Fluspirilene

Fluspirilene
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	IM
ATC code	N05AG01 (WHO) ;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name 8-[4,4-Bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one;
CAS Number	1841-19-6 ;
PubChem CID	3396;
IUPHAR/BPS	85;
DrugBank	DB04842 ;
ChemSpider	3279 ;
UNII	C5QA4GLR9M;
KEGG	D02629 ;
ChEMBL	ChEMBL46516 ;
CompTox Dashboard (EPA)	DTXSID7045152 ;
ECHA InfoCard	100.015.835
Chemical and physical data
Formula	C29H31F2N3O
Molar mass	475.573 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Fc1ccc(cc1)C(c2ccc(F)cc2)CCCN5CCC4(C(=O)NCN4c3ccccc3)CC5;
	InChI InChI=1S/C29H31F2N3O/c30-24-12-8-22(9-13-24)27(23-10-14-25(31)15-11-23)7-4-18-33-19-16-29(17-20-33)28(35)32-21-34(29)26-5-2-1-3-6-26/h1-3,5-6,8-15,27H,4,7,16-21H2,(H,32,35) ; Key:QOYHHIBFXOOADH-UHFFFAOYSA-N ;
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Fluspirilene (Redeptin, Imap, R6218) is a diphenylbutylpiperidine typical antipsychotic drug, used for the treatment of schizophrenia.[1] It is administered intramuscularly.[2] It was discovered at Janssen Pharmaceutica in 1963.[3] A 2007 systematic review investigated the efficacy of fluspirilene decanoate for people with schizophrenia:

Fluspirilene decanoate compared to oral antipsychotics[4]

Summary

Participant numbers in each comparison were small so power to identify clear difference is limited. Randomized controlled trial data identified no clear differences between the long-acting injection of fluspirilene and oral medication for outcomes that include adverse effects.[4]

Outcome	Findings in words	Findings in numbers	Quality of evidence
Global outcome
Leaving the study early Follow up: 6 weeks to 5 months	Fluspirilene decanoate may increase the risk of leaving the study (reasons not specified), but, the difference is not clear between people given fluspirilene decanoate and those receiving oral antipsychotics. These findings are based on data of low quality.	RR 1.18 (0.08 to 16.78)	Low
Mental state
Relapse Follow up: 6 weeks to 5 months	Using the depot, long-acting fluspirilene decanoate makes little difference for the outcome of 'relapse' compared with those receiving oral antipsychotics - at least for those willing to be engaged with trials. These findings are based on data of low quality.	RR 1.18 (0.08 to 16.78)	Low
Adverse effects
Needing anticholinergic drugs Follow up: 6 weeks to 5 months	The depot fluspirilene decanoate does not seem to cause any more movement disorders - for which anticholinergic drugs are used - compared with oral antipsychotics. These findings are based on data of low quality.	RR 0.07 (0.00 to 1.07)	Low
Dizziness	Fluspirilene decanoate may reduce the chance of experiencing dizziness compared with the oral antipsycotics. Data are based on low quality evidence.	RR 0.59 (0.37 to 0.95)	Low
Missing outcomes
	Data on quality of life, and service use (e.g. hospitalization) were not reported in trials.

References

van Epen JH (1970). "Experience with fluspirilene (R 6218), a long-acting neuroleptic". Psychiatr Neurol Neurochir. 73 (4): 277–284. PMID 5478771.
Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, van Nueten JM, Marsboom RH, Hérin VV, Schaper WK (1970). "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittelforschung. 20 (11): 1689–1698. PMID 4992598.
C. Janssen, NV Res. Lab., BE 633914 (1963)
Abhijnhan, A; Adams, C; David, A (2007). "Depot fluspirilene for schizophrenia". Cochrane Database of Systematic Reviews. 1: CD001718.pub2. doi:10.1002/14651858.CD001718.pub2.

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[1] van Epen JH (1970). "Experience with fluspirilene (R 6218), a long-acting neuroleptic". Psychiatr Neurol Neurochir. 73 (4): 277–284. PMID 5478771.

[2] Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, van Nueten JM, Marsboom RH, Hérin VV, Schaper WK (1970). "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittelforschung. 20 (11): 1689–1698. PMID 4992598.

