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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]

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.^[5] It is also more likely to cause somnolence and anticholinergic side effects such as red eye and xerostomia (dry mouth).^[5] All antipsychotics can cause the rare and sometimes fatal neuroleptic malignant syndrome.^[6] Trifluoperazine can lower the seizure threshold.^[7] The antimuscarinic action of trifluoperazine can cause excessive dilation of the pupils (mydriasis), which increases the chances of patients with hyperopia developing glaucoma.^[8]

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.

Pharmacology

Trifluoperazine has central antiadrenergic,^[9] antidopaminergic,^[10]^[11] and minimal anticholinergic effects.^[12] 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.^[5]

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.

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: CD010226.pub2. doi:10.1002/14651858.CD010226.pub2. 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: 293–302. doi:10.1017/S1461145704004870.
^ ^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. PMID 14974020.
^ 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 (Barcelona, Spain : 1998). 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. 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
2. 寄生虫妄想症の治療 treatment of delusional parasitosis
3. 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
4. 統合失調症に対する薬物療法：副作用マネージメント pharmacotherapy for schizophrenia side effect management
5. 精神病性特徴を伴う単極性大うつ病：急性期治療 unipolar major depression with psychotic features acute treatment

English Journal

Social feeding in Caenorhabditis elegans is modulated by antipsychotic drugs and calmodulin and may serve as a protophenotype for asociality.

Dwyer DS1, Awatramani P2, Thakur R2, Seeni R3, Aamodt EJ4.
Neuropharmacology.Neuropharmacology.2015 May;92:56-62. doi: 10.1016/j.neuropharm.2014.12.027. Epub 2015 Jan 7.
Here, we define a protophenotype as an endophenotype that has been conserved during evolution. Social feeding in Caenorhabditis elegans may be an example of a protophenotype related to asociality in schizophrenia. It is regulated by the highly conserved neuropeptide Y receptor, NPR-1, and we specula
PMID 25576370

Inhibition screening method of microsomal UGTs using the cocktail approach.

Gradinaru J1, Romand S1, Geiser L1, Carrupt PA1, Spaggiari D1, Rudaz S2.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.Eur J Pharm Sci.2015 Apr 25;71:35-45. doi: 10.1016/j.ejps.2015.02.001. Epub 2015 Feb 12.
A rapid method for the simultaneous determination of the in vitro activity of the 10 major human liver UDP-glucuronosyltransferase (UGT) enzymes was developed based on the cocktail approach. Specific substrates were first selected for each UGT: etoposide for UGT1A1, chenodeoxycholic acid for UGT1A3,
PMID 25684194

Cytotoxicity of phenothiazine derivatives associated with mitochondrial dysfunction: A structure-activity investigation.

de Faria PA1, Bettanin F2, Cunha RL3, Paredes-Gamero EJ4, Homem-de-Mello P5, Nantes IL6, Rodrigues T7.
Toxicology.Toxicology.2015 Apr 1;330:44-54. doi: 10.1016/j.tox.2015.02.004. Epub 2015 Feb 14.
Phenothiazine derivatives are neuroleptic drugs used in the treatment of schizophrenia and anxiety. Several side effects are described for these drugs, including hepatotoxicity, which may be related to their cytotoxic activity. Working with isolated rat liver mitochondria, we previously showed that
PMID 25686698

Japanese Journal

Inhibitory Effect of Hesperetin and Naringenin on Human UDP-Glucuronosyltransferase Enzymes: Implications for Herb–Drug Interactions

Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 39(12), 2052-2059, 2016
NAID 130005171490

トリフルオペラジンを用いた臭素酸イオンの蛍光測定法に関する基礎研究

EICA 16(2), 89-92, 2011-10-15
NAID 10029624358

Inhibitory Effect of Chlorpromazine on RANKL-Induced Osteoclastogenesis in Mouse Bone Marrow Cells

Journal of pharmacological sciences 117(1), 54-62, 2011-09-20
NAID 10029895980

Related Pictures

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★リンクテーブル★

リンク元	「フェノチアジン誘導体」「トリフロペラジン」「TFP」
拡張検索	「trifluoperazine maleate」

「フェノチアジン誘導体」

Trifluoperazine
Clinical data
Trade names	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
Biological 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);
ECHA InfoCard	100.003.837
Chemical and physical data
Formula	C21H24F3N3S
Molar mass	407.497 g/mol
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: phenothiazine derivative, phenothiazines
関: フェノチアジン phenothiazine、抗精神病薬

フェノチアジン核/骨格を有する化合物

作用機序

D2受容体拮抗

適応

抗精神病薬：統合失調症、躁病

副作用

錐体外路症状、意識障害、血圧低下(自律神経遮断作用による？)

所属する薬物

抗精神病薬

「トリフロペラジン」

　　[★]

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

「TFP」

　　[★]

トリフロペラジン

関: trifluoperazine、trifluoperazine maleate

「trifluoperazine maleate」

　　[★]

マレイン酸トリフロペラジン

関: TFP、trifluoperazine、trifluoperazine hydrochloride

[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: CD010226.pub2. doi:10.1002/14651858.CD010226.pub2. 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: 293–302. doi:10.1017/S1461145704004870.

[Marq-5] Marques LO, Lima MS, Soares BG (2004). "Trifluoperazine for schizophrenia". Cochrane Database of Systematic Reviews (1): CD003545. doi:10.1002/14651858.CD003545.pub2. PMID 14974020.

[6] 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.

[7] Hedges D, Jeppson K, Whitehead P (July 2003). "Antipsychotic medication and seizures: a review". Drugs of Today (Barcelona, Spain : 1998). 39 (7): 551–7. doi:10.1358/dot.2003.39.7.799445. PMID 12973403.

[8] 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.

[9] 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.

[10] 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.

[11] 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. PMID 9081563. Retrieved 2009-06-21.

[12] 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 Brexpiprazole Cariprazine RP-5063^† 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 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 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

trifluoperazine