Paliperidone palmitate: uses and side effects

This drug for psychotic disorders is administered as an injection.

Psychotic disorders are some of the best known and most striking to most of the population, with schizophrenia being the best known disorder of this type. Research on these problems has generated different pharmacological treatments to reduce and keep under control the symptomatology of those who suffer from it. One of these drugs, which is relatively recent, is paliperidone..

However, despite the usefulness of antipsychotics, not all patients are able or willing to take oral medication, or find it cumbersome to take it every few days. For this reason, depot presentations have been devised, an example of this being paliperidone palmitate.

Paliperidone and paliperidone palmitate: drug type

Paliperidone palmitate is a type of paliperidone presentation, an atypical or second-generation antipsychotic, which is which in turn is the active metabolite of another antipsychotic, risperidone. Paliperidone is a relatively new drug that is highly effective in the treatment of psychotic symptoms such as schizophrenia and schizoaffective disorder, reducing the likelihood of symptoms such as hallucinations, aggression or disorganized behavior.

As for paliperidone palmitate itself, it is a medication that is administered intramuscularly, intramuscularly, intramuscularly, intramuscularly and intramuscularly. is administered intramuscularly, by means of an injection.. In this type of presentation or administration of the drug, a crystallized form of , is injected into the muscle and slowly released into the blood over time without the subject having to take any pills (this is an extended release depot presentation). This is especially useful for those subjects with memory problems, who find it difficult to take pills or who are reluctant to take medication.

Generally a monthly or even quarterly injection is performed (although this may vary according to the medical center and the patient's symptoms), which should be carried out by a physician or competent health care professional.. In any case, if an oral administration is required, paliperidone can also be used.

Mechanism of action

Once injected, paliperidone palmitate will gradually hydrolyze and transform into paliperidone in the body as the drug is released into the bloodstream. in the body as the drug is released into the bloodstream.

Paliperidone and paliperidone palmitate are drugs classified as atypical antipsychotics. Their therapeutic action is due to their effects in blocking dopamine D2 and serotonin 5-HT2 receptors.

The antidopaminergic action at the mesolimbic level reduces hallucinations and maintains the levels of this hormone so that they do not occur, while the effect on serotonin makes it difficult for the reduction of dopamine to greatly affect other brain areas such as the cortex. It also has a mild antagonistic effect on alpha-adrenergic receptors and on histaminergic receptors, which generates some of the possible side effects of the drug.

Uses in the treatment of disorders

The main indication for paliperidone palmitate is the treatment of symptoms of psychotic disorders. is the treatment of symptoms of psychotic disorders, specifically schizophrenia.specifically schizophrenia. However, unlike other antipsychotics, paliperidone palmitate is not generally used as a treatment for acute psychotic episodes, but as a maintenance psychotropic drug.

In other words, for the treatment of an acute psychotic break, the patient would first be stabilized with other drugs (e.g. paliperidone) and then paliperidone palmitate would be used to keep the symptoms under control and to prevent new outbreaks from occurring.

The exception is found in those cases that even without being stabilized have already shown a positive response to paliperidone or risperidone and the psychotic symptomatology is mild or moderate. This drug has been approved by the FDA for the treatment of schizophrenia from the age of twelve years and older..

In addition to schizophrenia, paliperidone palmitate has been found to be effective in schizoaffective disorder or other problems, being possible its use as coadjuvant treatment of antidepressant medication (although it has to be something prescribed by the doctor, since it depends on which medication can interact in a dangerous way for the health).

Side effects and contraindications.

Although paliperidone palmitate is a useful and effective formulation in the maintenance treatment of schizophrenia and has many advantages, it can generate more or less undesirable side effects and may even be contraindicated in some people.

Some side effects that can appear after its administration are the presence of drowsiness, difficulty urinating and brownish or dark colored urine, headaches, chills, increased hunger and thirst, weight gain, cold symptoms, visual disturbances, tremorsheadaches, chills, increased hunger and thirst, weight gain, cold symptoms, visual disturbances, tremors, allergic reactions or inflammations in the area where the injection was made. Other more serious symptoms may be the presence of arrhythmias or tachycardia, hyperglycemia, convulsions or hypotension.

Although as an atypical antipsychotic its effect on serotonin reduces the effects on dopamine of the cortex and the tuberoinfundibular dopaminergic pathway, it has been observed that its administration can generate alterations and difficulties in sexuality related to the increase of prolactin, such as a decrease in libido or priapism in men.

As we have mentioned some people have contraindications for this drugThey should not be treated with it or have to evaluate with the doctor the suitability or not of doing so. Among them we can find patients with heart or cardiovascular, renal, stomach or liver problems.

Neither people with diabetes mellitus (since it can generate alterations in blood sugar levels), subjects with dementia (it increases the risk of death during treatment), pregnant women and nursing mothers. Likewise, it should not be mixed with other drugs since it can generate interactions between drugs such as lithium salts, levodopa, alcohol, Antibiotics and other psychopharmaceuticals.antibiotics and other psychotropic drugs.

Bibliographic references:

• Nussbaum, A.M. & Stroup, T.S. (2012). Paliperidone palmitate for schizophrenia. Cochrane Database of Systematic Reviews, 6. Art. No.: CD008296. DOI: 10.1002/14651858.CD008296.pub2.