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Trifluoperazine, sold under a number of brand names, is a typical antipsychotic primarily used to treat schizophrenia.^[1] It may also be used short term in those with generalized anxiety disorder but is less preferred to benzodiazepines.^[1] It is of the phenothiazine chemical class.

Medical uses

Schizophrenia

Trifluoperazine is an effective antipsychotic for people with schizophrenia.^[2] 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.^[2] There is low-quality evidence that trifluoperazine reduces the risk of relapse when compared with placebo when people are followed for 5 months.^[2] 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.^[2]

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.^[3]

Other

It appears to be effective for people with generalized anxiety disorder but the benefit–risk ratio was unclear as of 2005.^[4]

It has been experimentally used as a drug to kill eukaryotic pathogens like fungi and amoebozoa in humans.^[5]

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%.^{[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.^[6] It is also more likely to cause somnolence and anticholinergic side effects such as red eye and xerostomia (dry mouth).^[6] All antipsychotics can cause the rare and sometimes fatal neuroleptic malignant syndrome.^[7] Trifluoperazine can lower the seizure threshold.^[8] The antimuscarinic action of trifluoperazine can cause excessive dilation of the pupils (mydriasis), which increases the chances of patients with hyperopia developing glaucoma.^[9]

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,^[10] antidopaminergic,^[11]^[12] and minimal anticholinergic effects.^[13] 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.^[6]

Names

Brand names include Eskazinyl, Eskazine, Jatroneural, Modalina, Stelazine, Terfluzine, Trifluoperaz, 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.

GP studying pharmacological data has indicated cases of neck vertebrae irreversible fusing leading to NHS preparations being predominantly of the liquid form trifluoperazine as opposed to the tablet form as in Stela zine etc.

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. 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).

References

^ ^a ^b "Trifluoperazine Hydrochloride". The American Society of Health-System Pharmacists. Retrieved 8 January 2017.
^ ^a ^b ^c ^d Koch, K; Mansi, K; Haynes, E (2014). "Trifluoperazine versus placebo for schizophrenia". Cochrane Database of Systematic Reviews. 1 (1): CD010226.pub2. doi:10.1002/14651858.CD010226.pub2. PMC 6718209. PMID 24414883. Lay summary (20 July 2017).
^ Tardy, M; Dold, M; Engel, RR; Leucht, S (8 July 2014). "Trifluoperazine versus low-potency first-generation antipsychotic drugs for schizophrenia". The Cochrane Database of Systematic Reviews (7): CD009396. doi:10.1002/14651858.CD009396.pub2. PMID 25003310.
^ David S. Baldwin, Polkinghorn (2005). "Evidence-based pharmacotherapy of generalized anxiety disorder". International Journal of Neuropsychopharmacology. 8 (2): 293–302. doi:10.1017/S1461145704004870. PMID 15576000.
^ Deetz, T. R.; Sawyer, M. H.; Billman, G.; Schuster, F. L.; Visvesvara, G. S. (2003). "Successful Treatment of Balamuthia Amoebic Encephalitis: Presentation of 2 Cases". Clinical Infectious Diseases. 37 (10): 1304–1312. doi:10.1086/379020. ISSN 1058-4838. PMID 14583863.
^ ^a ^b ^c Marques LO, Lima MS, Soares BG (2004). "Trifluoperazine for schizophrenia". Cochrane Database of Systematic Reviews (1): CD003545. doi:10.1002/14651858.CD003545.pub2. PMC 7003674. PMID 14974020.CS1 maint: multiple names: authors list (link)
^ Smego RA, Durack DT (June 1982). "The neuroleptic malignant syndrome". Archives of Internal Medicine. 142 (6): 1183–5. doi:10.1001/archinte.142.6.1183. PMID 6124221.
^ Hedges D, Jeppson K, Whitehead P (July 2003). "Antipsychotic medication and seizures: a review". Drugs of Today. 39 (7): 551–7. doi:10.1358/dot.2003.39.7.799445. PMID 12973403.
^ Boet DJ (July 1970). "Toxic effects of phenothiazines on the eye". Documenta Ophthalmologica. Advances in Ophthalmology. 28 (1): 1–69. doi:10.1007/BF00153873. PMID 5312274.
^ Huerta-Bahena J, Villalobos-Molina R, García-Sáinz JA (January 1983). "Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects". Molecular Pharmacology. 23 (1): 67–70. PMID 6135146. Retrieved 2009-06-21.
^ Seeman P, Lee T, Chau-Wong M, Wong K (June 1976). "Antipsychotic drug doses and neuroleptic/dopamine receptors". Nature. 261 (5562): 717–9. Bibcode:1976Natur.261..717S. doi:10.1038/261717a0. PMID 945467.
^ Creese I, Burt DR, Snyder SH (1996). "Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs". The Journal of Neuropsychiatry and Clinical Neurosciences. 8 (2): 223–6. doi:10.1176/jnp.8.2.223. PMID 9081563. Retrieved 2009-06-21.
^ Ebadi, Manuchair S (1998). "Trifluoperazine Hydrochloride". CRC desk reference of clinical pharmacology (illustrated ed.). CRC Press. ISBN 978-0-8493-9683-0. Retrieved 2009-06-21.

