Trifluoperazine

Trifluoperazine, marketed under the brand name Stelazine among others, is a typical antipsychotic primarily used to treat schizophrenia.<ref name=AHFS2017>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref> It may also be used short term in those with generalized anxiety disorder but is less preferred to benzodiazepines.<ref name=AHFS2017/> It is of the phenothiazine chemical class. It was approved for medical use in the United States in 1959.<ref name="Howland2016">Template:Cite journal</ref>

Medical uses

Schizophrenia

Trifluoperazine is an effective antipsychotic for people with schizophrenia condition.<ref name=Koc2014/> There is low-quality evidence that trifluoperazine increases the chance of being improved when compared to placebo when people are followed up for 19 weeks.<ref name=Koc2014/> There is low-quality evidence that trifluoperazine reduces the risk of relapse when compared with placebo when people are followed for 5 months.<ref name=Koc2014/> As of 2014 there was no good evidence for a difference between trifluoperazine and placebo with respect to the risk of experiencing intensified symptoms over a 16-week period nor in reducing significant agitation or distress.<ref name=Koc2014>Template:Cite journal Template:Slink</ref>

There is no good evidence that trifluoperazine is more effective for schizophrenia than lower-potency antipsychotics like chlorpromazine, chlorprothixene, thioridazine and levomepromazine, but trifluoperazine appears to cause more adverse effects than these drugs.<ref>Template:Cite journal</ref>

Other

It appears to be effective for people with generalized anxiety disorder but the benefitTemplate:Endashrisk ratio was unclear as of 2005.<ref>Template:Cite journal</ref>

It has been experimentally used as a drug to kill eukaryotic pathogens such as Balamuthia in humans.<ref name="DeetzSawyer2003">Template:Cite journal</ref>

Side effects

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%.Template:Citation needed

A 2004 meta-analysis of the studies on trifluoperazine found that it is more likely than placebo to cause extrapyramidal side effects such as akathisia, dystonia, and Parkinsonism.<ref name="Marq">Template:Cite journal</ref> It is also more likely to cause somnolence and anticholinergic side effects such as red eye and xerostomia (dry mouth).<ref name="Marq"/> All antipsychotics can cause the rare and sometimes fatal neuroleptic malignant syndrome.<ref>Template:Cite journal</ref> Trifluoperazine can lower the seizure threshold.<ref>Template:Cite journal</ref> The antimuscarinic action of trifluoperazine can cause excessive dilation of the pupils (mydriasis), which increases the chances of patients with hyperopia developing glaucoma.<ref>Template:Cite journal</ref>

Contraindications

Trifluoperazine is contraindicated in CNS depression, coma, and blood dyscrasias. Trifluoperazine should be used with caution in patients suffering from renal or hepatic impairment.

Mechanism of action

Trifluoperazine has central antiadrenergic,<ref>Template:Cite journal</ref> antidopaminergic,<ref>Template:Cite journal</ref><ref>Template:Cite journal</ref> and minimal anticholinergic effects.<ref>Template:Cite book</ref> It is believed to work by blockading dopamine D₁ and D₂ receptors in the mesocortical and mesolimbic pathways, relieving or minimizing such symptoms of schizophrenia as hallucinations, delusions, and disorganized thought and speech.<ref name="Marq"/> It also has antihistaminergic properties (H₁ K_i = 17.5<ref>Template:Cite journal</ref>).

Names

Brand names include Eskazinyl, Eskazine, Jatroneural, Modalina, Sizonil, Stelazine, Stilizan, Terfluzine, Trifluoperaz and Triftazin.

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 (tranylcypromine/trifluoperazine) to attenuate the strong stimulating effects of this antidepressant. This combination was sold under the brand name Jatrosom N, Stelapar, Parstelin, among others. It remained available in Italy under the brand name Parmodalin (10 mg of tranylcypromine and 1 mg of trifluoperazine) until its discontinuation in 2019.

Likewise, a combination with amobarbital (potent sedative/hypnotic agent) for the amelioration of psychoneurosis and insomnia existed under the brand name Jalonac.