Psychotic disorders are some of the best known and most striking for the majority of the population, with schizophrenia being the best known disorder of this type. Research into these problems has generated different pharmacological treatments to reduce and keep the symptoms of those who suffer from it under control. 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 find it cumbersome to take it every so often. That is why depot presentations have been devised, being an example of this. paliperidone palmitate
Paliperidone and paliperidone palmitate: type of drug
Paliperidone palmitate is a type of presentation 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 the treatment of psychotic symptoms such as those of schizophrenia and schizoaffective disorder, reducing the likelihood of presenting symptoms such as hallucinations, aggression or disorganized behavior.
Regarding paliperidone palmitate itself, we are dealing with a medication that It is administered intramuscularly, by injection In this type of presentation or administration of the drug, a crystallized form of , which will be slowly released into the blood over time, is injected into the muscle without the subject having to take any pill (it is a prolonged release depot presentation ). This is especially useful for those subjects with memory problems, who find it difficult to schedule pills or who are reluctant to take medication.
Typically a monthly or even quarterly injection is performed (although this may vary depending on the medical facility and the patient’s symptoms), which must be carried out by a doctor or competent healthcare professional In any case, if you want oral administration you can also use paliperidone.
Mechanism of action
Once injected, Paliperidone palmitate will be hydrolyzed and gradually transformed 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 in blocking dopamine D2 and serotonin 5-HT2 receptors.
Antidopaminergic action at the mesolimbic level reduces hallucinations and maintains the levels of this hormone so that they are not produced, at the same time that 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 and histaminergic receptors, which generates some of the possible side effects of the drug.
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 generally used as a treatment for acute psychotic breaks, but rather as a maintenance psychotropic drug.
That is, to treat an acute psychotic outbreak, the patient would first be stabilized with other drugs (for example, paliperidone) and then paliperidone palmitate would be considered to keep the symptoms under control and prevent new outbreaks from appearing.
The exception is found in those cases that, even without being stabilized, have already expressed a positive response to paliperidone or risperidone and the psychotic symptoms are 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 found to be effective in schizoaffective disorder or other problems, Its use as an adjuvant treatment for antidepressant medication is possible (although it must be something prescribed by the doctor, since it depends on which medication can interact in a way that is dangerous to health).
Side effects and contraindications
Although paliperidone palmitate is a useful and effective formulation in the maintenance treatment of schizophrenia and has multiple advantages, it can generate more or less undesirable side effects and may even be contraindicated in some people.
Some side effects that may appear after administration are the presence of drowsiness, difficulty urinating, and brownish or dark urine, headaches, chills, increased hunger and thirst, weight gain, cold symptoms, visual disturbances, tremors, allergic reactions or inflammation in the area where the injection was performed. Other more serious ones may be the presence of arrhythmias or tachycardias, 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 men.
As we have mentioned some people have this drug contraindicated, not having to be treated with it or having to assess with the doctor the suitability or otherwise of doing so. Among them we can find patients with heart or cardiovascular, kidney, stomach or liver problems.
Nor are people with diabetes mellitus (since it can cause alterations in blood sugar levels), subjects with dementia (the risk of death during treatment increases), pregnant women and nursing mothers. Likewise, it should not be mixed with other medications since can generate interactions between drugs such as lithium salts, levodopa, alcohol antibiotics and other psychotropic drugs.