UpToDate Contents

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1. 第1世代抗精神病剤：薬理学、投与、および副作用の比較first generation antipsychotic medications pharmacology administration and comparative side effects [show details]
…high-potency FGAs (fluphenazine, haloperidol, loxapine, perphenazine, pimozide, thiothixene, and trifluoperazine) are dosed in the range of 1 to 10s of milligrams and have low activity at histaminic and muscarinic …
2. 皮膚寄生虫妄想の治療treatment of delusional infestation [show details]
…treating delusional infestation include pimozide , perphenazine , chlorpromazine , thioridazine , trifluoperazine, haloperidol, and fluphenazine . SGAs described in case reports and case series as effectively…
3. 産後精神病の治療treatment of postpartum psychosis [show details]
…to access limitations), we prefer the high-potency agents, such as haloperidol, perphenazine, trifluoperazine, and thiothixene. The decision as to which drug to use should be made on a case-by-case basis…
4. 授乳中の乳児：物質使用障害による抗精神病薬、リチウム、刺激薬、および薬剤への曝露の安全性breastfeeding infants safety of exposure to antipsychotics lithium stimulants and medications for substance use disorders [show details]
…flupenthixol, perphenazine, trifluoperazine, or zuclopenthixol (total n = 18 infants) found no acute adverse events . In addition, a review concluded that perphenazine and trifluoperazine are excreted in breast…
5. 妊娠女性における双極性障害：躁病および軽躁の治療bipolar disorder in pregnant women treatment of mania and hypomania [show details]
…alternatives to haloperidol include chlorpromazine, fluphenazine, perphenazine, thiothixene, and trifluoperazine . Clinicians can expect that response to a first-generation antipsychotic will occur in approximately …

English Journal

Trifluoperazine an Antipsychotic Drug and Inhibitor of Mitochondrial Permeability Transition Protects Cytarabine and Ifosfamide-Induced Neurotoxicity.

Kiani A, Nik SH, Khodadoost A, Salimi A, Pourahmad J.
Drug research. 2020 May;().
The link between Ca dysregulation, mitochondria damages, oxidative stress and cellular derangement is particularly evident in neurotoxicity induced by chemotherapeutic agents. In the current study, we investigated effects of trifluoperazine (TFP) as an inhibitor of calmodulin against the cytotoxicit
PMID 32365382

The dopamine receptor antagonist trifluoperazine prevents phenotype conversion and improves survival in mouse models of glioblastoma.

Bhat K, Saki M, Vlashi E, Cheng F, Duhachek-Muggy S, Alli C, Yu G, Medina P, He L, Damoiseaux R, Pellegrini M, Zemke NR, Nghiemphu PL, Cloughesy TF, Liau LM, Kornblum HI, Pajonk F.
Proceedings of the National Academy of Sciences of the United States of America. 2020 May;().
Glioblastoma (GBM) is the deadliest adult brain cancer, and all patients ultimately succumb to the disease. Radiation therapy (RT) provides survival benefit of 6 mo over surgery alone, but these results have not improved in decades. We report that radiation induces a glioma-initiating cell phenotype
PMID 32358191

The effect of neuroleptic drugs on DPPC/sphingomyelin/cholesterol membranes.

