Asenapine: characteristics, uses and side effects of this drug

This antipsychotic-type drug is one of the most effective against symptoms of schizophrenia.

Although it is not the most common, probably the type of mental health problem that is best known and has been considered as such since antiquity is schizophrenia and the other psychotic disorders.. This type of affectation usually involves some kind of rupture or split with reality, and generates a high level of suffering for the sufferer. It is also the most stigmatized mental disorder.

However, fortunately with the passing of time we have been able to advance in the understanding of what this type of disorder implies and even different strategies and methods have been generated to control its symptoms.

Among these methods we can find the use of psychotropic 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 in this article.

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 should be left to melt under the tongue without being used and without being able to use water or food until ten minutes later. It has a chemical structure derived from mianserin, an Antidepressant drug.It is an antidepressant drug, and in this sense it belongs to the group of diazepines, oxazepines, thiazepines and oxepines.

Among the antipsychotics, asenapine is one of the second generation or atypical antipsychotics. The development of this type of antipsychotic is due to the fact that first generation antipsychotics, although effective in the treatment of positive symptomatology (those that add something to the subject's usual functioning, such as hallucinations, delusions, agitation, etc.), generate side effects that may have side effects that can be very serious, generate side effects that can become dangerous and in addition they have no effect (and sometimes can even enhance) on negative symptoms (those which in themselves imply a decrease in the subject's capacities and functioning) such as abulia, apathy or alogia.

All this led to the search for safer substances, with a more specific effect on the areas in which they are needed and which can generate a higher level of improvement not only in positive symptoms but also in negative symptoms (although these are usually more complicated to treat pharmacologically): atypical neuroleptics.

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

However, in comparison with olanzapine it has not shown greater efficacy, although it has not been shown to be clearly inferior. It is also one of the antipsychotics that appears to be most effective in the treatment of the aforementioned negative symptoms and in the improvement or maintenance of cognition in cases of schizophrenia that show deterioration.

Mechanism of action of this substance

The effects of asenapine on our organism are based on a mechanism of action based on antagonism with multiple neurotransmitters, blocking their receptors. In the case of asenapine, its main effect derives from the blockade of dopamine D2 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 which generates the positive symptomatologyOn the other hand, it reduces serotonin levels in the cortex and mesocortical pathway, where there is a deficit of dopamine that generates the negative symptoms. Since serotonin has inhibitory effects on dopamine, inhibiting it causes dopamine levels in these areas to remain and even increase in this pathway (in other words, it inhibits a dopamine inhibitor in the cortex).

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

Main indications

As an antipsychotic, asenapine is a drug that is indicated for the treatment of schizophrenia and other psychotic disorders, in which, as mentioned above, asenapine is a drug indicated for the treatment of schizophrenia.As mentioned above, asenapine has a positive effect on negative symptoms such as apathy, abulia, poor speech and thinking 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, it is indicated in adult patients with bipolar disorder type 1either 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.

Side effects and risks

Although asenapine is a useful and effective drug, the truth is that, as with other antipsychotics and other psychotropic drugs, its use can lead to the appearance of different types of side effects, some of them of great danger.

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

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

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

Contraindications of asenapine

This drug can be useful for the treatment of certain conditions, but we must take into account that there are sectors of the population whose consumption is totally contraindicated or whose consumption must be extremely supervised, since it can have dangerous and even fatal consequences.

First of all, it should be noted that asenapine should not be taken by people who are allergic to asenapine or to any of the components of the drug and its presentation should not take asenapine. and its presentation. It should also be avoided by people with heart, cardiovascular or cerebrovascular problems.

Also It is also contraindicated in the elderly population with dementiasIt is also contraindicated in elderly people with dementia, since it has been shown to increase the risk of mortality. It should also be avoided in the presence of severe hepatic insufficiency. Likewise, subjects with diabetes (since it can generate hyperglycemia) or with a history of convulsions are also contraindicated.

It should not be mixed with alcohol, antihypertensive medication, fluvoxamine or dopaminergic agonists. Although there are not enough data, it is 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 excretion in breast milk.

Bibliographic references:

• Valencian Health Agency (2012). Asenapine (Sycrest). Consellería de Sanitat. Generalitat Valenciana.
• Cruz, N. and Vieta, E. (2011). Asenapine: a new approach for the treatment of mania. Journal of Psychiatry and Mental Health, 4 (2).