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Chemical Compound Review

PENFLURIDOL     1-[4,4-bis(4- fluorophenyl)butyl]-4-[4...

Synonyms: Micefal, Semap, Hydroxamates, Penfluridolum, PubChem15873, ...
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Disease relevance of PENFLURIDOL

  • Penfluridol patients had statistically fewer psychotic relapses [1].
  • The low incidence of side effects and other signs of toxicity, coupled with an effective prophylactic activity, suggests that penfluridol is an important addition to our therapeutic armamentarium for the treatment of chronic schizophrenia [2].
  • Although resting PRL levels were evaluated during initial penfluridol therapy (week 1), hypoglycemia provoked a further substantial PRL increment, not significantly different in magnitude from that induced by hypoglycemia during the drug-free period [3].
  • A case of neuroleptic malignant syndrome (NMS) is discussed which occurred in a 72-year-old paranoid psychotic patient while on maintainance neuroleptic therapy with penfluridol [4].
  • In rabbits tested for apomorphine-induced hyperthermia and gnawing, on the other hand, penfluridol blocks apomorphine for about a week [5].

Psychiatry related information on PENFLURIDOL


High impact information on PENFLURIDOL


Chemical compound and disease context of PENFLURIDOL


Biological context of PENFLURIDOL


Anatomical context of PENFLURIDOL


Associations of PENFLURIDOL with other chemical compounds

  • A long term comparative trial of penfluridol and fluphenazine decanoate in schizophrenic outpatients [24].
  • Penfluridol, a compound with Ca2+-calmodulin-blocking properties, decreased control and A23187-stimulated cAMP content and PRL release [25].
  • The coincubation of varying concentrations of penfluridol with 70 nM TRH, 50 mM K+, 3 mM (Bu)2cAMP, or 5 mM theophylline resulted in a dose-related inhibition of secretagogue-stimulated PRL secretion [26].
  • Trifluoperazine and penfluridol were found to antagonize all the above mentioned types of activation of Ca2+-transport ATPase in the same concentration range [27].
  • Furthermore, the penfluridol-induced increase of striatal DOPAC was more susceptible to reversal by apomorphine than was the increase of serum prolactin concentrations [28].

Gene context of PENFLURIDOL

  • Inhibiting cAMP-dependent calmodulin with penfluridol had no effect on the initial spike phase, but reduced the sustained plateau phase of the response to AVP [29].
  • In contrast cobalt, a calcium channel blocker, penfluridol, a calcium-binding protein inhibitor, and low-calcium medium decreased basal and TRH-induced prolactin release and diminished the TRH-induced release of arachidonate [30].
  • The site of action of penfluridol may occur after calcium mobilization, with calmodulin a possible target for penfluridol's inhibitory action on PRL secretion [26].
  • Preperifusion of the cells with 5 microM penfluridol, a calmodulin inhibitor, reduced CRF- and 8-Br-cAMP-induced ACTH release by 54% and 41%, respectively [31].
  • In general, for the efficacy and safety measures, no differences were established, but penfluridol was superior in keeping the patients in treatment; 'leaving the study early' (n=218, 5RCTs, RR 0.55 CI 0.3 to 0.97, NNT 6 CI 3.4 to 50) [32].

