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Use of Pipamperone and a D2-Receptor Antagonist Or (19) & (11) EP 1 708 790 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/4545 (2006.01) A61K 31/00 (2006.01) 21.04.2010 Bulletin 2010/16 A61K 31/519 (2006.01) A61K 31/343 (2006.01) A61P 25/18 (2006.01) (21) Application number: 04801138.1 (86) International application number: (22) Date of filing: 02.12.2004 PCT/BE2004/000172 (87) International publication number: WO 2005/053796 (16.06.2005 Gazette 2005/24) (54) USE OF PIPAMPERONE AND A D2-RECEPTOR ANTAGONIST OR A SEROTONIN/DOPAMIN ANTAGONIST FOR THE TREATMENT OF PSYCHOTIC DISORDERS VERWENDUNG VON PIPAMPERON UND EINEM D2-REZEPTOR ANTAGONISTEN ODER EINEM SEROTONIN/DOPAMIN ANTAGONISTEN ZUR BEHANDLUNG VON PSYCHOTISCHEN STÖRUNGEN UTILISATION DE PIPAMPERONE ET D’UN ANTAGONISTE DES RECEPTEURS D2 OU D’UN ANTAGONISTE A LA DOPAMINE ET A LA SEROTONINE POUR LE TRAITEMENT DE TROUBLES PSYCHOTIQUES (84) Designated Contracting States: (74) Representative: De Clercq, Ann G. Y. et al AT BE BG CH CY CZ DE DK EE ES FI FR GB GR De Clercq, Brants & Partners c.v. HU IE IS IT LI LT LU MC NL PL PT RO SE SI SK TR Edgard Gevaertdreef 10a Designated Extension States: 9830 Sint-Martens-Latem (BE) AL BA HR LV MK YU (56) References cited: (30) Priority: 02.12.2003 US 725965 WO-A-98/43646 WO-A-02/051833 02.12.2003 CA 2451798 DE-A- 4 039 631 US-A- 5 762 960 02.12.2003 EP 03447279 05.01.2004 EP 04447001 • VOLMAT R ET AL: "The treatment of depressions 06.01.2004 US 752423 by Cledial. Evolution and clinical state and 18.03.2004 EP 04447066 handwriting" PSYCHOLOGIE MEDICALE 1986 18.03.2004 US 803793 FRANCE, vol. 18, no. 10, 1986, pages 1615-1622, 18.03.2004 CA 2461248 XP009028776 21.10.2004 EP 04025035 • SQUELART P ET AL: "Pipamperone (Dipiperon), 04.11.2004 JP 2004349085 auseful sedative neuroleptic drug in troublesome 09.11.2004 US 984683 chronic psychotic patients." ACTA 15.11.2004 CA 2487529 PSYCHIATRICA BELGICA. BELGIUM 1977 MAR- APR, vol. 77, no. 2, March 1977 (1977-03), pages (43) Date of publication of application: 284-293, XP009028314 ISSN: 0300-8967 11.10.2006 Bulletin 2006/41 • DIEBOLD K. ET AL: "Are psychoactive-drug- induced changes in plasma lipid and lipoprotein (60) Divisional application: levels of significance for clinical remission in 09161718.3 psychiatric disorders?." PHARMACOPSYCHIATRY, (1998) 31/2 (60-67)., (73) Proprietor: PharmaNeuroBoost N.V. 1998, XP009029360 3570 Alken (BE) (72) Inventor: BUNTINX, Erik B-3750 Alken (BE) Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention). EP 1 708 790 B1 Printed by Jouve, 75001 PARIS (FR) (Cont. next page) EP 1 708 790 B1 • KOCH H J ET AL: "Successful therapy of tardive • VIJVER VAN DE D A M C ET AL: dyskinesia in a 71-year-old woman with a "ANTIPSYCHOTICS AND PARKINSON’S combination of tetrabenazine, olanzapine and DISEASE: ASSOCIATION WITH DISEASE AND tiapride." INTERNATIONAL JOURNAL OF DRUG CHOICE DURING THE FIRST 5 YEARS OF CLINICAL PRACTICE. ENGLAND MAR 2003, vol. ANTIPARKINSONIAN DRUG TREATMENT" 57, no. 2, March 2003 (2003-03), pages 147-149, EUROPEAN JOURNAL OF CLINICAL XP009030046 ISSN: 1368-5031 PHARMACOLOGY, SPRINGER VERLAG, DE, vol. • PERUGI G ET AL: "EFFECTIVENESS OF 58, no. 7, 2002, pages 157-161, XP009033980 ADJUNCTIVE GABAPENTIN