Perphenazine: Uses And Side Effects Of This Antipsychotic

Perphenazine

One of the best-known types of mental disorder is psychotic disorders. This type of disorder, considered a serious mental disorder, generates a high level of suffering for those who suffer from it and those around them.

The typical symptoms of this type of disorder, among which schizophrenia and schizoaffective disorder stand out, can be very disabling and greatly alter the quality of life of those who suffer from it if they do not receive treatment. In addition to that, It is one of the types of mental disorder with the highest level of social stigmatization something that makes the situation even more difficult for those who suffer from it.

Fortunately, there are different treatments that facilitate management and maintain the stability of patients, among them pharmacological treatment standing out. It is possible to find a wide variety of antipsychotic or neuroleptic drugs. One of them is perphenazine which we are going to talk about in this article.

Perphenazine: a typical antipsychotic

Perphenazine is one of several drugs that are part of the group of antipsychotics or neuroleptics. It is a psychoactive substance highly effective in the treatment of psychotic symptoms which acts by reducing the level of activity of certain neurotransmitters.

It is considered a medium-potency antipsychotic, being much more powerful (it is estimated that up to five times more) than chlorpromazine and being especially effective in the treatment of positive symptoms (that is, those that are added to the patients’ usual functioning such as hallucinations and delusions, disorganized behavior or agitation).

Among antipsychotics, Perphenazine is classified as one of the typical or classic antipsychotics which, although they are very useful in the treatment of the aforementioned symptoms, do not have a great effect on negative symptoms (symptoms that reduce the functionality and capabilities of the subject, such as apathy or poverty of thought), and could even lead to cause aggravation).

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In addition, they can lead to the appearance of considerably annoying and disabling secondary symptoms, these two factors being elements that led to continued research towards a more favorable mechanism of action that would lead to the generation of atypical or second-generation antipsychotics.

This does not mean that perphenazine and other typical antipsychotics are not used in clinical practice, but It is not usually the first therapeutic option and is usually used when other drugs are not effective.

Mechanism of action

Like most antipsychotics, the main mechanism of action of perphenazine is through its action on brain dopamine. Specifically, perphenazine works by blocking dopamine D2 receptors in the brain.

And it has been observed that patients with schizophrenia or other psychotic disorders usually have an excess of dopamine in the mesolimbic pathway, an excess that has been seen to be related to positive symptoms. In this way, perphenazine blocks the dopamine receptors of this pathway at the postsynaptic level, making its activity in this region less and reducing agitation and positive symptoms.

However, the action of perphenazine is not selective: blockade of D2 receptors occurs not only in the mesolimbic pathway but also in other areas whose dopamine levels were not altered, or even in areas where some people have a deficiency of this substance.

Specifically, negative symptoms (avolition, apathy, etc.) have been linked to a deficiency of this substance in the mesocortical pathway, in such a way that the action of perphenazine would not help to solve this type of symptoms or could even aggravate them. This means that different side effects may appear depending on the pathway that suffers an unnecessary decrease in dopamine levels, something that can alter aspects as diverse as motor skills, sexuality or systems as diverse as motor, sexual or sleep.

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In addition to the above, perphenazine also interacts with norepinephrine, histamine, serotonin and acetylcholine.

Main indications

The main indication for perphenazine, as an antipsychotic, is schizophrenia treatment In this sense, it is especially effective in the treatment of positive symptoms such as the aforementioned hallucinations and delusions. It is especially useful in patients with a high level of agitation (since it has sedative effects) and aggression. Also in catatonic patients.

In addition, in some cases perphenazine is used as an antiemetic, allowing the control of vomiting and nausea in patients with serious problems and constant and dangerous vomiting. In some cases it can also be used in the treatment of manic episodes.

Side effects

Perphenazine is an effective and very useful drug, but Like other drugs, it has a large number of possible side effects of great relevance. And as we have said previously, perphenazine can cause different annoying side effects in different nervous pathways, which in turn can alter various body systems.

Some of the different secondary symptoms that can occur are drowsiness, the appearance of headaches, dizziness and blurred vision, dryness or excess salivation, the appearance of parkinsonian symptoms such as tremors, spasms and involuntary movements such as those of tardive dyskinesia. Weight gain, loss of appetite, diarrhea or constipation may also occur. Other possible symptoms are the appearance of arterial hypotension, hyperglycemia, loss of libido and the appearance of galactorrhea (regardless of sex) and gynecomastia.

Sleep problems, despite the existence of drowsiness, are also possible, as are urinary problems (due to excess or deficiency), jaundice and the appearance of agitation and decreased ability to express facially. It is also possible that it may cause increased sensitivity to sunlight, fever, skin rashes, dark urine, leukopenia, thrombocytopenia or priapism.

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More serious symptoms may include confusion, the possible appearance of arrhythmias and bradycardias, hyperthermia seizures and even neuroleptic malignant syndrome (a dangerous syndrome that can lead to the death of the patient, being one of the reasons that requires precise control of the dosage).

Contraindications

In addition to the above, it must be taken into account that some sectors of the population are contraindicated for this drug, or its consumption must be carefully assessed. These include all those people who have suffered brain injuries, liver or kidney diseases, epileptic seizures, major depression, respiratory problems or heart or cardiovascular problems (especially in the case of a previous heart attack). In addition, It is contraindicated for those people who have had pheochromocytoma (tumor of the adrenal medulla).

Another sector of the population that is contraindicated for this drug is people with diabetes, since it tends to increase blood glucose levels. It is also necessary to take into account the possible interaction with other drugs and drugs, which can intensify or cancel the effect of the drug with dangerous results for health. For example, Its use is contraindicated with depressant substances such as alcohol and other drugs Elderly people with dementia also have it contraindicated, having observed that in these types of patients the probability of death increases.