Triflupromazine

N05AA05

Neuroleptic

• 352.42 g · mol -1 ( triflupromazine )
• 388.88 g.mol -1 ( triflupromazine · hydrochloride)

Hydrochloride

Risk

185 mg · kg -1 ( LD50, rat, oral)

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Triflupromazine, a phenothiazine derivative, was used as antipsychotic and antiemetic. Due to changes in admission requirements, it is since 2003 in Germany no longer commercially available (former name: Psyquil ®).

Mechanism of Action

Triflupromazine is an antagonist to the D1 and D2 receptors.

It exhibits a moderate affinity for the D2, α1, 5- HT2 and H1 receptors, and a weak affinity for M1 receptors. Triflupromazine also acts as FIASMA ( functional inhibitors of acid sphingomyelinase ).

Side effects

Under treatment with triflupromazine can - for a dopamine antagonist typical - extrapyramidal side effects such as tremor, rigidity, akathisia or tardive dyskinesia occur. It also lowers blood pressure. Cardiac arrhythmias are possible.

Pharmacokinetics

Triflupromazine undergoes extensive first -pass effect. Elimination occurs mainly through reduction in the liver.