Paliperidone Palmitate: Uses and Side Effects

Psychotic disorders are some of the best known and striking for 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 control the symptoms of those who suffer from it. One of these drugs, relatively recent, is paliperidone.

However, despite the usefulness of antipsychotics, not all patients can or want to take medication orally, or they find it cumbersome to take it every so often. For this reason, depot presentations have been devised, being an example of this paliperidone palmitate.

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Paliperidone and paliperidone palmitate: type of drug

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

As regards paliperidone palmitate itself, we are dealing with a medication that given intramuscularly, by injection. In this type of presentation or administration of the drug, a crystallized form of is injected into the muscle, which will be released slowly. in the blood over time without the subject having to take any pills (this is a release depot presentation prolonged). This is especially useful for those subjects with memory problems, who find it difficult to schedule taking pills or who are reluctant to take medication.

A monthly or even quarterly injection is usually done (although this can vary depending on the medical center and the patient's symptoms), which must be carried out by a doctor or competent health professional. In any case, if you want an oral administration, you can also resort to paliperidone.

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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.

Paliperidone and paliperidone palmitate are drugs classified as atypical antipsychotics. Its therapeutic action occurs due to its effects when it comes to blocking the D2 receptors of dopamine and the 5-HT2 of serotonin.

Antidopaminergic action at the mesolimbic level reduces hallucinations and maintains the levels of this hormone so that they do not occur, along with the effect on the 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 histaminergic receptors, leading to some of the possible side effects of the drug.

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Uses in treatments against disorders

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

That is, for the treatment of an acute psychotic episode, the patient would first be stabilized with other drugs (for example, paliperidone) and later the use of paliperidone palmitate was considered to keep the symptoms under control and prevent them from appearing new shoots.

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

In addition to schizophrenia, paliperidone palmitate has been shown to be effective in schizoaffective disorder or other problems, being possible its use as an adjuvant treatment of antidepressant medication (Although it must be prescribed by the doctor, since it depends on which medication can interact in a way that is dangerous to health).

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Side effects and contraindications

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

Some side effects that may 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, tremors, allergic reactions or inflammations in the area where the injection. Other more serious symptoms may be the presence of arrhythmias or tachycardia, hyperglycemia, seizures or hypotension.

Although as an atypical antipsychotic its effect on serotonin reduces the effects on dopamine in 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 in prolactin, such as a decrease in libido or priapism in children. men.

as we have mentioned some people have contraindicated this drug, not having to be treated with it or having to assess with the doctor the suitability or not of doing so. Among them we can find patients with heart or cardiovascular, kidney, stomach or liver problems.

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