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Fluspirilene

From Wikipedia, the free encyclopedia
Typical antipsychotic medication
Pharmaceutical compound
Fluspirilene
Clinical data
Trade namesImap
AHFS/Drugs.comInternational Drug Names
Routes of
administration		IM
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • 8-[4,4-Bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.015.835Edit this at Wikidata
Chemical and physical data
FormulaC29H31F2N3O
Molar mass475.584 g·mol−1
3D model (JSmol)
  • Fc1ccc(cc1)C(c2ccc(F)cc2)CCCN5CCC4(C(=O)NCN4c3ccccc3)CC5
  • 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) checkY
  • Key:QOYHHIBFXOOADH-UHFFFAOYSA-N checkY
  (verify)

Fluspirilene (Redeptin,Imap, R6218) is adiphenylbutylpiperidinetypical antipsychoticdrug, used for the treatment ofschizophrenia.[1] It is administeredintramuscularly.[2] It was discovered atJanssen Pharmaceutica in 1963.[3] A 2007systematic 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]
OutcomeFindings in wordsFindings in numbersQuality 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
DizzinessFluspirilene 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.
Pharmacokinetics of long-acting injectable antipsychotics
MedicationBrand nameClassVehicleDosageTmaxt1/2 singlet1/2 multiplelogPcRef
Aripiprazole lauroxilAristadaAtypicalWatera441–1064 mg/4–8 weeks24–35 days?54–57 days7.9–10.0
Aripiprazole monohydrateAbilify MaintenaAtypicalWatera300–400 mg/4 weeks7 days?30–47 days4.9–5.2
Bromperidol decanoateImpromen DecanoasTypicalSesame oil40–300 mg/4 weeks3–9 days?21–25 days7.9[5]
Clopentixol decanoateSordinol DepotTypicalViscoleob50–600 mg/1–4 weeks4–7 days?19 days9.0[6]
Flupentixol decanoateDepixolTypicalViscoleob10–200 mg/2–4 weeks4–10 days8 days17 days7.2–9.2[6][7]
Fluphenazine decanoateProlixin DecanoateTypicalSesame oil12.5–100 mg/2–5 weeks1–2 days1–10 days14–100 days7.2–9.0[8][9][10]
Fluphenazine enanthateProlixin EnanthateTypicalSesame oil12.5–100 mg/1–4 weeks2–3 days4 days?6.4–7.4[9]
FluspirileneImap, RedeptinTypicalWatera2–12 mg/1 week1–8 days7 days?5.2–5.8[11]
Haloperidol decanoateHaldol DecanoateTypicalSesame oil20–400 mg/2–4 weeks3–9 days18–21 days7.2–7.9[12][13]
Olanzapine pamoateZyprexa RelprevvAtypicalWatera150–405 mg/2–4 weeks7 days?30 days–
Oxyprothepin decanoateMeclopinTypical?????8.5–8.7
Paliperidone palmitateInvega SustennaAtypicalWatera39–819 mg/4–12 weeks13–33 days25–139 days?8.1–10.1
Perphenazine decanoateTrilafon DekanoatTypicalSesame oil50–200 mg/2–4 weeks??27 days8.9
Perphenazine enanthateTrilafon EnanthateTypicalSesame oil25–200 mg/2 weeks2–3 days?4–7 days6.4–7.2[14]
Pipotiazine palmitatePiportil LongumTypicalViscoleob25–400 mg/4 weeks9–10 days?14–21 days8.5–11.6[7]
Pipotiazine undecylenatePiportil MediumTypicalSesame oil100–200 mg/2 weeks???8.4
RisperidoneRisperdal ConstaAtypicalMicrospheres12.5–75 mg/2 weeks21 days?3–6 days–
Zuclopentixol acetateClopixol AcuphaseTypicalViscoleob50–200 mg/1–3 days1–2 days1–2 days4.7–4.9
Zuclopentixol decanoateClopixol DepotTypicalViscoleob50–800 mg/2–4 weeks4–9 days?11–21 days7.5–9.0
Note: All byintramuscular injection.Footnotes:a =Microcrystalline ornanocrystallineaqueous suspension.b = Low-viscosityvegetable oil (specificallyfractionated coconut oil withmedium-chain triglycerides).c = Predicted, fromPubChem andDrugBank.Sources:Main: See template.

See also

[edit]

References

[edit]
  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.
  3. ^BE 633914, issued 1963, assigned to C. Janssen, NV Res. Lab. 
  4. ^abAbhijnhan A, Adams CE, David A, Ozbilen M (January 2007)."Depot fluspirilene for schizophrenia".The Cochrane Database of Systematic Reviews.2007 (1): CD001718.doi:10.1002/14651858.CD001718.pub2.PMC 7025783.PMID 17253464.
  5. ^Parent M, Toussaint C, Gilson H (1983). "Long-term treatment of chronic psychotics with bromperidol decanoate: clinical and pharmacokinetic evaluation".Current Therapeutic Research.34 (1):1–6.
  6. ^abJørgensen A, Overø KF (1980). "Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. III. Serum levels".Acta Psychiatrica Scandinavica. Supplementum.279:41–54.doi:10.1111/j.1600-0447.1980.tb07082.x.PMID 6931472.
  7. ^abReynolds JE (1993). "Anxiolytic sedatives, hypnotics and neuroleptics.".Martindale: The Extra Pharmacopoeia (30th ed.). London: Pharmaceutical Press. pp. 364–623.
  8. ^Ereshefsky L, Saklad SR, Jann MW, Davis CM, Richards A, Seidel DR (May 1984). "Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches".The Journal of Clinical Psychiatry.45 (5 Pt 2):50–9.PMID 6143748.
  9. ^abCurry SH, Whelpton R, de Schepper PJ, Vranckx S, Schiff AA (April 1979)."Kinetics of fluphenazine after fluphenazine dihydrochloride, enanthate and decanoate administration to man".British Journal of Clinical Pharmacology.7 (4):325–31.doi:10.1111/j.1365-2125.1979.tb00941.x.PMC 1429660.PMID 444352.
  10. ^Young D, Ereshefsky L, Saklad SR, Jann MW, Garcia N (1984).Explaining the pharmacokinetics of fluphenazine through computer simulations. (Abstract.). 19th Annual Midyear Clinical Meeting of the American Society of Hospital Pharmacists. Dallas, Texas.
  11. ^Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, van Nueten JM, Marsboom RH, Hérin VV, Schaper WK (November 1970). "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug".Arzneimittel-Forschung.20 (11):1689–98.PMID 4992598.
  12. ^Beresford R, Ward A (January 1987). "Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis".Drugs.33 (1):31–49.doi:10.2165/00003495-198733010-00002.PMID 3545764.
  13. ^Reyntigens AJ, Heykants JJ, Woestenborghs RJ, Gelders YG, Aerts TJ (1982). "Pharmacokinetics of haloperidol decanoate. A 2-year follow-up".International Pharmacopsychiatry.17 (4):238–46.doi:10.1159/000468580.PMID 7185768.
  14. ^Larsson M, Axelsson R, Forsman A (1984). "On the pharmacokinetics of perphenazine: a clinical study of perphenazine enanthate and decanoate".Current Therapeutic Research.36 (6):1071–88.
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