Asenapine: characteristics, uses and side effects of this drug

Although it is not the most frequent, probably the type of mental health problem that is best known and has been considered as such since ancient times is schizophrenia and other psychotic disorders. This type of affectation usually supposes some type of rupture or split with reality, and generates a high level of suffering for those who suffer from it. It is also the most stigmatized mental disorder.

However, fortunately with the passage of time we have been able to make progress in understanding what it implies this type of disorder and different strategies and methods have even been generated to manage to control their symptoms.

Within these methods we can find the use of psychoactive drugs, among which we can find asenapine. It is about this drug, also used in the treatment of bipolar disorder, that we are going to talk about throughout this article.

• Related article: "Types of psychoactive drugs: uses and side effects"

Asenapine: what is it?

Asenapine is a drug with psychoactive properties, which belongs to the group of antipsychotics or neuroleptics

. It is a type of drug aimed at treating problems of psychotic origin, such as hallucinations and delusions, as well as agitation or states of high nervous activation. However, despite belonging to this group of drugs, asenapine is also indicated for the treatment of other mental disorders.

Asenapine can be found in the form of sublingual tablets, which must be allowed to dissolve under the tongue without using it and without being able to use water or food for up to ten minutes afterwards. It has a chemical structure derived from mianserin., an antidepressant-type drug, and in this sense it is within the group of diazepines, oxazepines, thiazepines and oxepines.

Within the antipsychotics, asenapine is part of the second generation or atypical. The development of this type of antipsychotics is due to the fact that the first generation, although effective in the treatment of positive type symptoms (those that add something to the normal functioning of the subject, such as hallucinations, delusions, agitation...), generate side effects that can be dangerous and also have no effect (and sometimes can even potentiate) on the negative symptoms (those that involve by themselves a decrease in the capacities and functioning of the subject) such as apathy, apathy or hails

All this led to the search to create safer substances, with a more specific effect on the areas in which it is needed and that can generate a higher level of improvement not only in positive symptoms but also in negative ones (although these tend to be more complicated to treat at a pharmacological level): neuroleptics atypical.

Asenapine has some advantages over other similar second-generation ones, such as the fact that it has a lower risk of causing cholinergic alterations and that it usually generates less weight gain, although on the other hand it can generate more extrapyramidal symptoms than, for example, olanzapine. It also presents a lower risk of generating a possible metabolic syndrome.

However, compared with olanzapine, it has not shown greater efficacy, although it has not shown itself to be clearly inferior either. It is also one of the antipsychotics that appears to be more effective in the treatment of negative symptoms, mentioned above, and in improving or maintaining cognition in deteriorating cases of schizophrenia.

• You may be interested in: "Types of antipsychotics (or neuroleptics)"

Mechanism of action of this substance

The effects of asenapine on our body stem from a mechanism of action based on antagonism with multiple neurotransmitters, blocking their receptors. In the case of asenapine, its main effect is derived from the blockade of dopamine D2 receptors and serotonin 5-HT2A receptors. It also affects other types of serotonergic receptors, as well as histamine and some adrenergic receptors (although to a much lesser degree).

Thus, what asenapine does is on the one hand eliminate or reduce the excess of dopamine in the mesolimbic system that generates the positive symptoms, while on the other it reduces serotonin levels at the level of the cortex and mesocortical pathway, in which there is a dopamine deficit that generates negative symptoms. Since serotonin has inhibitory effects on dopamine, inhibiting it causes dopamine levels to rise. these areas remain and even increase in this pathway (in other words, it inhibits a dopamine inhibitor in the Cortex).

Within this mechanism, the great affinity for serotonin receptors is remarkable, in a much higher proportion with respect to dopamine than is usual in other antipsychotics. This also explains the fact that it generates beneficial effects on the cognition of patients with schizophrenia and other ailments that use it and why it is considered one of the best atypical antipsychotics in the treatment of negative symptoms.

Main indications

As an antipsychotic, asenapine is a drug that is indicated for treatment of schizophrenia and other psychotic disorders, in which, as previously mentioned, it stands out for having a positive effect when it comes to combating negative symptoms such as apathy, abulia, poverty of speech and thought or alogia.

However, in addition to this, asenapine is usually indicated for the treatment of manic episodes of bipolar disorder, this being its most common use. Specifically, indicated in adult patients with bipolar disorder type 1, either as monotherapy or in combination with other drugs. It is used both in the treatment of acute phases and in the maintenance and prevention of episodes.

• Related article: "What is schizophrenia? symptoms and treatments"

Side effects and risks

Although asenapine is a useful and effective drug, the truth is that its, like the rest of the antipsychotics and other psychotropic drugs, their consumption can lead to the appearance of different types of effects secondary, some of them very dangerous.

Among the most frequent side effects of asenapine we can find sedation and fatigue (like the rest of antidepressants), weight gain (although it is less than with other neuroleptics), the increase in the sensation of hunger or oral hypoesthesia (loss of sensation in part of the mouth).

In addition to this, it is also possible that fainting, dysarthria and tardive dyskinesia, arrhythmias (both tachycardia and bradycardia), hyperglycemia, hypotension, hyperthermia, as well as galactorrhea (milk emission from the breast regardless of sex) or gynecomastia and sexual dysfunctions. Dysphagia or swallowing problems may also appear, and it can facilitate falls by also generating dizziness and problems such as hypotension. Finally, it should be noted that it can generate extrapyramidal effects, such as tardive dyskinesia. (involuntary chewing movements in the face or other parts of the body), or restlessness or motor agitation.

More serious and more dangerous can be the presence of rhabdomyolysis, pulmonary embolism, or the very dangerous neuroleptic malignant syndrome (which can easily cause death).

Asenapine Contraindications

This drug can be useful for the treatment of certain conditions, but we must bear in mind that there are sectors of the population that have its consumption is totally contraindicated or in which it must be extremely monitored, because it can have dangerous consequences and even deadly.

First of all, it should be noted that they should not take asenapine those people who have an allergy to asenapine or any of the components of the drug and your presentation. In addition to this, it should be avoided by those with heart, cardiovascular or cerebrovascular problems.

Also It is contraindicated in the elderly population with dementia, since it has been seen to increase the risk of mortality. It should also be avoided in the presence of severe liver failure. Likewise, subjects with diabetes (since it can generate hyperglycemics) or with a history of seizures also have it contraindicated.

It should also not be mixed with alcohol, antihypertensive medication, fluvoxamine or dopamine agonists. Although there is not enough data, not recommended in pregnant women since problems have been seen in embryos in the case of animal studies. Neither during lactation, due to the risk of it being excreted in breast milk.

Bibliographic references:

• Valencian Health Agency (2012). Asenapine (Sycrest). Ministry of Health. Valencian generalitat.
• Cruz, N. and Vieta, E. (2011). Asenapine: a new approach to the treatment of mania. Journal of Psychiatry and Mental Health, 4 (2).