Triflupromazine

Triflupromazine belongs to the class of neuroleptics. As such, the drug is used to treat psychiatric illnesses. However, it can also be used in other medical fields. In the Federal Republic of Germany, triflupromazine has not been allowed to 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. Medications or substances that have psychotropic effects, i.e. have a sedative, antipsychotic or anti-autistic effect, are considered neuroleptic. Such preparations are known as neuroleptics and are used in psychiatry to treat various mental illnesses with drugs. For this reason, the active ingredient triflupromazine is also classified as psychotropic or neuroleptic and is referred to as such.

A preparation is anti-emetic if it prevents vomiting. Due to its antimetic properties, triflupromazine is also indicated outside of psychiatry. In 2003 the active ingredient lost its approval in the Federal Republic of Germany, where it was sold under the trade name Psyquil®.

In chemistry and pharmacology, triflupromazine is described by the empirical formula C 18 - H 19 - F 3 - N 2 - S. In its basic form, the active ingredient has a moral mass of 352.42 g / mol. The hydrochloride form, which is also frequently used, on the other hand, has a moral mass of 388.88 g / mol.

Pharmacological effect

The mechanism of action of triflupromazine is based on its property as an antagonist of the D1 and D2 receptors. The drug thus inhibits the substances that bind to the free receptors.

In addition, a moderate affinity for other receptors has been recognized in numerous cases in the literature. Taking triflupromazine therefore also affects other receptors. These include D2, 5-HT2, Alpha1, and H1 receptors. A weak affinity for M1 receptors could be demonstrated.

It is also known that triflupromazine can act as an inhibitor of acid sphringomyelinase. Use as FIASMA (functional inhibitor of acid sphingomyelinase) is therefore conceivable.

Medical application & use

Triflupromazine has both neuroleptic and antimetic properties. Nevertheless, the main field of application of the active ingredient is psychiatry. An indication is therefore for severe psychoses or hallucinations (especially those that occur in connection with schizophrenia) and acute psychomotor excitement.

Outside of psychiatry, there is also an indication for the treatment of severe vomiting, acute nausea and dizziness.

In all cases, the active ingredient is administered orally in the form of film-coated tablets. These can be taken by the patient independently. However, the active ingredient is subject to pharmacy and prescription requirements in all countries for which there is approval.

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Risks & side effects

Triflupromazine can lead to undesirable side effects, so that it is not risk-free. The treatment should be discontinued completely or completely omitted if an intolerance (allergy) to the drug is known. 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 to be an involuntary, strictly rhythmic disturbance of movement that is caused by a continuous contraction of various muscle groups. Rigidity is used when the body is hardened or solidified. The term is the counterpart to flexibility. Akinesia, on the other hand, describes a pathogenic immobility of the skeletal or heart muscles.

It has also been shown that triflupromazine influences the liver values. Patients who suffer from acute liver damage should only be treated with the active ingredient if no milder agent is available.

Interactions with centrally acting substances such as alcohol are also conceivable. With regard to antihypertensive drugs, an unexpected increase in the effect is possible. The effectiveness of dopamine agonists such as amantadine, levodopa or bromocriptine, on the other hand, can be severely restricted by taking triflupromazine. This also applies to the blood pressure lowering effect of guanethidine. The attending physician must therefore always be informed about all preparations.

Because of the risk of an excessive drop in blood pressure, special care must be taken before an operation is performed. Medical supervision of the patient may be necessary. The amount of anesthetics to be administered should be reduced appropriately.