Trifluperidol belongs to the class of typical neuroleptics. It was mainly used to treat mania and schizophrenia. Today, it is rarely used.
What is trifluperidol?
Trifluperidol belongs to the class of typical neuroleptics. It has been used mainly for mania and schizophrenia. Typical neuroleptics are the generation of older neuroleptics that were used before the discovery of the active ingredient clozapine in 1979, but are rarely used today because of their severe side effects. Trifluperidol belongs to this group. Chemically, trifluperidol is a butyrophenone and related to haloperidol (Haldol). It is a very potent antipsychotic drug developed by Janssen Phamaceutica in 1959. While haliperidol is still widely used due to its highly potent antipsychotic effects, comparative studies have shown that trifluperidol has stronger side effects but performs much worse in terms of efficacy. For this reason, interest in trifluperidol has waned considerably. Numerous experts believe that it should no longer be relevant in psychiatric practice today, as more effective drugs with significantly fewer side effects are available. The use of trifluperidol was widespread mainly in the US. It was administered either in tablet form or as a depot injection, with depot injections being preferred because patients were rather unwilling to take the drug voluntarily on a regular basis because of the severe side effects.
Pharmacologic effect
Trifluperidol is a so-called dopamine antagonist. Most scientists believe that psychotic symptoms, such as those seen in mania and schizophrenia, are due to an imbalance of dopamine balance in the synaptic cleft. Dopamine is a neurotransmitter that acts as an information transmitter between nerve cells. If there is too much dopamine in the synaptic cleft, this leads to stimulus overload and consequently to psychotic symptoms such as hallucinations, thought disorders, ego disorders and paranoid delusions, which can vary in severity. Trifluperidol docks onto the dopamine receptors in the central nervous system, especially the so-called D2 receptors. This is to prevent too much dopamine from overwhelming the nerve cells. Rather, the goal is to achieve a balance in the neurotransmitter area. This, in turn, is hoped to curb psychotic symptoms. However, trifluperidol – like all psychotropic drugs – not only affects certain metabolic processes in the brain, but has an impact on the entire body, since it is in the bloodstream when administered. As a result, the administration of trifluperidol, for example, also has effects on the so-called basal ganglia. These are nuclei located below the cerebral cortex that are responsible for motor function, but also play a significant role in affect, personal will, spontaneity, and so on. The heart, hormonal balance, sexual functions, kidneys, etc. can also be affected by the administration of neuroleptics (both typical and atypical). Psychotropic drugs that act only on specific sites in the brain do not yet exist. Consequently, a range of side effects must be expected.
Medical application and use
In psychiatric practice, trifluperidol is/was mainly used against psychotic symptoms in the context of manic or schizophrenic disorders. These may include delusions, ego disorders, affect disorders, formal thought disorders, etc. The drug can also be used to treat organically caused psychoses in some circumstances. Organically caused psychoses are physically justifiable and may be caused, for example, by a brain tumor or craniocerebral trauma. Because the symptoms resemble those of manic or schizophrenic psychosis, trifluperidol may thus be indicated. Other uses of trifluperidol include psychomotor agitation, agitation in the context of mental retardation or in the context of autism spectrum disorder, and nausea and vomiting. In rare cases, trifluperidol is also used to treat tic disorders. This is because trifluperidol, as a highly potent neuroleptic, also has a sedative effect. Between 2.5 and 16 mg of the active ingredient are administered.The optimal dose varies from patient to patient, with higher doses usually administered for acute psychotic episodes than for other indications. In addition to use in acute psychotic episodes, trifluperidol is/was also used to prevent them. While the sedative effect is immediate, the antipsychotic effect occurs only after a few days or weeks. Regular use of the drug may help prevent relapse by keeping dopamine levels in the synaptic cleft in balance.
Risks and side effects
Trifluperidol is among the most potent neuroleptics. However, it is also a drug that generally causes very serious side effects. Chief among these are the so-called extrapyramidal motor disorders (EPMS), which can include Parkinson’s-like symptoms, sedentary behavior, and early and tardive dyskinesia. Early and tardive dyskinesias are involuntary twitches in the pharyngeal and lingual areas that are often irreversible and cause particular distress in patients. These extrapyramidal motor disturbances have been found to be particularly frequent and severe with trifluperidol administration. Drug-induced depression is also a regularly occurring consequence, as are hormonal imbalances, seizures, blood count disturbances, and headaches. In rare cases, a so-called malignant neuroleptic syndrome can be caused by the drug, which can become life-threatening and require immediate medical intervention and discontinuation of the drug. Because of these side effects, which are not well proportioned to the beneficial effects, trifluperidol is an unpopular drug that has long been replaced by others.
