Pimavanserin (antipsychotic): Indications, Uses And Side Effects

Pimavanserin

Psychotic symptoms do not only appear in psychotic disorders such as schizophrenia or delusional disorder. They also frequently appear in some dementias, such as Parkinson’s dementia and Alzheimer’s dementia.

Pimavanserin is a third-generation antipsychotic that was approved in 2016 for the treatment of psychoses in Parkinson’s Other effects that it may have are still being investigated to treat symptoms such as agitation and depression in Alzheimer’s, for example.

In this article we will learn about its characteristics, mechanism of action, uses and adverse effects, as well as the results of clinical trials carried out with this recently released drug.

Pimavanserin: what is it and what is it effective for?

Pimavanserin is a recent antipsychotic, specifically an atypical antipsychotic, and considered third generation It is marketed under the name Nuplazid, and is synthesized by Acadia Pharmaceuticals laboratories.

This is a drug that has recently been discovered that can relieve psychotic symptoms in people with Alzheimer’s disease without causing the common side effects of other antipsychotics, such as risks of relapse, stroke or death.

However, at the moment its use has only been approved to treat psychoses that appear in patients with Parkinson’s dementia.

For its part, Parkinson’s disease is a pathology that can end up developing dementia (and this happens in many cases); We usually know this by its motor symptoms (tremors, rigidity…), but in many cases of Parkinson’s patients, notable psychotic symptoms also appear, such as delusions and/or hallucinations.

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Applied studies

This effect of Pimavanserin to treat psychotic symptoms in patients with Alzheimer’s has been demonstrated in a study In addition, another study (a clinical trial) conducted with pimavanserin showed how this drug was also effective in relieving psychotic symptoms in people with dementia caused by Parkinson’s disease.

FDA approval

This last finding allowed the FDA (United States government agency responsible for regulating medications and other products) to approve pimavanserin for this indication in April 2016.

It should be noted that the authorization of pimavanserin was based on the results of a single placebo-controlled trial, which lasted 6 weeks and in which 199 patients with Parkinson’s disease participated, all of them with symptoms of hallucinations and/or delusions ( psychotic symptoms).

Another relevant fact is that the patients who participated in the clinical trial with pimavanserin did not worsen their primary motor symptoms.

Innovative therapy

Pimavanserin Named “Breakthrough Therapy” by FDA ; Thus, its approval as a treatment for psychoses in patients with Parkinson’s dementia was logical.

The “breakthrough therapy” designation granted by the FDA is awarded to those drugs that, according to preliminary clinical evidence, can significantly improve the symptoms of patients with serious diseases.

Mechanism of action

On the other hand, Pimavanserin has a different mechanism of action than is usual in classic antipsychotics; What it does is block a specific serotonergic nerve receptor, called THT2A or 5HT2A.

This receptor has been related to memory processes, cognitive functions and other organic functions; It is believed to play a mediating role in them.

Characteristics

As we have seen, pimavanserin is an atypical antipsychotic that is approved as an indication to treat psychotic symptoms associated with Parkinson’s dementia (it is marketed under the name “Nuplazid”).

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Besides, A recent study has also found that pimavanserin can relieve psychosis in patients with another type of dementia, Alzheimer’s dementia, although research continues and conclusive statements or definitive conclusions cannot yet be established. Specifically, what pimavanserin would do is reduce the frequency and intensity of psychotic symptoms in dementia (generally, hallucinations and delusions).

Thus, pimavanserin is currently under development (under investigation) in relation to the possibility of treating possible cases of psychosis, schizophrenia, agitation and major depressive disorder in patients with dementia due to Alzheimer’s disease.

Format and take

Pimavanserin is taken orally, in “tablet” format. Generally its administration schedule is once a day; It can be taken with or without food. It is recommended that it be taken at the same time each day, as with other drugs.

Different from previous antipsychotics

As we already mentioned, the mechanism of action of pimavanserin is different from the usual mechanism of antipsychotics, which block the dopaminergic D2 receptors in the brain (being dopaminergic antagonists).

In the case of pimavanserin, it is an inverse agonist and antagonist of the serotonergic 5-HT2A receptors; It has a high binding affinity with them (fits almost perfectly).

Pimavanserin is a well-tolerated and fairly safe antipsychotic as demonstrated by various clinical trials, carried out prior to its commercialization.

Adverse effects

Regarding the adverse effects (AEs) of pimavanserin, The clinical trials mentioned showed how these were similar to those of the placebo condition Specifically, they were: a confusional state and peripheral edema. These adverse effects were found in at least 5% of patients in the trials.

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An important warning regarding the use of pimavanserin, which is worth knowing, is that, like any antipsychotic, it can increase mortality in older patients (elderly) with psychotic symptoms related to their dementia. These are the adverse effects that appeared in clinical trials, but others are also associated, such as: nausea and swelling (in hands, feet or ankles). As for the serious adverse effects of pimavanserin, they include: hallucinations, rashes, difficulty walking, confusion, hives, tightness in the throat, shortness of breath, and swelling of the tongue.

It is important to go to an emergency doctor if you experience any of the last mentioned adverse effects.

Conclusions

Pimavanserin is a relatively recent drug, with antipsychotic actions and that has been shown to be effective in Parkinson’s dementia, to treat the associated psychosis. However, We must be cautious, since although it is already marketed, pimavanserin is still under investigation

On the other hand, although the symptoms that we know most about in patients with Parkinson’s are motor symptoms (and cognitive symptoms in the case of Alzheimer’s), psychotic symptoms also appear in these pathologies, and with relative frequency. In addition, they cause notable discomfort in these patients and the people around them.

These are symptoms that significantly interfere with the daily functioning of these patients. This is why pimavanserin can be a hopeful drug that helps improve the quality of life of these people, reducing their emotional deterioration and improving their psychological well-being.