Amisulpride: uses and side effects of this antipsychotic drug
Schizophrenia and other psychotic disorders are some of the most severe and disruptive mental health problems. Hallucinations, delusions, catatonia, erratic and disorganized behavior, flight of ideas or altered speech are some of the symptoms that can appear, and they imply a split or partial break with reality.
But fortunately, over time and from various branches of science, different methodologies have been generated to reduce the symptoms and maintain the stability of those who suffer from it, so that they can maintain a normative life. Among them is the use of antipsychotic drugs, a fundamental pillar of the treatment of this condition. And one of the many that exist is amisulpride , which we will discuss throughout this article.
Amisulpride: a powerful antipsychotic
Amisulpride is an antipsychotic drug, i.e. a medicine or substance with psychoactive properties whose effects help to combat psychotic symptoms, especially with regard to problems such as hallucinations and delusions.
It is an antipsychotic derived from the atypical or second generation neuroleptics , which were developed with the purpose of combating the previously mentioned symptoms without the frequent side effects that the first generation ones have.
In addition, one of the main advantages of the second generation is that they achieve a therapeutic effect on negative symptoms (those that involve a mental impoverishment of the patient and a loss of functionality, such as abulia and apathy, alogia or impoverishment of language), something in which the first generation neuroleptics fail or do not have much effect (in some cases they even get worse).
This medicine is marketed in tablet form , and its main route of administration is oral. With a half-life of 12 hours, it is partially metabolised and excreted through urine and faeces. Its high potency makes it comparable to highly recognized typical antischotics such as haloperidol, although it is much safer and generates less discomfort and side effects than the latter. It has also been compared with other drugs such as risperidone, a comparison in which amisulpride has a slight superiority in terms of efficacy.
Mechanism of action
The mechanism of action of amisulpride is based on its effect on our brain chemistry, specifically on the dopaminergic system. Despite the fact that it is an atypical or second generation drug, which generally implies that in addition to dopamine it also has an effect on the serotonin system , amisulpride is an exception: it only has a relevant effect on dopamine receptors.
Specifically, amisulpride is a dopamine D2 and D3 receptor antagonist . At doses less than 300 mg, its effect is on the receptors of presynaptic neurons, which has the effect of increasing dopamine levels by inhibiting their reuptake. This aspect is fundamental for treating negative symptoms, given that it is linked to a dopaminergic deficit in the mesocortical pathway.
On the other hand, if the doses are greater or equal to 400 mg, the antagonistic effects occur on the post-synaptic neurons, which implies that the dopamine will not be used by these neurons and will be degraded, with the dopamine having less effect and its levels decreasing over time. This is very useful to combat positive symptomatology , linked to an excess of dopamine in the mesolimbic pathway.
Amisulpride, as an antipsychotic or neuroleptic, has as its main therapeutic indication schizophrenia. In this sense, amisulpride is useful both in the treatment of psychotic outbreaks and acute states and in more chronic phases , as well as in the prevention of new outbreaks.
In addition, it should be noted that this drug is effective in both positive and negative symptoms, with great efficacy in both. Although it is not an official indication, it has also been used on occasion in cases of depression and dysthymia.
Although amisulpride is a very useful drug, its administration can generate a number of uncomfortable or even dangerous side effects (even though such effects tend to occur on a smaller scale and less frequently than typical ones).
Some of the most common are the existence or appearance of tremors, hypotension, reduced libido and difficulties in reaching orgasm, increased prolactin in the blood which can lead to sexual alterations (menstrual problems, erectile dysfunction or galactorrhea, or release of milk from the breasts, among others). At the gastric level, they can generate constipation, nausea and vomiting. Although to a lesser extent than other neuroleptics, it can also cause some drowsiness and slight weight gain. Other frequent side effects are dystonia or dyskinesia, anxiety and irritability.
Others with greater danger can be possible hyperglycemia, heart alterations and arrhythmias, convulsions , agranulocytosis (reduction of granulocytes, a type of white blood cell), leukopenia (the number of leukocytes is reduced), hypercholesterolemia or hyponatremia. It can also occur for cardiac, venous thromboembolism, angioedema or even the life-threatening neuroleptic malignant syndrome. It can also contribute to the growth of various types of tumors.
The use of amisulpride is contraindicated for all those who are allergic to this drug or any of its components. It should also be avoided by people who suffer or have suffered from tumors such as breast, pituitary or adrenal gland. Those who have or have had epilepsy should avoid using it.
It should also not be taken by people with heart or cardiovascular problems, kidney problems or failure (at least the dose should be reduced and controlled), Parkinson’s (the drug can impair Parkinsonian symptoms) or other dementias (the risk of stroke is tripled and the risk of death from infectious causes is increased). Special caution should also be taken by diabetic patients, as the drug can cause hypotension or high blood pressure. In this sense, those with cardiovascular problems should also avoid it or consult their suitability to control the doses.
It should be avoided with alcohol, lithium salts, antacids, antidepressants, antihypertensives, antiarrhythmics, antipsychotics, or levodopa, among others. Those who suffer from blood or endocrine problems should monitor and control their condition, given the risk of alterations in white blood cells and blood composition.
Pregnant and lactating women are also contraindicated to this drug , since although there are not enough data on this subject, exposure to antipsychotics during pregnancy can generate alterations in the babies, or even neonatal abstinence syndrome.
- Spanish Agency for Medicines and Healthcare Products (2015). Leaflet: information for the patient: Amisulprida Zentiva 200 mg EFG tablets. Available at: https://cima.aemps.es/cima/pdfs/es/p/63998/Prospecto_63998.html.pdf
- Carretero, M. (2004). Amisulprida. Offarm, 23 (3): 11-178.
- Mota Nota, J.S., Silva de Lima, M., Soares, B., Silveira de Mota Neto, J.I. (2002). Amisulpride for schizophrenia. Cochrane Database of Systematic Reviews. Available at: https://www.cochrane.org/es/CD001357/amisulprida-para-la-esquizofrenia