Asenapine: Characteristics, Uses And Side Effects Of This Drug
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 ancient times is schizophrenia and other psychotic disorders This type of affectation usually involves 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 this type of disorder entails and different strategies and methods have even been generated to control its symptoms.
Within 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 throughout this article.
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 conditions.
Asenapine can be found in the form of sublingual tablets, which must be left to dissolve under the tongue without using it and without being able to use water or food for up to ten minutes. It has a chemical structure derived from mianserin an antidepressant type drug, and in this sense it is within the group of diazepines, oxazepines, tiazepines and oxepins.
Among antipsychotics, asenapine is part of the second generation or atypical antipsychotics. The development of this type of antipsychotics 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 usual functioning, such as hallucinations, delusions, agitation…), generate side effects that can be dangerous and furthermore they have no effect (and sometimes can even enhance) on negative symptoms (those that in themselves imply a decrease in the subject’s abilities and functioning) such as avolition, apathy or alogia.
All of this led to a search for creating safer substances, with a more specific effect on the areas in which it is needed and that can generate a greater level of improvement not only in the positive symptoms but also in the negative ones (although these tend to be more complicated). to treat at a pharmacological level): atypical neuroleptics.
Asenapine has some advantages over other similar second generation drugs, such as the fact that has a lower risk of causing cholinergic type 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 to olanzapine, it has not demonstrated greater efficacy, although it has not been clearly inferior either. It is also one of the antipsychotics that appears to be most effective in treating the negative symptoms mentioned above, and in improving or maintaining cognition in cases of schizophrenia that present deterioration.
Mechanism of action of this substance
The effects of asenapine on our body 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).
In this way, what asenapine does is on the one hand eliminate or reduce excess dopamine in the mesolimbic system that generates positive symptoms, while on the other hand 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 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 great affinity for serotonin receptors is notable, 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 mentioned above, 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, It 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, as with the rest of antipsychotics and other psychotropic drugs, its consumption can lead to the appearance of different types of side effects, 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), increased feelings of hunger or oral hypoesthesia (loss of sensitivity 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 (emission of milk 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-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 cause death).
Contraindications of asenapine
This drug can be useful for the treatment of certain conditions, but we must keep in mind that there are sectors of the population whose consumption is totally contraindicated or in which it must be extremely monitored, because it can have dangerous and even fatal consequences.
First of all, it should be noted that they should not consume asenapine those people who have an allergy to asenapine or any of the components of the drug and its presentation. In addition, it should be avoided by those people 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 cause hyperglycemia) 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 for pregnant women since problems have been seen in embryos in animal studies. Nor during breastfeeding, due to the risk of it being excreted in breast milk.
