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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/08/16 17:28:20」(JST)

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Pipamperone (INN, USAN, BAN), also known as carpiperone and floropipamide or fluoropipamide, and as floropipamide hydrochloride (JAN), is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia.^[1]^[2] It is or has been marketed under brand names including Dipiperon, Dipiperal, Piperonil, Piperonyl, and Propitan.^[2] Pipamperone was discovered at Janssen Pharmaceutica in 1961, and entered clinical trials in the United States in 1963.^[3]

Pharmacology

Pipamperon neuraxpharm, 40mg

Pipamperone acts as an antagonist of the 5-HT_2A,^[4] 5-HT_2B,^[5] 5-HT_2C^[6] D₂,^[4] D₃,^[7] D₄,^[4]^[8] α₁-adrenergic,^[7] and α₂-adrenergic receptors.^[7] It shows much higher affinity for the 5-HT_2A and D₄ receptors over the D₂ receptor (15-fold in the case of the D₄ receptor, and even higher in the case of the 5-HT_2A receptor),^[4]^[7]^[9] being regarded as "highly selective" for the former two sites at low doses.^[9]^[10] Pipamperone has low and likely insignificant affinity for the H₁ and mACh receptors, as well as for other serotonin and dopamine receptors.^[7]

Pipamperone is considered to have been a forerunner to the atypical antipsychotics, if not an atypical antipsychotic itself, due to its prominent serotonin antagonism.^[11]^[12]^[13]

Antidepressant effects

Low-dose pipamperone (5 mg twice daily) has been found to accelerate and enhance the antidepressant effect of citalopram (40 mg once daily), in a combination (citalopram/pipamperone) referred to as PipCit (code name PNB-01).^[9]^[14]

References

^ Dr. Ian Morton; I.K. Morton; Judith M. Hall (31 October 1999). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 222–. ISBN 978-0-7514-0499-9.
^ ^a ^b J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 985–. ISBN 978-1-4757-2085-3.
^ David Healy (1 July 2009). The Creation of Psychopharmacology. Harvard University Press. pp. 251–. ISBN 978-0-674-03845-5.
^ ^a ^b ^c ^d Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE (1996). "Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding". Psychopharmacology (Berl.) 124 (1-2): 57–73. PMID 8935801.
^ Wainscott DB, Lucaites VL, Kursar JD, Baez M, Nelson DL (1996). "Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences". J. Pharmacol. Exp. Ther. 276 (2): 720–7. PMID 8632342.
^ Prinssen EP, Koek W, Kleven MS (2000). "The effects of antipsychotics with 5-HT(2C) receptor affinity in behavioral assays selective for 5-HT(2C) receptor antagonist properties of compounds". Eur. J. Pharmacol. 388 (1): 57–67. PMID 10657547.
^ ^a ^b ^c ^d ^e Bart A. Ellenbroek; Alexander R. Cools (6 December 2012). Atypical Antipsychotics. Birkhäuser. pp. 62–. ISBN 978-3-0348-8448-8.
^ Van Craenenbroeck K, Gellynck E, Lintermans B, Leysen JE, Van Tol HH, Haegeman G, Vanhoenacker P (2006). "Influence of the antipsychotic drug pipamperone on the expression of the dopamine D4 receptor". Life Sci. 80 (1): 74–81. doi:10.1016/j.lfs.2006.08.024. PMID 16978659.
^ ^a ^b ^c Wade AG, Crawford GM, Nemeroff CB, Schatzberg AF, Schlaepfer T, McConnachie A, Haazen L, Buntinx E (2011). "Citalopram plus low-dose pipamperone versus citalopram plus placebo in patients with major depressive disorder: an 8-week, double-blind, randomized study on magnitude and timing of clinical response". Psychol Med 41 (10): 2089–97. doi:10.1017/S0033291711000158. PMID 21349239.
^ Michael S. Lidow (22 June 2000). Neurotransmitter Receptors in Actions of Antipsychotic Medications. CRC Press. pp. 88–. ISBN 978-1-4200-4177-4.
^ Awouters FH, Lewi PJ (2007). "Forty years of antipsychotic Drug research--from haloperidol to paliperidone--with Dr. Paul Janssen". Arzneimittelforschung 57 (10): 625–32. doi:10.1055/s-0031-1296660. PMID 18074755.
^ Vanden Bussche G, Gelders YG, Heylen SL (1990). "[Development of new antipsychotic drugs]". Acta Psiquiatr Psicol Am Lat (in Spanish; Castilian) 36 (1-2): 13–25. PMID 2127339. CS1 maint: Unrecognized language (link)
^ Niemegeers CJ, Awouters F, Janssen PA (1990). "[Serotonin antagonism involved in the antipsychotic effect. Confirmation with ritanserine and risperidone]". Encephale (in French) 16 (2): 147–51. PMID 1693560.
^ Kirk R (2010). "Clinical trials in CNS--SMi's eighth annual conference". IDrugs 13 (2): 66–9. PMID 20127552.

