borderline personality disorder, and autism.
On the other hand, improve the positive symptoms of schizophrenia (hallucinations, delusions, disorganized behavior,…). The second generation also improves negative symptoms (apathy, apathy, depression…) although to a lesser extent.
Butyrophenones
As we have seen, Moperone belongs to the butyrophenones, a group of neuroleptic drugs (antipsychotics); The best known and most used of this group is haloperidol, a classic (first generation) antipsychotic. It is also, although not as much, droperidol.
Pharmacologically and clinically, butyrophenones are similar to phenothiazines, chemical intermediates in the synthesis of antipsychotic drugs.
Regarding the effects of butyrophenones, in addition to alleviating psychotic symptoms, in some cases They also reduce the choreic symptoms of Huntington’s chorea as well as the tics and coprolalia (uttering insults and swear words) typical of Gilles de la Tourette syndrome.
The main side effects of moperone are extrapyramidal motor symptoms, thirst and insomnia
Extrapyramidal motor symptoms (also called EPS, extrapyramidal syndrome) encompass a series of symptoms such as tardive dyskinesia, akathisia, dystonia and parkinsonism. These motor symptoms are common side effects of antipsychotics such as moperone, along with others such as the antihistamine effect (which produces sedation and weight gain), the anticholinergic effect (produced by a muscarinic blockade) and cardiovascular effects (produced by the blockade of the alpha1 receptor).
However, although it has certain side effects, moperone has low toxicity ; This means that high doses of it are needed to become intoxicated or cause serious damage, which makes it a fairly safe substance.
Pregnancy and lactation
Like many other drugs, moperone requires special use if you are pregnant and/or breastfeeding
In pregnancy, extrapyramidal and withdrawal symptoms, respiratory disorders, tremors, drowsiness, eating disorders, as well as irritability and hypotonia have been detected in neonates whose mothers took antipsychotics (such as moperone) at the end of their pregnancy.
Regarding breastfeeding, moperone passes into breast milk, like other antipsychotics such as haloperidol. It is because of that Its use is not recommended in lactating stages