IN RESISTANT ISSN: 0031-6970 BIPOLAR DISORDER: IS IT DUE TO ANXIOUS- • ENGELBORGHS S ET AL: "AMINO ACIDS AND ALCOHOL ABUSE COMORBIDITY?" JOURNAL BIOGENIC AMINES IN CEREBROSPINAL FLUID OF CLINICAL PSYCHOPHARMACOLOGY, OF PATIENTS WITH PARKINSON’S DISEASE" WILLIAMS AND WILKINS, US, vol. 22, no. 6, 2002, NEUROCHEMICAL RESEARCH, PLENUM pages 584-591, XP009029358 ISSN: 0271-0749 PRESS, NEW YORK, US, vol. 28, no. 8, August • ADLER L ET AL: "PRAXIS DER STATIONAEREN 2003 (2003-08), pages 1145-1150, XP009031514 AKUTBEHANDLUNG VON MANIEN ISSN: 0364-3190 RETROSPEKTIVE • DATABASE EMBASE [Online] ELSEVIER VERGLEICHSUNTERSUCHUNG AN JE 100 SCIENCE PUBLISHERS, AMSTERDAM, NL; 1999, PATIENTEN ZWEIER PSYCHIATRISCHER ETCHEPAREBORDA M C: "Neurocognitive and ZENTREN PRACTICE OF IN-PATIENT ACUTE pharmacological approach to specific learning TREATMENT OF MANIAS" FORTSCHRITTE DER disorders" XP002311106Database accession no. NEUROLOGIE PSYCHIATRIE, STUTTGART, DE, EMB-2000050033 & REVISTA DE NEUROLOGIA vol. 62, no. 12, 1994, pages 479-488, XP009029389 1999 SPAIN, vol. 28, no. SUPPL. 2, 1999, pages ISSN: 0720-4299 S81-S93, ISSN: 0210-0010 • ANSOMS C ET AL: "Sleep disorders in patients • WIRZ-JUSTICE A ET AL: "HALOPERIDOL with severe mental depression: double-blind DISRUPTS, CLOZAPINE REINSTATES THE placebo-controlled evaluation of the value of CIRCADIAN REST-ACTIVITY CYCLE IN A pipamperone (Dipiperon)." ACTA PATIENT WITH EARLY-ONSET ALZHEIMER PSYCHIATRICA SCANDINAVICA. FEB 1977, vol. DISEASE" ALZHEIMER DISEASE AND 55, no. 2, February 1977 (1977-02), pages 116-122, ASSOCIATEDDISORDERS, RAVEN PRESS, NEW XP009041169 ISSN: 0001-690X YORK, NY, US, vol. 14, no. 4, 2000, pages 212-215, • LEYSEN J E ET AL: "RECEPTOR INTERACTI0NS XP009029353 ISSN: 0893-0341 OF NEW ANTIPSYCHOTICS: RELATION TO • FAHS H ET AL: "THYMOREGULATEURS DANS PHARMACODYNAMICAND CLINICAL EFFECTS" L’AGITATION ET LES TROUBLES DU INTERNATIONAL JOURNAL OF PSYCHIATRY IN COMPORTEMENT CHEZ LE SUJET DEMENT A CLINICAL PRACTICE, MARTIN DUNITZ, PROPOS DE HUIT CAS ANTICONVULSIVANTS LONDON, GB, vol. 2, no. 1, 1998, pages S03-S17, AND AGGRESSIVE BEHAVIORS IN XP001009585 ISSN: 1365-1501 ALZHEIMER’S DISEASE. EIGHT CASES • DATABASE BIOSIS [Online] BIOSCIENCES REPORTS" ENCEPHALE, PARIS, FR, vol. 25, no. INFORMATION SERVICE, PHILADELPHIA, PA, 2, 1999, pages 169-174, XP009039295 ISSN: US; 1996, SCHOTTE A ET AL: "Risperidone 0013-7006 compared with new and reference antipsychotic • GRÖZINGER M ET AL: "Melperone is an inhibitor drugs: In vitro and in vivo receptor binding" of the CYP2D6 catalyzed O-demethylation of XP002290498 Database accession no. venlafaxine." PHARMACOPSYCHIATRY. PREV199698829913 & GERMANY JAN 2003, vol. 36, no. 1, January 2003 PSYCHOPHARMACOLOGY, vol. 124, no. 1-2, (2003-01), pages 3-6, XP009029363 ISSN: 1996, pages 57-73, ISSN: 0033-3158 0176-3679 • VANHOENACKER P ET AL: "EFFICIENT • WERTH ESTHER ET AL: "Decline in long-term EXPRESSION OF THE HUMAN DOPAMINE D4.2 circadian rest-activity cycle organization in a RECEPTOR: POSITIVE INFLUENCE OF patientwith dementia." JOURNAL OF GERIATRIC PIPAMPERONE ON EXPRESSION LEVELS" PSYCHIATRY AND NEUROLOGY. 