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Penfluridol

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Chemical compound
Pharmaceutical compound
Penfluridol
Clinical data
Trade namesSemap
AHFS/Drugs.comInternational Drug Names
ATC code
Legal status
Legal status
Identifiers
  • 1-[4,4-Bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]piperidin-4-ol
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.043.689Edit this at Wikidata
Chemical and physical data
FormulaC28H27ClF5NO
Molar mass523.97 g·mol−1
3D model (JSmol)
  • FC(F)(F)c1c(Cl)ccc(c1)C4(O)CCN(CCCC(c2ccc(F)cc2)c3ccc(F)cc3)CC4
  • InChI=1S/C28H27ClF5NO/c29-26-12-7-21(18-25(26)28(32,33)34)27(36)13-16-35(17-14-27)15-1-2-24(19-3-8-22(30)9-4-19)20-5-10-23(31)11-6-20/h3-12,18,24,36H,1-2,13-17H2 checkY
  • Key:MDLAAYDRRZXJIF-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Penfluridol (Semap,Micefal,Longoperidol) is a highly potent, first generationdiphenylbutylpiperidineantipsychotic.[2] It was discovered atJanssen Pharmaceutica in 1968.[3] Related to other diphenylbutylpiperidine antipsychotics,pimozide andfluspirilene, penfluridol has an extremely long elimination half-life and its effects last for many days after single oral dose. Its antipsychotic potency, in terms of dose needed to produce comparable effects, is similar to bothhaloperidol and pimozide. It is only slightlysedative, but often causesextrapyramidal side-effects, such asakathisia,dyskinesiae and pseudo-Parkinsonism. Penfluridol is indicated for antipsychotic treatment of chronicschizophrenia and similarpsychotic disorders, it is, however, like most typical antipsychotics, being increasingly replaced by theatypical antipsychotics. Due to its extremely long-lasting effects, it is often prescribed to be taken orally as tablets only once a week (q 7 days). The once-weekly dose is usually 10–60 mg. A 2006systematic review examined the use of penfluridol for people with schizophrenia:

Penfluridol compared to typical antipsychotics (oral) for schizophrenia[4]
Summary
Although there are shortcomings and gaps in the data, there appears to be enough overall consistency for different outcomes. Theeffectiveness and adverse effects profile of penfluridol are similar to other typicalantipsychotics; both oral and depot. Furthermore, penfluridol is shown to be an adequate treatment option for people with schizophrenia, especially those who do not respond to oral medication on a daily basis and do not adapt well to depot drugs. One of the results favouring penfluridol was a lower drop out rate in medium term when compared to depot medications. It is also an option for people with long-term schizophrenia with residual psychotic symptoms who nevertheless need continuous use ofantipsychotic medication. An additional benefit of penfluridol is that it is a low-cost intervention.[4]
OutcomeFindings in wordsFindings in numbersQuality of evidence
Global state
No marked improvement (CGI)
Follow-up: 3 to 12 months
Penfluridol does not clearly change the chance of experiencing 'no marked improvement' when compared with receiving typical antipsychotic drugs. These findings are based on data of low quality.RR 0.92 (0.68 to 1.24)Low
Global state - needing additional antipsychotic
Follow-up: less than 3 months
There is no clear difference between people given penfluridol and those receiving typical antipsychotics. These findings are based on data of low quality.RR 1.35 (0.90 to 2.01)Low
Mental state
Average score (BPRS)
Follow-up: 3 to 12 months
On average, people receiving penfluridol scored higher than people treated with typical antipsychotics (oral) but there was no clear difference between the groups and this finding is based on data of low quality. The meaning of this in day-to-day care is unclear.MD 1.24 higher (4.4 lower to 6.88 higher)Low
Adverse events
Needing antiparkinsonism medication
Follow-up: less than 3 months
There is no clear difference between people given penfluridol and those receiving typical antipsychotics (oral). These findings are based on data of low quality.RR 1.09 (0.61 to 1.97)Low
Insomnia
Follow-up: less than 3 months
There is no clear difference between people given penfluridol and those receiving typical antipsychotics (oral). These findings are based on data of low quality.RR 1.07 (0.51 to 2.24)Low
No study reported any data on outcomes such asquality of life and information relating to time in services

See also

[edit]

References

[edit]
  1. ^Anvisa (2023-03-31)."RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese).Diário Oficial da União (published 2023-04-04).Archived from the original on 2023-08-03. Retrieved2023-08-16.
  2. ^van Praag HM, Schut T, Dols L, van Schilfgaarden R (December 1971)."Controlled trial of penfluridol in acute psychosis".British Medical Journal.4 (5789):710–713.doi:10.1136/bmj.4.5789.710.PMC 1799991.PMID 4943034.
  3. ^Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, Van Nueten JM, Schaper WK (July 1970). "The pharmacology of penfluridol (R 16341) a new potent and orally long-acting neuroleptic drug".European Journal of Pharmacology.11 (2):139–154.doi:10.1016/0014-2999(70)90043-9.PMID 5447800.
  4. ^abSoares BG, Lima MS (April 2006)."Penfluridol for schizophrenia".The Cochrane Database of Systematic Reviews.2 (2): CD002923.doi:10.1002/14651858.CD002923.pub2.PMC 11830468.PMID 16625563.

Further reading

[edit]
  • Benkert O, Hippius H (1976).Psychiatrische Pharmakotherapie (2nd ed.). Springer-Verlag.ISBN 3-540-07916-5.
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