[Janssen-3] C. Janssen, NV Res. Lab., BE 633914 (1963)

[Abh2007-4] Abhijnhan, A; Adams, C; David, A (2007). "Depot fluspirilene for schizophrenia". Cochrane Database of Systematic Reviews. 1: CD001718.pub2. doi:10.1002/14651858.CD001718.pub2.

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

Histamine receptor modulators
H₁	Agonists: 2-Pyridylethylamine Betahistine Histamine HTMT L-Histidine UR-AK49 Antagonists: First-generation: 4-Methyldiphenhydramine Alimemazine Antazoline Azatadine Bamipine Benzatropine (benztropine) Bepotastine Bromazine Brompheniramine Buclizine Captodiame Carbinoxamine Chlorcyclizine Chloropyramine Chlorothen Chlorphenamine Chlorphenoxamine Cinnarizine Clemastine Clobenzepam Clocinizine Cloperastine Cyclizine Cyproheptadine Dacemazine Decloxizine Deptropine Dexbrompheniramine Dexchlorpheniramine Dimenhydrinate Dimetindene Diphenhydramine Diphenylpyraline Doxylamine Embramine Etodroxizine Etybenzatropine (ethylbenztropine) Etymemazine Fenethazine Flunarizine Histapyrrodine Homochlorcyclizine Hydroxyethylpromethazine Hydroxyzine Isopromethazine Isothipendyl Meclozine Medrylamine Mepyramine (pyrilamine) Mequitazine Methafurylene Methapyrilene Methdilazine Moxastine Orphenadrine Oxatomide Oxomemazine Perlapine Phenindamine Pheniramine Phenyltoloxamine Pimethixene Piperoxan Pipoxizine Promethazine Propiomazine Pyrrobutamine Talastine Thenalidine Thenyldiamine Thiazinamium Thonzylamine Tolpropamine Tripelennamine Triprolidine Second/third-generation: Acrivastine Alinastine Astemizole Azelastine Bamirastine Barmastine Bepiastine Bepotastine Bilastine Cabastinen Carebastine Cetirizine Clemastine Clemizole Clobenztropine Desloratadine Dorastine Ebastine Efletirizine Emedastine Epinastine Fexofenadine Flezelastine Ketotifen Latrepirdine Levocabastine Levocetirizine Linetastine Loratadine Mapinastine Mebhydrolin Mizolastine Moxastine Noberastine Octastine Olopatadine Perastine Pibaxizine Piclopastine Quifenadine (phencarol) Rocastine Rupatadine Setastine Sequifenadine (bicarphen) Talastine Temelastine Terfenadine Vapitadine Zepastine Others: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, brilaroxazine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, zotepine) Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione) Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline) Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine) Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene) Unknown/unsorted: Azanator Belarizine Elbanizine Flotrenizine GSK1004723 Napactadine Tagorizine Trelnarizine Trenizine
H₂	Agonists: Amthamine Betazole Dimaprit Histamine HTMT Impromidine L-Histidine UR-AK49 Antagonists: Bisfentidine Burimamide Cimetidine Dalcotidine Donetidine Ebrotidine Etintidine Famotidine Isolamtidine Lafutidine Lamtidine Lavoltidine (loxtidine) Lupitidine Metiamide Mifentidine Niperotidine Nizatidine Osutidine Oxmetidine Pibutidine Quisultazine (quisultidine) Ramixotidine Ranitidine Roxatidine Sufotidine Tiotidine Tuvatidine Venritidine Xaltidine Zolantidine
H₃	Agonists: α-Methylhistamine Cipralisant Histamine Imetit Immepip Immethridine L-Histidine Methimepip Proxyfan Antagonists: A-349,821 A-423,579 ABT-239 ABT-652 AZD5213 Bavisant Betahistine Burimamide Ciproxifan Clobenpropit Conessine Enerisant GSK-189,254 Impentamine Iodophenpropit Irdabisant JNJ-5207852 NNC 38-1049 PF-03654746 Pitolisant SCH-79687 Thioperamide VUF-5681
H₄	Agonists: 4-Methylhistamine α-Methylhistamine Histamine L-Histidine OUP-16 VUF-8430 Antagonists: JNJ-7777120 Mianserin Seliforant Thioperamide Toreforant VUF-6002
See also: Receptor/signaling modulators • Monoamine metabolism modulators • Monoamine reuptake inhibitors

Fluspirilene

See also

References