Trifluoperazine

Trifluoperazine is an effective antipsychotic for people with schizophrenia condition. 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. There is low-quality evidence that trifluoperazine reduces the risk of relapse when compared with placebo when people are followed for 5 months. 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.{{cite journal | vauthors = Koch K, Mansi K, Haynes E, Adams CE, Sampson S, Furtado VA | title = Trifluoperazine versus placebo for schizophrenia | journal = The Cochrane Database of Systematic Reviews | volume = 1 | issue = 1 | pages = CD010226 | date = January 2014 | pmid = 24414883 | pmc = 6718209 | doi = 10.1002/14651858.CD010226.pub2 }} {{slink|Wikiversity:Trifluoperazine_versus_placebo_for_schizophrenia|References}}

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.{{cite journal | vauthors = Tardy M, Dold M, Engel RR, Leucht S | title = Trifluoperazine versus low-potency first-generation antipsychotic drugs for schizophrenia | journal = The Cochrane Database of Systematic Reviews | issue = 7 | pages = CD009396 | date = July 2014 | pmid = 25003310 | doi = 10.1002/14651858.CD009396.pub2 | pmc = 11227318 }}

It appears to be effective for people with generalized anxiety disorder but the benefit{{endash}}risk ratio was unclear as of 2005.{{cite journal | vauthors = Baldwin DS, Polkinghorn C | title = Evidence-based pharmacotherapy of Generalized Anxiety Disorder | journal = The International Journal of Neuropsychopharmacology | volume = 8 | issue = 2 | pages = 293–302 | date = June 2005 | pmid = 15576000 | doi = 10.1017/S1461145704004870 | doi-access = free }}

It has been experimentally used as a drug to kill eukaryotic pathogens such as Balamuthia in humans.{{cite journal | vauthors = Deetz TR, Sawyer MH, Billman G, Schuster FL, Visvesvara GS | title = Successful treatment of Balamuthia amoebic encephalitis: presentation of 2 cases | journal = Clinical Infectious Diseases | volume = 37 | issue = 10 | pages = 1304–1312 | date = November 2003 | pmid = 14583863 | doi = 10.1086/379020 | doi-access = free }}

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%.{{Citation needed|date=April 2009}}

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.{{cite journal |vauthors=Marques LO, Lima MS, Soares BG | title = Trifluoperazine for schizophrenia| journal = Cochrane Database of Systematic Reviews| issue = 1| pages = CD003545| year = 2004| volume = 2004| pmid = 14974020| doi = 10.1002/14651858.CD003545.pub2| pmc = 7003674}} It is also more likely to cause somnolence and anticholinergic side effects such as red eye and xerostomia (dry mouth). All antipsychotics can cause the rare and sometimes fatal neuroleptic malignant syndrome.{{cite journal|vauthors=Smego RA, Durack DT | title = The neuroleptic malignant syndrome| journal = Archives of Internal Medicine| volume = 142| issue = 6| pages = 1183–5| date=June 1982| pmid = 6124221| doi = 10.1001/archinte.142.6.1183}} Trifluoperazine can lower the seizure threshold.{{cite journal|vauthors=Hedges D, Jeppson K, Whitehead P | title = Antipsychotic medication and seizures: a review| journal = Drugs of Today| volume = 39| issue = 7| pages = 551–7| date=July 2003| pmid = 12973403| doi = 10.1358/dot.2003.39.7.799445}} The antimuscarinic action of trifluoperazine can cause excessive dilation of the pupils (mydriasis), which increases the chances of patients with hyperopia developing glaucoma.{{cite journal | vauthors = Boet DJ | title = Toxic effects of phenothiazines on the eye | journal = Documenta Ophthalmologica. Advances in Ophthalmology | volume = 28 | issue = 1 | pages = 1–69 | date = July 1970 | pmid = 5312274 | doi = 10.1007/BF00153873 | hdl-access = free | s2cid = 26145461 | hdl = 1765/26543 }}

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

Trifluoperazine has central antiadrenergic,{{cite journal|vauthors=Huerta-Bahena J, Villalobos-Molina R, García-Sáinz JA | title = Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects| journal = Molecular Pharmacology| volume = 23| issue = 1| pages = 67–70| date=January 1983| pmid = 6135146| url = http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=6135146| access-date = 2009-06-21}} antidopaminergic,{{cite journal|vauthors=Seeman P, Lee T, Chau-Wong M, Wong K | title = Antipsychotic drug doses and neuroleptic/dopamine receptors| journal = Nature| volume = 261| issue = 5562| pages = 717–9| date=June 1976| pmid = 945467| doi = 10.1038/261717a0| bibcode=1976Natur.261..717S| s2cid = 4164538}}{{cite journal| vauthors = Creese I, Burt DR, Snyder SH| title = Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs| journal = The Journal of Neuropsychiatry and Clinical Neurosciences| volume = 8| issue = 2| pages = 223–6| year = 1996| pmid = 9081563| doi = 10.1176/jnp.8.2.223| url = http://neuro.psychiatryonline.org/cgi/content/abstract/8/2/223| access-date = 2009-06-21| archive-date = 2011-07-27| archive-url = https://archive.today/20110727191024/http://neuro.psychiatryonline.org/cgi/content/abstract/8/2/223| url-status = dead| url-access = subscription}} and minimal anticholinergic effects.{{cite book| vauthors = Ebadi MS | title=CRC desk reference of clinical pharmacology| url=https://books.google.com/books?id=-EAxShTKfGAC| access-date=2009-06-21| edition=illustrated| year=1998| publisher=CRC Press| isbn=978-0-8493-9683-0| chapter=Trifluoperazine Hydrochloride| chapter-url=https://books.google.com/books?id=-EAxShTKfGAC&q=trifluoperazine%20anticholinergic&pg=PA580}} 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. It also has antihistaminergic properties (H₁ K_i = 17.5{{cite journal | vauthors = Hill SJ, Young M | title = Antagonism of central histamine H1 receptors by antipsychotic drugs | journal = European Journal of Pharmacology | volume = 52 | issue = 3–4 | pages = 397–399 | date = December 1978 | pmid = 32056 | doi = 10.1016/0014-2999(78)90297-2 }}).

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.

{{Reflist|30em}}

{{Antipsychotics}}

{{Navboxes

| title = Pharmacodynamics

| titlestyle = background:#ccccff

| list1 =

{{Adrenergic receptor modulators}}

{{Dopamine receptor modulators}}

{{Histamine receptor modulators}}

{{Serotonin receptor modulators}}

{{Sigma receptor modulators}}

}}

{{Tricyclics}}

Category:Trifluoromethyl compounds

Category:Phenothiazines

Category:4-Methylpiperazin-1-yl compounds

Category:Typical antipsychotics