English Journal

Withdrawal versus continuation of chronic antipsychotic drugs for behavioural and psychological symptoms in older people with dementia.

Declercq T, Petrovic M, Azermai M, Vander Stichele R, De Sutter AI, van Driel ML, Christiaens T.SourceDepartment of General Practice and Primary Health Care, Ghent University, Ghent, Belgium. tomrw.declercq@ugent.be.
The Cochrane database of systematic reviews.Cochrane Database Syst Rev.2013 Mar 28;3:CD007726. doi: 10.1002/14651858.CD007726.pub2.
BACKGROUND: Antipsychotic agents are often used to treat neuropsychiatric symptoms (NPS) in dementia, although the literature is sceptical about their long-term use for this indication. Their effectiveness is limited and there is concern about adverse effects, including higher mortality with long-te
PMID 23543555

Phelan-McDermid syndrome: clinical report of a 70-year-old woman.

Verhoeven WM, Egger JI, Cohen-Snuijf R, Kant SG, de Leeuw N.SourceVincent van Gogh Institute for Psychiatry, Centre of Excellence for Neuropsychiatry, Venray, The Netherlands. wverhoeven@vvgi.nl
American journal of medical genetics. Part A.Am J Med Genet A.2013 Jan;161A(1):158-61. doi: 10.1002/ajmg.a.35597. Epub 2012 Nov 19.
Phelan-McDermid or 22q13.3 deletion syndrome is characterized by global intellectual disability, childhood hypotonia, severely delayed or absent speech, features of autism spectrum disorder, without any major dysmorphisms or somatic anomalies. It is typically diagnosed before adolescence and data ab
PMID 23166010

Therapeutic drug monitoring of common antipsychotics.

Patteet L, Morrens M, Maudens KE, Niemegeers P, Sabbe B, Neels H.SourceToxicological Centre, University of Antwerp, Universiteitsplein 1, Antwerp, Belgium. patteet@ua.ac.be
Therapeutic drug monitoring.Ther Drug Monit.2012 Dec;34(6):629-51. doi: 10.1097/FTD.0b013e3182708ec5..
The aim of this review is to provide information for interpreting outcome results from monitoring of antipsychotics in biological samples. A brief overview of the working mechanisms, pharmacological effects, drug interactions, and analytical methods of classical and atypical antipsychotics is given.
PMID 23149440

Japanese Journal

Management of a severe forceful breather with Rett Syndrome using carbogen

SMEETS Eric E. J.,JULU Peter O. O.,VAN WAARDENBURG Dick,ENGERSTROM Ingegerd Witt,HANSEN Stig,APARTOPOULOS Flora,CURFS Leopold M. G.,SCHRANDER-STUMPEL Connie T. R. M.
Brain & development 28(10), 625-632, 2006-11-01
NAID 10018642194

Sleep disorders in patients with severe mental depression : double-blind placebo-controlled evaluation of the value of pipamperone (Dipiperon)

ANSOMS C
Acta Psychiatr Scand 55, 116-122, 1977
NAID 30029215410

Related Pictures

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リンク元	「ピパンペロン」
拡張検索	「pipamperone hydrochloride」

