Triflupromazine belongs to the class of neuroleptics. As such, the drug is used to treat psychiatric disorders. In addition, however, it can also be used in other medical specialties. In the Federal Republic of Germany, triflupromazine may no longer be used or prescribed since 2003 due to changes in drug law, as there is no approval.
What is triflupromazine?
Triflupromazine is a drug with neuroleptic and antiemetic effects. Neuroleptic drugs or substances are those that have psychotropic effects, i.e., sedative, antipsychotic, or antiautism. Such preparations are called neuroleptics and are used in psychiatry to treat various mental disorders with medication. For this reason, the active ingredient triflupromazine is also classified as a psychotropic drug or neuroleptic and is referred to as such. A drug is antiemetic if it prevents vomiting. Because of its antimetics properties, triflupromazine also has an indication outside psychiatry. In 2003, however, the active ingredient lost its approval in the Federal Republic of Germany, where it was marketed under the trade name Psyquil. In chemistry or pharmacology, triflupromazine is described by the molecular formula C 18 – H 19 – F 3 – N 2 – S. In its basic form, the drug has a moral mass of 352.42 g/mol. In contrast, the hydrochloride form, which is also commonly used, has a morale mass of 388.88 g/mol.
Pharmacologic Action
The mechanism of action of triflupromazine is built on its property as an antagonist of D1 and D2 receptors. Thus, the drug causes inhibition of substances that bind to the free receptors. In addition, a moderate affinity for other receptors has been recognized in numerous cases in the literature. Therefore, the ingestion of triflupromazine also has effects on other receptors. These include D2, 5-HT2, alpha1, and H1 receptors. A weak affinity has been demonstrated towards M1 receptors. Furthermore, triflupromazine is known to act as an inhibitor of acid sphringomyelinase. Thus, its use as a FIASMA (functional inhibitor of acid sphingomyelinase) is conceivable.
Medical application and use
Triflupromazine has both neuroleptic and antimetabolic properties. Nevertheless, the main field of application of the active ingredient represents psychiatry. Accordingly, an indication exists for severe psychosis or hallucinations (especially those associated with schizophrenia) and acute psychomotor agitation. Outside of psychiatry, there is also an indication for the treatment of severe vomiting, acute nausea, and dizziness. In all cases, the active substance is administered orally in the form of film-coated tablets. These can be taken independently by the patient. However, the active ingredient is subject to pharmacy and prescription requirements in all countries for which approval exists.
Risks and side effects
Triflupromazine may cause undesirable side effects, so taking it is not risk-free. Treatment should be discontinued or completely omitted if there is a known intolerance (allergy) to the drug. In these cases, there is a contraindication. The most common side effects of triflupromazine include the development of cardiac arrhythmias, hypotension, the development of rigidity, akinesia, and tremor. Tremor is understood as an involuntary, strictly rhythmic disturbance of movement caused by continuous contraction of various muscle groups. Rigidity is spoken of when the body hardens or solidifies. The term forms the counterpart of flexibility. Akinesia, on the other hand, refers to a pathogenic immobility of skeletal or cardiac muscles. Furthermore, triflupromazine has been shown to affect liver enzymes. Patients suffering from acute liver damage should only be treated with the active substance if no milder agent is available. Interactions with centrally acting substances such as alcohol are also conceivable. With regard to antihypertensives, an unanticipated potentiation of the effect is possible. The efficacy of dopamine agonists such as amantadine, levodopa or bromocriptine, on the other hand, can be greatly reduced by taking triflupromazine.This also applies to the antihypertensive effect of guanethidine. The attending physician must therefore always be informed about all preparations. Because of the risk of a too massive drop in blood pressure, special caution is also required before performing surgery. Medical monitoring of the patient may be necessary. The amount of anesthetics to be administered should be reduced appropriately.