Pérez-Isidoro R, Costas M.
Chemistry and physics of lipids. 2020 Apr;()104913.
The hydrophobic nature of neuroleptic drugs renders that these molecules interact not only with protein receptors, but also with the lipids constituting the membrane bilayer. We present a systematic study of the effect of seven neuroleptic drugs on a biomembrane model composed of DPPC, sphingomyelin
PMID 32335028

Japanese Journal

Tamoxifen and trifluoroperazine (Stelazine) potentiate cytostatic/cytotoxic effects of P-30 Protein, a novel protein possessing antitumor activity

MIKULSKI SM
Cell Tissue Kinet 32, 237-246, 1990
NAID 30036933572

Phenothiazines and Chromosome Damage

Jenkins Edmund C.
ＣＹＴＯＬＯＧＩＡ 35(4), 552-560, 1970
… The phenothiazines involved in the study are chlorpromazine (thorazine) and trifluoperazine hydrochloride (stelazine). …
NAID 130003954377

「トリフロペラジン」

Trifluoperazine
Clinical data
Trade names	Stelazine, Eskazinyl, Eskazine, Jatroneural, others
AHFS/Drugs.com	Monograph
MedlinePlus	a682121
Pregnancy; category	AU: C ; US: C (Risk not ruled out) ; ;
Routes of; administration	By mouth, IM
ATC code	N05AB06 (WHO) ;
Legal status
Legal status	UK: POM (Prescription only) ; US: ℞-only ;
Pharmacokinetic data
Metabolism	Liver
Elimination half-life	10–20 hours
Identifiers
	IUPAC name 10-[3-(4-methylpiperazin-1-yl)propyl]-; 2-(trifluoromethyl)-10H-phenothiazine;
CAS Number	117-89-5 ;
PubChem CID	5566;
IUPHAR/BPS	214;
DrugBank	DB00831 ;
ChemSpider	5365 ;
UNII	214IZI85K3;
ChEBI	CHEBI:45951 ;
ChEMBL	ChEMBL422 ;
PDB ligand	TFP (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID1046928 ;
ECHA InfoCard	100.003.837
Chemical and physical data
Formula	C21H24F3N3S
Molar mass	407.497 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES FC(F)(F)c2cc1N(c3c(Sc1cc2)cccc3)CCCN4CCN(C)CC4;
	InChI InChI=1S/C21H24F3N3S/c1-25-11-13-26(14-12-25)9-4-10-27-17-5-2-3-6-19(17)28-20-8-7-16(15-18(20)27)21(22,23)24/h2-3,5-8,15H,4,9-14H2,1H3 ; Key:ZEWQUBUPAILYHI-UHFFFAOYSA-N ;
(verify)

　　[★]

英: trifluoperazine TFP
化: マレイン酸トリフロペラジン trifluoperazine maleate、trifluoperazine hydrochloride
商: トリフロペラジン、Stelazine

向精神薬

抗精神病薬

フェノチアジン系

[AHFS2017-1] "Trifluoperazine Hydrochloride". The American Society of Health-System Pharmacists. Retrieved 8 January 2017.

[Koc2014-2] Koch, K; Mansi, K; Haynes, E (2014). "Trifluoperazine versus placebo for schizophrenia". Cochrane Database of Systematic Reviews. 1 (1): CD010226.pub2. doi:10.1002/14651858.CD010226.pub2. PMC 6718209. PMID 24414883. Lay summary (20 July 2017).

[3] Tardy, M; Dold, M; Engel, RR; Leucht, S (8 July 2014). "Trifluoperazine versus low-potency first-generation antipsychotic drugs for schizophrenia". The Cochrane Database of Systematic Reviews (7): CD009396. doi:10.1002/14651858.CD009396.pub2. PMID 25003310.

[4] David S. Baldwin, Polkinghorn (2005). "Evidence-based pharmacotherapy of generalized anxiety disorder". International Journal of Neuropsychopharmacology. 8 (2): 293–302. doi:10.1017/S1461145704004870. PMID 15576000.

