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Contraindications and side effects of Trifluoperazine

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Discover the contraindications and side effects of Trifluoperazine.

This drug is part of the treatments sometimes used for the symptoms of schizophrenia.Contraindications and side effects of Trifluoperazine

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Trifluoperazine is a drug that is prescribed to treat some manifestations of schizophrenia.

This is because it has important effects on the mesolimbic pathways that regulate dopamine release.

It is likewise a drug that is not marketed anywhere and that is subject to medical prescription.

In this article, we will see what trifluoperazine is, how it acts on the limbic system, what are its indications and side effects.

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What is Trifluoperazine?

Trifluoperazine is an antidopaminergic reaction chemical compound. In other words, it acts as an antagonist of dopamine receptors, with which it has powerful tranquilizing, anxiolytic, and antipsychotic effects.

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Due to these effects, trifluoperazine is within the group of typical antipsychotics, which are also called conventional antipsychotics with neuroleptic effects (central nervous system depressants).

Broadly speaking, it is a drug that reduces the excitation of electrical activity in the brain.

What is it for and in what disorders is it used?

Trifluoperazine is prescribed to treat some manifestations of the diagnosis of schizophrenia and its main objective is to reduce psychotic experiences.

Due to its important sedative action, it is commonly recommended in acute attacks of schizophrenia with intense anxiety and mania.

Its non-prolonged use is also recommended to treat anxiety disorders that have not responded to other medications.

This medicine is purchased with a prescription and is marketed under different names, depending on the country.

Some of the most common are Cuait Trifluoperazine, Eskazine, Estelazina, Tristazina, and Stelazine and their presentation of tablets for oral administration.

In the case of Spain, it has stopped being marketed since the beginning of 2018. However, there are some generic presentations and it is also distributed by import.

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Mechanism of action

Although this mechanism is not precisely defined, different studies have linked anti-dopaminergic actions with a decrease in psychotic experiences.

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The “antidopaminergic actions” are those that produce a blockage of the postsynaptic receptors in the mesolimbic cortical pathways.

The latter is one of the brain’s dopaminergic pathways that begins in the midbrain and ends in the limbic system (passing through the amygdala, the hippocampus, and the prefrontal cortex, among other areas).

The mesolimbic pathway is one of those that has been significantly related to situations such as emotional regulation, motivation, emotional gratification, and reward mechanisms. The main neurotransmitter that acts within this pathway is dopamine.

Due to its effects in terms of emotional and behavioral regulation, the activity of the mesolimbic pathway is associated with the behavioral and psychic manifestations of schizophrenia.

More specifically with the manifestations of what has been called “positive symptoms” or “psychosis”, where the experiences of hearing voices or depersonalization, among others, are very present.

There is a dopaminergic hypothesis that says that these latest experiences are related to the overactivity of the mesolimbic pathways in the brain, with which drugs, such as trifluoperazine, have been developed that act as dopamine receptors blockers.

In the long term, trifluoperazine is expected to prevent further psychotic outbreaks.

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Side effects of trifluoperazine

The dopaminergic action not only has neuroleptic effects in the reduction of psychotic manifestations but also has effects on other neuronal receptors and other systems beyond the central nervous, for example in the endocrinological system or the metabolic system.

Within the central nervous system, and while trifluoperazine also impacts other pathways (not only the mesolimbic), it can produce some reactions such as drowsiness, dizziness, decreased alertness and responsiveness, photosensitivity, and some visual disturbances.

In addition, the use of trifluoperazine can lead to more serious adverse reactions such as constant and involuntary motor agitation, combined with periods of extremely slow movements.

Concerning other systems, such as the metabolic or endocrine, it can cause constipation, reduced sexual activity, hyperglycemia, among other reactions.

In the case of the prescription or taking of excessive doses, as well as in the case of the abrupt withdrawal of the drug, seizures, loss of consciousness, fever, tachycardia, and liver failure have occurred in high doses, neuroleptic malignant syndrome, among other reactions adverse events that can be fatal.

It is not recommended for use during pregnancy and lactation and should be avoided mixing with other narcotics, anesthetics, sedatives, and alcoholic beverages (otherwise the likelihood of adverse reactions is increased).

Older adults are especially sensitive to the effects of this drug, so special precautions are recommended in this case.

It is especially contraindicated in the case of people with dementia (because it increases the risk of cardiovascular accident and mortality), it is used only if other pharmacological options have not worked and it is recommended not to prolong the treatment for more than 3 months.

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The same is the case for people who have glaucoma, angina pectoris, and other associated medical conditions

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