The primary application of trifluoperazine is for schizophrenia. Other official indications may vary country by country, but generally it is also indicated for use in agitation and patients with behavioural problems, severe nausea and vomiting as well as severe anxiety. Trials have shown a moderate benefit of this drug in patients with boderline personality disorder. Its use in many parts of the world has declined because of highly frequent and severe early and late tardive dyskinesia, a type of extrapyramidal symptom. The annual development rate of tardive dyskinesia may be as high as 4%.
The results of a randomized placebo-controlled, flexible-dose acute treatment study indicate that the antipsychotic drug trifluoperazine had superior efficacy from the first week of double-blind treatment, although there were markedly more treatment emergent adverse events with trifluoperazine (62%,compared to 46% with placebo)
A 2006 study suggested that trifluoperazine may be able to reverse addiction to opioids.
A multi-year UK study by the Alzheimer's Research Trust suggested that this and other antipsychotic drugs commonly given to Alzheimer's patients with mild behavioural problems often make their condition worse. The study concluded that
For most patients with AD, withdrawal of neuroleptics had no overall detrimental effect on functional and cognitive status and by some measures improved functional and cognitive status. Neuroleptics may have some value in the maintenance treatment of more severe neuropsychiatric symptoms, but this possibility must be weighed against the unwanted effects of therapy. The current study helps to inform a clinical management strategy for current practice, but the considerable risks of maintenance therapy highlight the urgency of further work to find, develop, and implement safer and more effective treatment approaches for neuropsychiatric symptoms in people with AD.
Trifluoperazine is contraindicated in CNS depression, coma, and blood dyscrasias. Trifluoperazine should be used with caution in patients suffering from renal or hepatic impairment.
In the United Kingdom and some other countries, Trifluoperazine is sold and marketed under the brand 'Stelazine'.
The drug is sold as tablet, liquid and 'Trifluoperazine-injectable USP' for deep intramuscular short-term use.
In the past, trifluoperazine was used in fixed combinations with the MAO inhibitor (antidepressant) tranylcypromine to attenuate the strong stimulating effects of this antidepressant. This combination was sold under the brand name Jatrosom N. Likewise a combination with amobarbital (potent sedative/hypnotic agent) for the amelioration of psychoneurosis and insomnia existed under the brand name Jalonac. In Italy the first combination is still available, sold under the brand name Parmodalin (10 mg of Tranylcypromine and 1 mg of Trifluoperazine).
Trifluoperazine (2-trifluoromethyl-10-[3-(4-methyl-1-piperazinyl)propyl]phenothazine) is synthesized in the manner described already for prochlorperazine, alkylation is performed using 2-trifluoromethylphenothazin-4-methyl-1-piperazinylpropylchloride as the substrate.
Craig, P.; Nodiff, E.; Lafferty, J.; Ullyot, G. (1957). Journal of Organic Chemistry22 (6): 709. doi:10.1021/jo01357a618.edit
B.H. Chung, F. Zimalkowski, Arch. Pharm., 317, 323 (1984).
^Rex William Cowdry, David L. Gardner (1988). "Pharmacotherapy of Borderline Personality DisorderAlprazolam, Carbamazepine, Trifluoperazine, and Tranylcypromine". Arch Gen Psychiatry45 (2): 111–119. doi:10.1001/archpsyc.1988.01800260015002.
^David S. Baldwin, Polkinghorn (2005). "Evidence-based pharmacotherapy of generalized anxiety disorder". International Journal of Neuropsychopharmacology8: 293–302. doi:10.1017/S1461145704004870.