[DeetzSawyer2003-5] Deetz, T. R.; Sawyer, M. H.; Billman, G.; Schuster, F. L.; Visvesvara, G. S. (2003). "Successful Treatment of Balamuthia Amoebic Encephalitis: Presentation of 2 Cases". Clinical Infectious Diseases. 37 (10): 1304–1312. doi:10.1086/379020. ISSN 1058-4838. PMID 14583863.

[Marq-6] Marques LO, Lima MS, Soares BG (2004). "Trifluoperazine for schizophrenia". Cochrane Database of Systematic Reviews (1): CD003545. doi:10.1002/14651858.CD003545.pub2. PMC 7003674. PMID 14974020.CS1 maint: multiple names: authors list (link)

[7] Smego RA, Durack DT (June 1982). "The neuroleptic malignant syndrome". Archives of Internal Medicine. 142 (6): 1183–5. doi:10.1001/archinte.142.6.1183. PMID 6124221.

[8] Hedges D, Jeppson K, Whitehead P (July 2003). "Antipsychotic medication and seizures: a review". Drugs of Today. 39 (7): 551–7. doi:10.1358/dot.2003.39.7.799445. PMID 12973403.

[9] Boet DJ (July 1970). "Toxic effects of phenothiazines on the eye". Documenta Ophthalmologica. Advances in Ophthalmology. 28 (1): 1–69. doi:10.1007/BF00153873. PMID 5312274.

[10] Huerta-Bahena J, Villalobos-Molina R, García-Sáinz JA (January 1983). "Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects". Molecular Pharmacology. 23 (1): 67–70. PMID 6135146. Retrieved 2009-06-21.

[11] Seeman P, Lee T, Chau-Wong M, Wong K (June 1976). "Antipsychotic drug doses and neuroleptic/dopamine receptors". Nature. 261 (5562): 717–9. Bibcode:1976Natur.261..717S. doi:10.1038/261717a0. PMID 945467.

[12] Creese I, Burt DR, Snyder SH (1996). "Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs". The Journal of Neuropsychiatry and Clinical Neurosciences. 8 (2): 223–6. doi:10.1176/jnp.8.2.223. PMID 9081563. Retrieved 2009-06-21.

[13] Ebadi, Manuchair S (1998). "Trifluoperazine Hydrochloride". CRC desk reference of clinical pharmacology (illustrated ed.). CRC Press. ISBN 978-0-8493-9683-0. Retrieved 2009-06-21.

v t e Antipsychotics (N05A)
Typical	Butyrophenones: Benperidol Bromperidol Droperidol Haloperidol^# Moperone Pipamperone Spiperone Timiperone Trifluperidol Diphenylbutylpiperidines: Fluspirilene Penfluridol Pimozide Phenothiazines: Acetophenazine Butaperazine Carphenazine (carfenazine)^‡ Chlorpromazine Cyamemazine Dixyrazine Fluphenazine Levomepromazine (methotrimeprazine) Mesoridazine Perazine Periciazine Perphenazine Piperacetazine Pipotiazine Prochlorperazine Promazine Sulforidazine Thiopropazate Thioproperazine Thioridazine Trifluoperazine Triflupromazine Thioxanthenes: Chlorprothixene Clopenthixol Flupentixol Tiotixene (thiothixene) Zuclopenthixol
Disputed	Benzamides: Amisulpride Levosulpiride Nemonapride Remoxipride^‡ Sulpiride Sultopride Tiapride Veralipride^‡ Butyrophenones: Melperone Tricyclics: Carpipramine Clocapramine Clorotepine Clotiapine Loxapine Mosapramine Others: Molindone
Atypical	Benzisoxazole/benzisothiazoles: Iloperidone Lurasidone Paliperidone Paliperidone palmitate Perospirone Risperidone^# Ziprasidone Butyrophenones: Lumateperone Phenylpiperazines/quinolinones: Aripiprazole Aripiprazole lauroxil Brilaroxazine^† Brexpiprazole Cariprazine Tricyclics: Asenapine Clozapine^# Olanzapine Quetiapine Zotepine Others: Blonanserin Pimavanserin Sertindole
Others	Azacyclonol Cannabidiol Oxypertine Reserpine Tetrabenazine
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