2002 SPRING, ABSTRACTS OF THE SOCIETY FOR vol. 15, no. 1, April 2002 (2002-04), pages 55-59, NEUROSCIENCE, SOCIETY FOR XP009042127 ISSN: 0891-9887 NEUROSCIENCE,WASHINGTON, DC, US, vol. 26, • STAHL STEPHEN M ET AL: "Examination of no. 1/2, 2000, page 1, XP001181469 ISSN: nighttime sleep-related problems during double- 0190-5295 blind, placebo-controlled trials of galantamine in patients with Alzheimer’s disease." CURRENT MEDICAL RESEARCH AND OPINION. APR 2004, vol. 20, no. 4, April 2004 (2004-04), pages 517-524, XP009041652 ISSN: 0300-7995 2 (Cont. next page) EP 1 708 790 B1 • DATABASE BIOSIS [Online] BIOSCIENCES • Retrieved from the Internet: URL:http: INFORMATION SERVICE, PHILADELPHIA, PA, //www.biam2.org/www/Sub2783.html> US; 1995, MELTZER HERBERT Y ET AL: "Plasma • Retrieved from the Internet: URL:http: clozapine levels and the treatment of L-DOPA- //www.adiph.org/pic/pedia-neurole ptiques.pdf> induced psychosis in Parkinson’s disease. A • FITZGERALD K D: "Risperidone augmentation of high potency effect of clozapine" XP002290499 serotonin reuptake inhibitor treatment of Database accession no. PREV199598192811 & pediatric obsessive compulsive disorder" NEUROPSYCHOPHARMACOLOGY,vol. 12, no. 1, JOURNAL OF CHILD AND ADOLESCENT 1995, pages 39-45, ISSN: 0893-133X PSYCHOPHARMACOLOGY, vol. 9, no. 2, 1999, • MUENCHAU A ET AL: "PHARMACOLOGICAL pages 115-123, UNITED STATES TREATMENT OF PARKINSON’S DISEASE" • MCDOUGLE: "A double-blind, placebo- POSTGRADUATE MEDICAL JOURNAL, controlled study of risperidone addition in MCMILLAN PRESS, BASINGSTOKE, GB, vol. 76, serotonin reuptake inhibitor-refractory no. 900, October 2000 (2000-10), pages 602-610, obsessive-compulsive disorder" ARCHIVES OF XP009034316 ISSN: 0032-5473 GENERAL PSYCHIATRY, vol. 57, no. 8, 2000, • FALTRACO F ET AL: "AKTUELLE pages 794-801, THERAPIEMOEGLICHKEITEN DER ALZHEIMER • MAINAGIUSEPPE: "Antipsychotic augmentation DEMENZ CURRENT THERAPEUTICAL for treatment resistant obsessive-compulsive STRATEGIES IN DEMENTIA" NEUROLOGIE UND disorder: What if antipsychotic is discontinued? " REHABILITATION, BONN, DE, vol. 9, no. 1, 2003, INTERNATIONAL CLINICAL pages 15-22, XP009041267 ISSN: 0947-2177 PSYCHOPHARMACOLOGY, vol. 18, no. 1, 2003, • WIELING W ET AL: "INITIAL ORTHOSTATIC pages 23-28, HYPOTENSION AS A CAUSE OF RECURRENT • HIROSE SHIGEHIRO: "An open pilot study SYNCOPE: A CASE REPORT" CLINICAL combining risperidone and a selective serotonin AUTONOMIC RESEARCH, RAPID reuptake inhibitor as initial antidepressant COMMUNICATIONS, vol. 11, no. 4, 2001, pages therapy" THE JOURNAL OF CLINICAL 269-270, XP009039296 Oxford, GB PSYCHIATRY, vol. 63, no. 8, 2002, pages 733-736, • FOUKS D ET AL: "TRAITEMENT DES TROUBLES US CARACTERIELS PAR UNE NOUVELLE BUTYROPHENONE:LE R. 3345 OU Remarks: PIPAMPERONE" ANNALES MEDICO- Thefile contains technical information submitted after PSYCHOLOGIQUES,
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    Original article | Published 24 July 2017 | doi:10.4414/smw.2017.14471 Cite this as: Swiss Med Wkly. 2017;147:w14471 Pipamperone and delirium: a preliminary evaluation of its effectiveness in the management of delirium and its subtypes Boettger Soenkea, Knoepfel Silvanaa, Schubert Mariabd, Garcia Nuñez Davidc, Plichta Michael Martine, Klaghofer Richarda, Jenewein Josefa a Department of Psychiatry and Psychotherapy, University of Zurich, University Hospital Zurich, Switzerland b Centre of Clinical Nursing