Analytical, diagnostic and therapeutic context of PENFLURIDOL


  1. Long-acting oral vs injectable antipsychotic drugs in schizophrenics: a one-year double-blind comparison in multiple episode schizophrenics. Quitkin, F., Rifkin, A., Kane, J., Ramos-Lorenzi, J.R., Klein, D.F. Arch. Gen. Psychiatry (1978) [Pubmed]
  2. A controlled study of penfluridol in the treatment of chronic schizophrenia. Lapierre, Y.D. The American journal of psychiatry. (1978) [Pubmed]
  3. Failure of dopaminergic blockade to affect prolactin, growth hormone, and cortisol responses to insulin-induced hypoglycemia in schizophrenics. Nathan, R.S., Sachar, E.J., Ostrow, L., Asnis, G.M., Halbreich, U., Halpern, F.S. J. Clin. Endocrinol. Metab. (1981) [Pubmed]
  4. Treatment of neuroleptic malignant syndrome with dopamine hydrochloride: a case report. Ungvari, G.A. Pharmacopsychiatry (1987) [Pubmed]
  5. Penfluridol blockade of apomorphine: dependence of duration on species and endpoint. Weissman, A. Eur. J. Pharmacol. (1975) [Pubmed]
  6. A twelve month comparison of penfluridol and trifluoperazine in chronic schizophrenic outpatients. Donlon, P.T., Meyer, J.E. The Journal of clinical psychiatry. (1978) [Pubmed]
  7. The effect of long-term penfluridol treatment on the sensitivity of the dopamine receptors in the nucleus accumbens and in the corpus striatum. Jackson, D.M., Andén, N.E., Engel, J., Liljequist, S. Psychopharmacologia. (1975) [Pubmed]
  8. Penfluridol: an open phase III study in acute newly admitted hospitalized schizophrenic patients. Shopsin, B., Klein, H., Gerbino, L., Selzer, G. Psychopharmacology (Berl.) (1977) [Pubmed]
  9. Changes in psychopathology in relation to EEG variables and visual averaged evoked responses (V.AER) in schizophrenic patients treated with penfluridol or thiothixene. d'Elia, G., Jacobsson, L., von Knorring, L., Mattsson, B., Mjörndal, T., Oreland, L., Perris, C., Rapp, W. Acta psychiatrica Scandinavica. (1977) [Pubmed]
  10. Effects of penfluridol and other drugs on apomorphine-induced stereotyped behavior in monkeys. Shintomi, K., Yamamura, M. Eur. J. Pharmacol. (1975) [Pubmed]
  11. Plasma prolactin and testosterone during penfluridol treatment. Rubin, R.T. Lancet (1980) [Pubmed]
  12. Plasma prolactin and testosterone during penfluridol treatment. Nathan, R.S., Asnis, G.M., Dyrenfurth, I., Halpern, F.S., Halbreich, U., Ostrow, L.C., Sachar, E.J. Lancet (1980) [Pubmed]
  13. Neuroleptic drugs attenuate calcium influx and tension development in rabbit thoracic aorta: effects of pimozide, penfluridol, chlorpromazine, and haloperidol. Flaim, S.F., Brannan, M.D., Swigart, S.C., Gleason, M.M., Muschek, L.D. Proc. Natl. Acad. Sci. U.S.A. (1985) [Pubmed]
  14. Release of Ca(2+) from intracellular stores and entry of extracellular Ca(2+) are involved in sea squirt sperm activation. Butler, D.M., Allen, K.M., Garrett, F.E., Lauzon, L.L., Lotfizadeh, A., Koch, R.A. Dev. Biol. (1999) [Pubmed]
  15. Preferential block of T-type calcium channels by neuroleptics in neural crest-derived rat and human C cell lines. Enyeart, J.J., Biagi, B.A., Mlinar, B. Mol. Pharmacol. (1992) [Pubmed]
  16. Neuroleptic malignant syndrome due to combination of penfluridol and sulpiride? Lühdorf, K., Kruse, A., Schulz, V. Acta psychiatrica Scandinavica. (1987) [Pubmed]
  17. Penfluridol steady-state kinetics in psychiatric patients. Cooper, S.F., Dugal, R., Albert, J.M., Bertrand, M. Clin. Pharmacol. Ther. (1975) [Pubmed]
  18. A molecular modeling study on binding of drugs to calmodulin. Höltje, H.D., Hense, M. J. Comput. Aided Mol. Des. (1989) [Pubmed]