v t e Tricyclics
Classes	Acridine Anthracene Dibenzazepine Dibenzocycloheptene Dibenzodiazepine Dibenzothiazepine Dibenzothiepin Dibenzoxazepine Dibenzoxepin Phenothiazine Pyridazinobenzoxazine Pyridinobenzodiazepine Thioxanthene
Antidepressants (TCAs and TeCAs)	7-OH-Amoxapine Amezepine Amineptine Amitriptyline Amitriptylinoxide Amoxapine Aptazapine Azepindole Azipramine Batelapine Butriptyline Cianopramine Ciclazindol Ciclopramine Cidoxepin Clomipramine Cotriptyline Cyanodothiepin Demexiptiline Depramine (balipramine) Desipramine (desmethylimipramine) Desmethylclomipramine Desmethyltrimipramine Dibenzepin Dimetacrine Dosulepin (dothiepin) Doxepin Enprazepine Esmirtazapine Fantridone Fluotracen Hepzidine Homopipramol Imipramine Imipraminoxide Intriptyline Iprindole Ketipramine Litracen Lofepramine Losindole Loxapine Maprotiline Mariptiline Mazindol Melitracen Metapramine Mezepine Mianserin Mirtazapine Monometacrine Naranol Nitroxazepine Norbutriptyline Nordoxepin Northiaden (nordosulepin) Nortriptyline (noramitriptyline) Noxiptiline Octriptyline Opipramol Oxaprotiline Pipofezine Pirandamine Propizepine Protriptyline Quinupramine Setiptiline (teciptiline) Spiroxepin Tandamine Tampramine Tianeptine Tienopramine Trimipramine
Antihistamines	Azatadine Bisulepin Clobenzepam Cyproheptadine Dacemazine Deptropine Desloratadine Epinastine Etymemazine Fenethazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Ketotifen Latrepirdine Loratadine Mebhydrolin Mequitazine Methdilazine Olopatadine Oxomemazine Phenindamine Pimethixene Promethazine Propiomazine Rupatadine Thiazinamium
Antipsychotics	Acetophenazine Alimemazine Amoxapine Asenapine Butaclamol Butaperazine Carfenazine (carphenazine) Carpipramine Chlorpromazine Chlorprothixene Ciclindole Citatepine Clocapramine Clomacran Clorotepine Clotiapine Clozapine Cyanothepin Doclothepin Docloxythepin Erizepine Flucindole Flumezapine Fluotracen Flupentixol Fluphenazine Gevotroline Homopipramol Isofloxythepin Levomepromazine/Methotrimeprazine Loxapine Lurasidone Maroxepin Meperathiepin Mesoridazine Metiapine Metitepine Metoxepin Mosapramine Naranol Octomethothepin Olanzapine Oxyclothepin Oxyprothepin Pentiapine Peradithiepin Perathiepin Perazine Perphenazine Periciazine Pinoxepin Piperacetazine Pipotiazine Piquindone Prochlorperazine Promazine Prothipendyl Quetiapine Savoxepin/Cipazoxapine Sulforidazine Tenilapine Thiethylperazine Thiopropazate Thioridazine Thiothixene Tilozepine Traboxopine Trifluoperazine Triflupromazine Trifluthepin Zotepine Zuclopenthixol
Anticonvulsants	Carbamazepine Dizocilpine Eslicarbazepine Eslicarbazepine acetate Etazepine Licarbazepine Oxcarbazepine Oxitriptyline Rispenzepine
Others	Adosopine Aminopromazine Atiprosin Beloxepin Benzoctamine Carvedilol Cidoxepin Cyclobenzaprine Damotepine Darenzepine Elanzepine Fluradoline Methylene blue Monatepil Nuvenzepine Oxetorone Perlapine P7C3 Pinadoline Pirenzepine Pirolate Pitrazepin Pizotifen Profenamine Serazapine Siltenzepine Telenzepine Tipindole Tropatepine Zolenzepine

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案内

案内

Stelazine