WordNet

tranquilizer used to treat psychotic disorders

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/07/22 13:52:23」(JST)

wiki en

Fluphenazine (sold under the brand names Prolixin, Modecate) is a typical antipsychotic drug used for the treatment of chronic psychoses such as schizophrenia.^[2]^[3] It is a phenothiazine with a piperazine side-chain. It works by antagonising (blocking) the dopamine D2 receptors in the brain. This also leads to some of its side effects like movement disorders (like parkinsonism and akathisia) and prolactin elevation. It is given via an intramuscular or subcutaneous depot injection (as its decanoate ester) or by mouth in the form of tablets.^[1] In some countries only the depot formulations are currently available.^[2]^[3] Compared to other antipsychotics it is less prone to causing sedation, low blood pressure or anticholinergic effects but is associated with a higher frequency of movement disorders.^[1]

It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.^[4]

Medical uses

Its primary uses is in the treatment of schizophrenia.^[5] It appears to be about equal in effectiveness to low-potency antipsychotics.^[6]

Adverse effects

Information sources:^[5]^[7]^[8]

Common adverse effects (i.e. those that have an incidence ≥1%) include

Hypotension
Orthostatic hypotension
Somnolence/drowsiness
Weight gain
Erectile dysfunction
Oligomenorrhea or amenorrhea
Anticholinergic effects, such as:

- Dry mouth

- Constipation

- Nasal congestion

- Blurred vision

- Diminished sweating

Extrapyramidal side effects, such as:

- Tremor

- Akathisia

- Muscle rigidity

- Dystonia

- Parkinsonism

Dizziness
Epithelial keratopathy
Eye / vision finding
Retinitis pigmentosa
Photosensitivity

Uncommon side effects (0.1%≤incidence<1%) include

Agitation
Anxiety
Cerebral oedema
Depression
Euphoria
Headache
Ineffective temperature regulation
Restlessness
Weakness
Weight loss
Dyspepsia
Lens opacities (with prolonged use)
Photosensitivity
Pruritus
Diarrhoea
Galactorrhoea
Ejaculatory disorder
QT interval prolongation

Rare (incidence<0.1%) side effects include

Blood dyscrasia (e.g. neutropaenia, agranulocytosis, leukopaenia, etc.)
Seizures
Paralytic ileus
Torsades de Pointes
Heatstroke
Hypothermia
Priapism
Drug-induced Systemic lupus erythematosus
Obstipation
Neuroleptic malignant syndrome
Tardive dyskinesia
Cholestatic jaundice syndrome

Unknown frequency side effects include

Confusion
Decreased gag reflex
Silent pneumonia (likely rare)

References

^ ^a ^b ^c ^d Brayfield, A, ed. (13 December 2013). "Fluphenazine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 14 July 2014.
^ ^a ^b Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. pp. 237, 238. ISBN 978-0-85711-084-8.
^ ^a ^b Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3.
^ "WHO Model List of Essential Medicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
^ ^a ^b "PRODUCT INFORMATION MODECATE (Fluphenazine Decanoate Oily Injection)" (PDF). TGA eBusiness Services. Bristol-Myers Squibb Australia Pty Ltd. 1 November 2012. Retrieved 9 December 2013.
^ Tardy, M; Huhn, M; Engel, RR; Leucht, S (Aug 3, 2014). "Fluphenazine versus low-potency first-generation antipsychotic drugs for schizophrenia.". The Cochrane database of systematic reviews 8: CD009230. doi:10.1002/14651858.CD009230.pub2. PMID 25087165.
^ "FLUPHENAZINE HYDROCHLORIDE tablet, film coated [Sandoz Inc]". DailyMed. Sandoz Inc. October 2011. Retrieved 9 December 2013.
^ "Modecate Concentrate Injection 100mg/ml - Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Sanofi. 11 January 2013. Retrieved 9 December 2013.

"Fluphenazine". Davis's Drug Guide for Nurses, Eighth Edition. F.A. Davis Company, 2005. ISBN 0-8036-2455-7.
Fluphenazine - http://www.minddisorders.com/Flu-Inv/Fluphenazine.html#b#ixzz28etEdxu8 - dose, children, effects, therapy, adults, withdrawal, drug, person

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 統合失調症に対する薬物療法：持効性抗精神病薬注射製剤 pharmacotherapy for schizophrenia long acting injectable antipsychotic drugs
2. 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
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. 統合失調症と物質使用障害の併発に対する治療 treatment of co occurring schizophrenia and substance use disorder
5. 出産後女性における双極性障害：治療 bipolar disorder in postpartum women treatment

English Journal

Phenothiazine-derived antipsychotic drugs inhibit dynamin and clathrin-mediated endocytosis.

Daniel JA1,2, Chau N1, Abdel-Hamid MK3, Hu L4, von Kleist L5, Whiting A1, Krishnan S1, Maamary P1, Joseph SR4, Simpson F4, Haucke V5, McCluskey A3, Robinson PJ1.
Traffic (Copenhagen, Denmark).Traffic.2015 Jun;16(6):635-54. doi: 10.1111/tra.12272. Epub 2015 Apr 9.
Chlorpromazine is a phenothiazine-derived antipsychotic drug (APD) that inhibits clathrin-mediated endocytosis (CME) in cells by an unknown mechanism. We examined whether its action and that of other APDs might be mediated by the GTPase activity of dynamin. Eight of eight phenothiazine-derived APDs
PMID 25693808

Fluphenazine.HCl and epigallocatechin gallate modulate the rate of formation and structural properties of apolipoprotein C-II amyloid fibrils.

