Moperone: uses and side effects of this psychotropic drug
This drug, sold under the name Luvatren, is a butyrophenone-type antipsychotic.
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, their use is widespread.
In this article we will talk about moperone, an antipsychotic of the butyrophenone group.. It is a drug of high potency (it has a high affinity with the receptors on which it acts) and low toxicity (very safe).
Moperone: what is it and what is it for?
Moperone is a first generation antipsychotic drug, which is marketed as Luvatren. This drug originates from Japan, belongs to the butyrophenone group and is mainly used to treat schizophrenia as well as other psychotic disorders or disorders with psychotic symptoms.
It is a high potency antipsychotic, i.e. it has a high affinity to bind with its receptor and exert its effect. At the biochemical level and as a mechanism of action, the affinity of moperone is higher for dopamine D2 receptors, which are closely related to schizophrenia.D2 receptors, which are 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.
Its effects
Moperone acts by inhibiting aggression and reducing psychotic symptoms.. At the chemical level it does so through an antagonistic effect on apomorphine, adrenaline and noradrenaline.
Another of its effects is that it increases plasma and adrenal corticosterone concentrations.
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, which is so closely related to psychosis?
Dopamine is a brain neurotransmitter with several locations and functionsIt is found in the nigrostriatal system, in the mesolimbic system, in the mesocortical system and in the tuberoinfundibular system. In the nigrostriatal system it is related to movement, in the mesolimbic system to reinforcement and emotion, in the mesocortical system to executive functions and in the tuberoinfundibular system to prolactin inhibition.
Its receptors, in addition to D2, are also D1 and D5 (postsynaptic receptors). D2, together with D3 and D4, can be both pre- and postsynaptic. D2 receptors are altered in schizophrenia (by excess). These receptors are involved in reinforcement and addictions.
Antipsychotics
Moperone is a type of antipsychotic; antipsychotics generally act by blocking D2 (dopaminergic) receptors.
As for their indications, they are mainly used for psychosis, confusion and delirium, agitation and violent behavior, movement disorders (tics and tic disorder) and other disorders.They are also used for movement disorders (tics, Gilles de Tourette,...), severe OCD (Obsessive-Compulsive Disorder), alcohol withdrawal 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, they improve the positive symptoms of schizophrenia (hallucinations, delusions, disorganized behavior, etc.). Second generation drugs also improve negative symptoms (apathy, abulia, depression...) although to a lesser extent.
Butyrophenones
As we have seen moperone belongs to the butyrophenones, a group of neuroleptic drugs (antipsychotics). (antipsychotics); the best known and most widely used of this group is haloperidol, a classical (first generation) antipsychotic. Droperidol is also, but less so, a classical (first generation) antipsychotic.
Pharmacologically and clinically, butyrophenones are similar to phenothiazines, chemical intermediates in the synthesis of antipsychotic drugs.
As for the effects of butyrophenones, in addition to palliating psychotic symptoms, in some cases they also diminish the choreic symptoms of the psychotic symptoms. also diminish the choreic symptoms characteristic of Huntington's chorea, as well as tics and tachycardia.as well as tics and coprolalia (uttering insults and swear words) characteristic of Gilles de la Tourette syndrome.
Side effects of this drug
The main side effects of moperone are extrapyramidal motor symptoms, thirst and insomnia..
Extrapyramidal motor symptoms (also called SEP, extrapyramidal syndrome), encompass a number 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 (producing sedation and weight gain), the anticholinergic effect (produced by muscarinic blockade) and Cardiovascular effects (produced by alpha1-receptor blockade).
However, although it presents certain side effects, moperone has a low toxicityThis means that high doses of moperone are needed to become intoxicated or cause serious harm, making it a fairly safe substance.
Pregnancy and lactation
Like so many other drugs, moperone requires special use in case of pregnancy and/or breast-feeding..
In pregnancy, extrapyramidal and withdrawal symptoms, respiratory disorders, tremors, somnolence, feeding 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.
As for lactation, moperone passes into breast milk, as do other antipsychotics such as haloperidol. For this reason its use is not recommended in breastfeeding stages.
Bibliographic references:
- Aimoto, T; Kaida, M; Sato, M; Sato, M; Kimura, R; Murata, T. (1980). Effects of neuroleptic butyrophenones on pituitary-adrenal activity in rats. Journal of pharmacobio-dynamics 3(1): 46-52.
- Janicaz, P.G. (1999) Handbook of Psychopharmacotherapy. Philadelphia: Lippincott Williams& Wilkins.
- Stahl, S.M. (2002). Essential psychopharmacology. Neuroscientific bases and clinical applications. Barcelona: Ariel.
- Stolerman, I. (2010). Encyclopedia of Psychopharmacology. (Online-Ausg. edition). Berlin, Heidelberg: Springer-Verlag Berlin Heidelberg, 798.
(Updated at Apr 13 / 2024)