Science, University of Zurich, University Hospital Zurich, Switzerland c University Basel, University Hospital Basel, Switzerland d Directorate of Nursing/MTT, Inselspital, University Hospital Bern, Switzerland e Department of Psychiatry, Psychosomatic Medicine and Psychotherapy, Goethe University, Frankfurt, Germany Summary Key words: haloperidol, pipamperone, antipsychotics, delirium, subtypes, effectiveness INTRODUCTION: Delirium has been recognised as an underdiagnosed and undermanaged syndrome with sub- Introduction stantial prevalence rates and potentially deleterious con- sequences in the medically ill population. Despite its fre- Delirium is a neuropsychiatric syndrome characterised by quent administration in the management of delirium, the an abrupt onset and fluctuating disturbances in conscious- effectiveness of pipamperone has not yet been evaluated. ness and cognition, as well as a range of noncognitive domains including disturbances in motor behaviour, emo- METHODS: In this retrospective, descriptive cohort study tionality and sleep-wake cycle, caused by an underlying of 192 patients, pipamperone as monotherapy and as an aetiology [1, 2]. adjunct to haloperidol, haloperidol alone, or atypical an- Delirium is a common occurrence over the course of hos- tipsychotics were compared with respect to their effective- pitalisation, depending, among other factors, on the age ness in the management of delirium and its subtypes over and gender of the patient, previous episodes of delirium, the course of 20 days.
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  • Concentrations of Antidepressants, Antipsychotics, and Benzodiazepines in Hair Samples from Postmortem Cases
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    (19) & (11) EP 2 236 138 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 06.10.2010 Bulletin 2010/40 A61K 31/4545 (2006.01) A61K 45/06 (2006.01) A61P 25/22 (2006.01) A61P 25/24 (2006.01) (2006.01) (21) Application number: 09156752.9 A61K 31/343 (22) Date of filing: 30.03.2009 (84) Designated Contracting States: • van der Geest, Ronald AT BE BG CH CY CZ DE DK EE ES FI FR GB GR 4835 AA, Breda (BE) HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK TR (74) Representative: De Clercq, Ann G. Y. et al Designated Extension States: De Clercq & Partners cvba AL BA RS Edgard Gevaertdreef 10 a 9830 Sint-Martens-Latem (BE) (71) Applicant: PharmaNeuroBoost N.V. 3570 Alken (BE) Remarks: Claim .17-19,21-24ed to be abandoned due to non- (72) Inventors: payment of the claims fee (Rule 45(3) EPC). • Buntinx, Erik 3570, Alken (BE) (54) Low dose pipamperone in treating mood and anxiety disorders (57) The present invention relates to the use of combinations comprising pipamperone and an SSRI, SNDRI or SNRI and compositions comprising the same for the treatment of mood or anxiety disorders. EP 2 236 138 A1 Printed by Jouve, 75001 PARIS (FR) EP 2 236 138 A1 Description Field of the invention 5 [0001] The invention relates to the field of neuropsychiatry. More specifically, the invention relates to the use of pipamperone in augmenting and in a faster onset of serotonin re- uptake inhibitors, such as SSRIs, SNDRIs and SNRIs, in treating mood and anxiety disorders.
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