Penfluridol

Penfluridol

drugbox
IUPAC_name = 1- [4,4-bis(4-fluorophenyl)butyl] -4- [4-chloro-3-(trifluoromethyl)phenyl] piperidin-4-ol



CAS_number = 26864-56-2
ATC_prefix = N05
ATC_suffix = AG03
PubChem = 33630
DrugBank =
C=28 | H=27 | Cl=1 | F=5 | N=1 | O=1
molecular_weight = 523.965
bioavailability =
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Penfluridol (Semap, Micefal) is a highly potent, first generation diphenylbutylpiperidine antipsychotic. It was discovered at Janssen Pharmaceutica in 1968. 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 dosis is usually 10 — 60 mg.

References

* Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, Van Nueten JM, Schaper WK., The pharmacology of penfluridol (R 16341) a new potent and orally long-acting neuroleptic drug, Eur J Pharmacol. 1970 Jul 15;11(2):139-54.
* van Praag HM, Schut T, Dols L, van Schilfgaarden R., Controlled trial of penfluridol in acute psychosis, Br Med J. 1971 Dec 18;4(5789):710-3.
* Benkert O, Hippius H.: Psychiatrische Pharmakotherapie, Springer-Verlag, 1976, 2. Auflage. ISBN 3-540-07916-5


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