「ピパンペロン」

Pipamperone
Systematic (IUPAC) name
	1'-[4-(4-fluorophenyl)-4-oxobutyl]-1,4'-bipiperidine-4'-carboxamide
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
Identifiers
CAS Registry Number	1893-33-0
ATC code	N05AD05
PubChem	CID: 4830
IUPHAR/BPS	92
ChemSpider	4664
UNII	5402501F0W
KEGG	D02622
ChEMBL	CHEMBL440294
Synonyms	McN-JR 3345; R-3345
Chemical data
Formula	C21H30FN3O2
Molecular mass	375.480 g/mol
	SMILES Fc1ccc(cc1)C(=O)CCCN3CCC(C(=O)N)(N2CCCCC2)CC3 ;
	InChI InChI=1S/C21H30FN3O2/c22-18-8-6-17(7-9-18)19(26)5-4-12-24-15-10-21(11-16-24,20(23)27)25-13-2-1-3-14-25/h6-9H,1-5,10-16H2,(H2,23,27) ; Key:AXKPFOAXAHJUAG-UHFFFAOYSA-N ;
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英: pipamperone
同: 塩酸フロロピパミド floropipamide hydrochloride、フロロピパミド
商: プロピタン
関: 塩酸ピパンペロン pipamperone hydrochloride

抗精神病薬
ブチロフェノン系

「pipamperone hydrochloride」

　　[★]

塩酸ピパンペロン

関: pipamperone

[MortonMorton1999-1] Dr. Ian Morton; I.K. Morton; Judith M. Hall (31 October 1999). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 222–. ISBN 978-0-7514-0499-9.

[Elks2014-2] J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 985–. ISBN 978-1-4757-2085-3.

[Healy2009-3] David Healy (1 July 2009). The Creation of Psychopharmacology. Harvard University Press. pp. 251–. ISBN 978-0-674-03845-5.

[pmid8935801-4] Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE (1996). "Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding". Psychopharmacology (Berl.) 124 (1-2): 57–73. PMID 8935801.

[pmid8632342-5] Wainscott DB, Lucaites VL, Kursar JD, Baez M, Nelson DL (1996). "Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences". J. Pharmacol. Exp. Ther. 276 (2): 720–7. PMID 8632342.

[pmid10657547-6] Prinssen EP, Koek W, Kleven MS (2000). "The effects of antipsychotics with 5-HT(2C) receptor affinity in behavioral assays selective for 5-HT(2C) receptor antagonist properties of compounds". Eur. J. Pharmacol. 388 (1): 57–67. PMID 10657547.

[EllenbroekCools2012-7] Bart A. Ellenbroek; Alexander R. Cools (6 December 2012). Atypical Antipsychotics. Birkhäuser. pp. 62–. ISBN 978-3-0348-8448-8.

[pmid16978659-8] Van Craenenbroeck K, Gellynck E, Lintermans B, Leysen JE, Van Tol HH, Haegeman G, Vanhoenacker P (2006). "Influence of the antipsychotic drug pipamperone on the expression of the dopamine D4 receptor". Life Sci. 80 (1): 74–81. doi:10.1016/j.lfs.2006.08.024. PMID 16978659.

[pmid21349239-9] Wade AG, Crawford GM, Nemeroff CB, Schatzberg AF, Schlaepfer T, McConnachie A, Haazen L, Buntinx E (2011). "Citalopram plus low-dose pipamperone versus citalopram plus placebo in patients with major depressive disorder: an 8-week, double-blind, randomized study on magnitude and timing of clinical response". Psychol Med 41 (10): 2089–97. doi:10.1017/S0033291711000158. PMID 21349239.

[Lidow2000-10] Michael S. Lidow (22 June 2000). Neurotransmitter Receptors in Actions of Antipsychotic Medications. CRC Press. pp. 88–. ISBN 978-1-4200-4177-4.

[pmid18074755-11] Awouters FH, Lewi PJ (2007). "Forty years of antipsychotic Drug research--from haloperidol to paliperidone--with Dr. Paul Janssen". Arzneimittelforschung 57 (10): 625–32. doi:10.1055/s-0031-1296660. PMID 18074755.

[pmid2127339-12] Vanden Bussche G, Gelders YG, Heylen SL (1990). "[Development of new antipsychotic drugs]". Acta Psiquiatr Psicol Am Lat (in Spanish; Castilian) 36 (1-2): 13–25. PMID 2127339. CS1 maint: Unrecognized language (link)

[pmid1693560-13] Niemegeers CJ, Awouters F, Janssen PA (1990). "[Serotonin antagonism involved in the antipsychotic effect. Confirmation with ritanserine and risperidone]". Encephale (in French) 16 (2): 147–51. PMID 1693560.

[pmid20127552-14] Kirk R (2010). "Clinical trials in CNS--SMi's eighth annual conference". IDrugs 13 (2): 66–9. PMID 20127552.

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pipamperone