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

Fortunately, however, over time we have been able to make progress in understanding what this type of disorder entails and have even generated different strategies and methods to achieve control of its symptoms.

Within these methods we can find the use of psychopharmaceuticals, 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.

Asenapina: 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 psychological disorders.

Asenapine can be found in the form of sublingual tablets, which should be left to dissolve under the tongue unused and without the use of food or water for up to ten minutes. It has a chemical structure derived from myanserin , an antidepressant type of drug, and in this sense it is found in the group of diazepines, oxazepines, thiazepines and oxepines.

Asenapine is one of the second generation or atypical antipsychotics. The development of this type of antipsychotic is due to the fact that the first generation, although effective in the treatment of positive symptoms (those that add something to the subject’s habitual functioning, such as hallucinations, delusions, agitation…), generate side effects that can be dangerous and also have no effect (and sometimes can even potentiate) on negative symptoms (those that imply by themselves a decrease in the capacities and functioning of the subject) such as abulia, apathy or alogia.

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

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

However, compared to olanzapine, it has not proved more effective, although it has not been clearly inferior either. It is also one of the most effective antipsychotics for treating the negative symptoms mentioned above and for improving or maintaining cognition in deteriorating schizophrenia.

Mechanism of action of this substance

The effects of asenapine on our body are based on a mechanism of action based on the antagonism with multiple neurotransmitters, blocking their receptors. In the case of asenapine, its main effect is derived from the blocking of dopamine D2 receptors and serotonin 5-HT2A. It also affects other types of serotoninergic 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 hand it reduces the levels of serotonin at the cortex level and mesocortical pathway, in which there is a deficit of dopamine that generates the negative symptoms. Since serotonin has inhibitory effects on dopamine, inhibiting it causes the 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 it is remarkable the great affinity for serotonin receptors, 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 who 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 the treatment of schizophrenia and other psychotic disorders , in which, as previously mentioned, it stands out for having a positive effect when 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, and this is its most common use. Specifically, is 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.

Side effects and risks

Although asenapine is a useful and effective drug, the truth is that its use, as with the rest of the antipsychotics and other psychopharmaceuticals, can lead to the appearance of different types of side effects, some of which are very dangerous .

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

In addition, it is also possible to generate fainting, dysarthria and tardive dyskinesia, arrhythmias (both tachycardia and bradycardia), hyperglycemia, hypotension , hyperthermia, as well as galactorrhea (release of milk from the breast regardless of sex) or gynecomastia and sexual dysfunction. 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 masticatory movements in the face or other parts of the body), or restlessness or motor agitation.

More serious and dangerous can be rhabdomyolysis, pulmonary embolism, or the extremely 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 bear in mind that there are sectors of the population whose consumption is totally contraindicated or where it must be extremely monitored, because it can have dangerous and even fatal consequences.

Firstly, it should be noted that those who are allergic to asenapine or any of the components of the drug and its presentation should not consume asenapine . In addition, it should be avoided by those with heart, cardiovascular or cerebrovascular problems.

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

Nor should it be mixed with alcohol, antihypertensive medication, fluvoxamine or dopamine agonists. Although there are not enough data, is not recommended in pregnant women since problems have been seen in embryos in the case of animal studies. Nor is it recommended during lactation, given the risk of excretion in breast milk.

Bibliographic references:

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