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 the release of dopamine. It is also a drug that is not marketed everywhere and is subject to a doctor’s prescription.

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

What is Trifluoperazine?

Trifluoperazine is a chemical compound with an antidopaminergic reaction. That is to say that it acts as an antagonist of the dopamine receptors, with which, it has tranquilizing, anxiolytic and powerful antipsychotic effects.

Because of these effects, trifluoperazine belongs to the group of typical antipsychotics , which are also called conventional antipsychotics with neuroleptic (central nervous system depressant) effects.

In very broad terms, it is a drug that decreases the excitation of electrical activity in the brain.

What is it used for and in what disorders?

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 schizophrenic crises with intense anxiety and mania. It is also recommended to treat anxiety that has not responded to other medications.

This drug is available with a prescription and is marketed under different names, depending on the country. Some of the most common are Cuait Trifluoperazine, Eskazine, Stelazine, Tristazine and Stelazine and its oral tablet presentation. In the case of Spain, it has not been marketed since the beginning of 2018. However, there are some generic presentations and it is also distributed by import.

Mechanism of action

Although this mechanism is not precisely defined, several investigations have linked anti-doping actions to the reduction of psychotic experiences. Anti-dopaminergic actions” are those that produce a blockage of the post-synaptic receptors in the mesolimbic cortical pathways.

The latter is one of the brain’s dopaminergic pathways that starts in the midbrain and ends in the limbic system (passing through the amygdala, hippocampus and prefrontal cortex, among other areas). The mesolimbic pathway is one that has been significantly related to situations such as emotional regulation, motivation, emotional gratification and reward mechanisms . The main neurotransmitter acting within this pathway is dopamine.

Because of 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 listening to voices or depersonalization, among others, are very present.

There is a dopaminergic hypothesis that says that these last experiences are related to a hyperactivity of the mesolimbic pathways in the brain, with which, drugs, such as trifluoperazine, have been developed that act as blockers of the dopamine receptors. It is hoped that in the long term trifluoperazine may prevent further psychotic breaks.

Side effects and contraindications

Dopaminergic action not only has neuroleptic effects in reducing psychotic manifestations, but also has effects on other neuronal receptors and on other systems beyond the central nervous system, for example the endocrine 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 may generate more severe adverse reactions such as constant and involuntary motor agitation , combined with periods of extremely slow movement. In relation to other systems, such as the metabolic or endocrine systems, it can cause constipation, reduced sexual activity, hyperglycaemia, among other reactions.

In the case of prescription or overdose, as well as in the case of abrupt withdrawal of the drug, there have been convulsions, loss of consciousness, fever, tachycardia and high-dose liver failure, neuroleptic malignant syndrome, among other adverse reactions that can be fatal.

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

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 in case other pharmacological options have not worked and it is recommended not to prolong the treatment for more than 3 months. The same is true for people who have glaucoma, angina and other associated medical conditions.

Bibliographic references:

  • Marques, LO., Lima, MS. & Soares, BGO. (2004). Trifluoperazine for schizophrenia. Cochrane. Recovered June 15, 2018. Available at http://www.cochrane.org/es/CD003545/trifluoperacina-para-la-esquizofrenia.
  • Psychopharmaceuticals.info (2018). Classification of antipsychotics. Recovered June 15, 2018. Available at http://www.psicofarmacos.info/?contenido=antipsicoticos&farma=eskazine-stelazine-estelazina-triftazina.
  • Vademecum (2015). Trifluoperazine. Recovered June 15, 2018. Available at https://www.vademecum.es/principios-activos-trifluoperazina-n05ab06.