Penfluridol

Chemical compound
  • N05AG03 (WHO)
Legal statusLegal status
Identifiers
  • 1-[4,4-Bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]piperidin-4-ol
CAS Number
  • 26864-56-2 ☒N
PubChem CID
  • 33630
ChemSpider
  • 31017 checkY
UNII
  • 25TLU22Q8H
KEGG
  • D02630 checkY
ChEMBL
  • ChEMBL47050 checkY
CompTox Dashboard (EPA)
  • DTXSID5049021 Edit this at Wikidata
ECHA InfoCard100.043.689 Edit this at WikidataChemical and physical dataFormulaC28H27ClF5NOMolar mass523.97 g·mol−13D model (JSmol)
  • Interactive image
  • FC(F)(F)c1c(Cl)ccc(c1)C4(O)CCN(CCCC(c2ccc(F)cc2)c3ccc(F)cc3)CC4
InChI
  • 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 generation diphenylbutylpiperidine antipsychotic.[2] It was discovered at Janssen Pharmaceutica in 1968.[3] Related to other diphenylbutylpiperidine antipsychotics, pimozide and fluspirilene, 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 both haloperidol and pimozide. It is only slightly sedative, but often causes extrapyramidal side-effects, such as akathisia, dyskinesiae and pseudo-Parkinsonism. Penfluridol is indicated for antipsychotic treatment of chronic schizophrenia and similar psychotic disorders, it is, however, like most typical antipsychotics, being increasingly replaced by the atypical 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 2006 systematic 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. The effectiveness and adverse effects profile of penfluridol are similar to other typical antipsychotics; 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 of antipsychotic medication. An additional benefit of penfluridol is that it is a low-cost intervention.[4]
Outcome Findings in words Findings in numbers Quality 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 as quality of life and information relating to time in services

See also

References

  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. Retrieved 2023-08-16.
  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. ^ a b Soares BG, Lima MS (April 2006). "Penfluridol for schizophrenia". The Cochrane Database of Systematic Reviews. 2 (2): CD002923. doi:10.1002/14651858.CD002923.pub2. PMID 16625563.

Further reading

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