Zlatic CO, Mao Y, Ryan TM, Mok YF, Roberts BR, Howlett GJ, Griffin MD.
Biochemistry.Biochemistry.2015 May 29. [Epub ahead of print]
Protein misfolding and aggregation, leading to amyloid fibril formation, are characteristic of many devastating and debilitating amyloid diseases. Accordingly, there is significant interest in the mechanisms underlying amyloid fibril formation and identification of possible intervention tools. Small
PMID 26021642

Dose escalation of antipsychotic drugs in schizophrenia: A meta-analysis of randomized controlled trials.

Dold M1, Fugger G1, Aigner M2, Lanzenberger R1, Kasper S3.
Schizophrenia research.Schizophr Res.2015 May 22. pii: S0920-9964(15)00219-4. doi: 10.1016/j.schres.2015.04.024. [Epub ahead of print]
BACKGROUND: Non-response to an initial antipsychotic trial emerges frequently in the pharmacological management of schizophrenia. Increasing the dose (high-dose treatment, dose escalation) is an often applied strategy in this regard, but there are currently no meta-analytic data available to ascerta
PMID 26008883

Japanese Journal

Comparison of Cytochrome P450 Mediated Metabolism of Three Central Nervous System Acting Drugs

Attia Tamer Zekry,Yamashita Taku,Miyamoto Masayoshi [他]
Chemical and pharmaceutical bulletin 60(12), 1544-1549, 2012-12
NAID 40019497219

Comparison of Cytochrome P450 Mediated Metabolism of Three CNS Acting Drugs

Zekry Attia Tamer,Yamashita Taku,Miyamoto Masayoshi,Koizumi Atsushi,Yasuhara Yuki,Node Jun-ichi,Erikawa Yumi,Komiyama Yumi,Horii Chiaki,Yamada Mayu,Ahmed Omar Mahmoud,Hassan Abdelmageed Osama,Mohamed Derayea Sayed,Uno Tadayuki
Chemical and Pharmaceutical Bulletin 2012(0), 2012
… In this study, the metabolic activities of three major hepatic CYP isoforms (2C19, 2D6, and 3A4) were investigated on structurally different central nervous system (CNS) acting drugs, amitriptyline, fluphenazine, and dothiepin. … By using our novel in vitro evaluation system, we could compare the kinetic parameters for the metabolism of fluphenazine and dothiepin for the first time. …
NAID 130001852550

Simple and simultaneous determination for twelve phenothiazines in human serum by reversed-phase high-performance liquid chromatography

TANAKA Einosuke,NAKAMURA Takako,TERADA Masaru,SHINOZUKA Tatsuo,HASHIMOTO Chikako,KURIHARA Katsuyoshi,HONDA Katsuya
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 854(1), 116-120, 2007-07-01
… A high-performance liquid chromatographic method has been developed for the simultaneous analysis of the 12 phenothiazines (chlorpromazine, fluphenazine, levomepromazine, perazine, perphenazine, prochlorperazine, profenamine, promethazine, propericiazine, thioproperazine, thioridazine and trifluoperazine) in human serum using HPLC/UV. …
NAID 10025805017

Related Pictures

Fluphenazine; Flufenazin Fluphenazine Decanoate, 25mg/mL, MDV, 5mL Vial | McGuff Medical Products Fluphenazine Decanoate - patient information, description, dosage and directions. Fluphenazine | Bad Drug Fluphenazine Decanoate Injection : Uses, Side Effects, Interactions, Pictures

★リンクテーブル★

リンク元	「フェノチアジン誘導体」「フルフェナジン」
拡張検索	「fluphenazine maleate」

「フェノチアジン誘導体」

Fluphenazine
Systematic (IUPAC) name
	2-[4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]piperazin-1-yl]ethanol
Clinical data
Trade names	Prolixin, Modecate
AHFS/Drugs.com	monograph
MedlinePlus	a682172
Pregnancy; category	AU: C; US: C (Risk not ruled out);
Legal status	AU: Prescription Only (S4); CA: ℞-only; UK: Prescription-only (POM); US: ℞-only;
Routes of; administration	oral, IM, decanoate
Pharmacokinetic data
Bioavailability	2.7% (Oral)
Metabolism	Hepatic (via CYP2D6)
Biological half-life	14.7 hours, 6-9 days (decanoate)
Excretion	Urine, faeces
Identifiers
CAS Registry Number	69-23-8
ATC code	N05AB02
PubChem	CID: 3372
IUPHAR/BPS	204
DrugBank	DB00623
ChemSpider	3255
UNII	S79426A41Z
KEGG	D07977
ChEBI	CHEBI:5123
ChEMBL	CHEMBL726
Chemical data
Formula	C22H26F3N3OS
Molecular mass	437.523 g/mol
	SMILES FC(F)(F)c2cc1N(c3c(Sc1cc2)cccc3)CCCN4CCN(CCO)CC4 ;
	InChI InChI=1S/C22H26F3N3OS/c23-22(24,25)17-6-7-21-19(16-17)28(18-4-1-2-5-20(18)30-21)9-3-8-26-10-12-27(13-11-26)14-15-29/h1-2,4-7,16,29H,3,8-15H2 ; Key:PLDUPXSUYLZYBN-UHFFFAOYSA-N ;
(what is this?) (verify)