  19. The comparative metabolism and disposition of penfluridol-3H in the rat, rabbit, dog, and man. Grindel, J.M., Migdalof, B.H., Cressman, W.A. Drug Metab. Dispos. (1979) [Pubmed]
  20. Dual pharmacological properties of a cyclic AMP-sensitive potassium channel. Gomora, J.C., Enyeart, J.J. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  21. Penfluridol: a neuroleptic drug designed for long duration of action. Migdalof, B.H., Grindel, J.M., Heykants, J.J., Janssen, P.A. Drug Metab. Rev. (1979) [Pubmed]
  22. Effects of the neuroprotectant lubeluzole on the cytotoxic actions of veratridine, barium, ouabain and 6-hydroxydopamine in chromaffin cells. Cano-Abad, M.F., López, M.G., Hernández-Guijo, J.M., Zapater, P., Gandía, L., Sánchez-García, P., García, A.G. Br. J. Pharmacol. (1998) [Pubmed]
  23. The effect of penfluridol and some psychotropic drugs on monoamine metabolism in central nervous system. Nose, T., Takemoto, H. Eur. J. Pharmacol. (1975) [Pubmed]
  24. A long term comparative trial of penfluridol and fluphenazine decanoate in schizophrenic outpatients. Iqbal, M.J., Young, M.A., Charles, J., Elgart, B., Von Greiff, H., Simpson, G.M. The Journal of clinical psychiatry. (1978) [Pubmed]
  25. Adenosine 3',5'-monophosphate (cAMP) and calcium-calmodulin interrelation in the control of prolactin secretion: evidence for dopamine inhibition of cAMP accumulation and prolactin release after calcium mobilization. Schettini, G., Cronin, M.J., MacLeod, R.M. Endocrinology (1983) [Pubmed]
  26. In vitro studies on basal and stimulated prolactin release by rat anterior pituitary: a possible role for calmodulin. Schettini, G., Judd, A.M., MacLeod, R.M. Endocrinology (1983) [Pubmed]
  27. A model for the regulation of the calmodulin-dependent enzymes erythrocyte Ca2+-transport ATPase and brain phosphodiesterase by activators and inhibitors. Gietzen, K., Sadorf, I., Bader, H. Biochem. J. (1982) [Pubmed]
  28. Comparative effects of penfluridol on circling behavior and striatal DOPAC and serum prolactin concentrations in the rat. Annunziato, L.A., Wuerthele, S.M., Moore, K.E. Eur. J. Pharmacol. (1978) [Pubmed]
  29. Roles of intracellular and extracellular calcium in the kinetic profile of adrenocorticotropin secretion by perifused rat anterior pituitary cells. II. Arginine vasopressin, oxytocin, and angiotensin-II stimulation. Won, J.G., Oki, Y., Orth, D.N. Endocrinology (1990) [Pubmed]
  30. A possible role of arachidonate metabolism in the mechanism of prolactin release. Judd, A.M., Koike, K., MacLeod, R.M. Am. J. Physiol. (1986) [Pubmed]
  31. Roles of intracellular and extracellular calcium in the kinetic profile of adrenocorticotropin secretion by perifused rat anterior pituitary cells. I. Corticotropin-releasing factor stimulation. Won, J.G., Orth, D.N. Endocrinology (1990) [Pubmed]
  32. Penfluridol for schizophrenia. Soares Bg, O., Lima, M. Cochrane database of systematic reviews (Online) (2006) [Pubmed]
  33. Study of penfluridol and chlorpromazine in the treatment of chronic schizophrenia. Wang, R.I., Larson, C., Treul, S.J. Journal of clinical pharmacology. (1982) [Pubmed]
  34. Peroral and parenteral administration of long-acting neuroleptics: a double-blind study of penfluridol compared to flupenthixol decanoate in the treatment of schizophrenia. Gerlach, J., Kramp, P., Kristjansen, P., Lauritsen, B., Lühdorf, K., Munkvad, I. Acta psychiatrica Scandinavica. (1975) [Pubmed]
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