関: clocapramine hydrochloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/02/13 03:21:32」(JST)

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Clocapramine (Clofekton, Padrasen), also known as 3-chlorocarpipramine, is an atypical antipsychotic of the imidobenzyl class which was introduced in Japan in 1974 by Yoshitomi for the treatment of schizophrenia.^[1]^[2]^[3]^[4]^[5] In addition to psychosis, clocapramine has also been used to augment antidepressants in the treatment of anxiety and panic.^[6]

Clocapramine has been reported to act as an antagonist of the D₂, 5-HT_2A, α₁-adrenergic, and α₂-adrenergic receptors, and does not inhibit the reuptake of either serotonin or norepinephrine.^[4]^[7]^[8]^[9]^[10] It has also been shown to have affinity for the σ receptors.^[11] Clocapramine's affinity for the 5-HT_2A receptor is greater than that for the D₂ receptor and it has a lower propensity for inducing extrapyramidal symptoms compared to typical antipsychotics, thus underlying its atypical nature.^[4]^[5]^[10]

In several clinical trials, clocapramine has been compared to other neuroleptic agents. Against haloperidol, though there was no significant difference in efficacy at the end of the study, clocapramine tended to be superior in alleviating motor retardation, alogia, and thought disorder, and also produced fewer side effects.^[12] Against sulpiride, clocapramine demonstrated more favorable effects in the treatment of both positive and negative symptoms, including motor retardation, delusions, hallucinations, and social isolation, though it produced more side effects.^[13] Against timiperone, clocapramine showed lower efficacy against both positive and negative symptoms and produced more side effects such as dyskinesia, insomnia, constipation, and nausea.^[14]

Clocapramine has been implicated in at least one fatality, a suicide in which there were two self-inflicted stab wounds and an overdose of clocapramine as well as three other antipsychotics was taken.^[15] The stab wounds could not explain the death, and thus, it was attributed to multiple drug toxicity instead.^[15]

References

^ David J. Triggle (1997). Dictionary of pharmacological agents. London: Chapman & Hall. ISBN 0-412-46630-9.
^ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. p. 1932. ISBN 3-88763-075-0.
^ Sittig, Marshall (1988). Pharmaceutical manufacturing encyclopedia. Park Ridge, N.J., U.S.A: Noyes Publications. p. 1756. ISBN 0-8155-1144-2.
^ ^a ^b ^c Sumiyoshi T, Suzuki K, Sakamoto H, et al. (February 1995). "Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy". Neuropsychopharmacology 12 (1): 57–64. doi:10.1016/0893-133X(94)00064-7. PMID 7766287.
^ ^a ^b Oka T, Hamamura T, Lee Y, et al. (November 2004). "Atypical properties of several classes of antipsychotic drugs on the basis of differential induction of Fos-like immunoreactivity in the rat brain". Life Sciences 76 (2): 225–37. doi:10.1016/j.lfs.2004.08.009. PMID 15519367.
^ Saito M, Miyaoka H (August 2007). "Augmentation of paroxetine with clocapramine in panic disorder". Psychiatry and Clinical Neurosciences 61 (4): 449. doi:10.1111/j.1440-1819.2007.01690.x. PMID 17610675.
^ Kurihara M, Tsumagari T, Setoguchi M, Fukuda T (1982). "A study on the pharmacological and biochemical profile of clocapramine". International Pharmacopsychiatry 17 (2): 73–90. PMID 6125486.
^ Tsukamoto T, Asakura M, Hirata N, Imafuku J, Matsui H, Hasegawa K (September 1984). "Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action". Biological Psychiatry 19 (9): 1283–91. PMID 6149771.
^ Setoguchi M, Sakamori M, Takehara S, Fukuda T (June 1985). "Effects of iminodibenzyl antipsychotic drugs on cerebral dopamine and alpha-adrenergic receptors". European Journal of Pharmacology 112 (3): 313–22. doi:10.1016/0014-2999(85)90776-9. PMID 2862053.
^ ^a ^b Schotte A, Bonaventure P, Janssen PF, Leysen JE (December 1995). "In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used". Japanese Journal of Pharmacology 69 (4): 399–412. doi:10.1254/jjp.69.399. PMID 8786644.
^ Morio Y, Tanimoto H, Yakushiji T, Morimoto Y (February 1994). "Characterization of the currents induced by sigma ligands in NCB20 neuroblastoma cells". Brain Research 637 (1-2): 190–6. doi:10.1016/0006-8993(94)91232-7. PMID 7910100.
^ Yamagami S (1985). "A crossover study of clocapramine and haloperidol in chronic schizophrenia". The Journal of International Medical Research 13 (6): 301–10. PMID 4076529.
^ Yamagami S, Kiriike N, Kawaguchi K (1988). "A single-blind study of clocapramine and sulpiride in hospitalized chronic schizophrenic patients". Drugs under Experimental and Clinical Research 14 (11): 707–13. PMID 3246215.
^ Nakazawa T, Ohara K, Sawa Y, et al. (1983). "Comparison of efficacy of timiperone, a new butyrophenone derivative, and clocapramine in schizophrenia: a multiclinic double-blind study". The Journal of International Medical Research 11 (5): 247–58. PMID 6139317.
^ ^a ^b Koreeda A, Yonemitsu K, Ng'walali PM, Muraoka N, Tsunenari S (October 2001). "Clocapramine-related fatality. Postmortem drug levels in multiple psychoactive drug poisoning". Forensic Science International 122 (1): 48–51. doi:10.1016/S0379-0738(01)00442-X. PMID 11587865.

English Journal

Comparative efficacy and safety of antipsychotics in the treatment of schizophrenia: a network meta-analysis in a Japanese population.

Kishi T1, Ikuta T2, Matsunaga S1, Matsuda Y1,3, Oya K1, Iwata N1.
Neuropsychiatric disease and treatment.Neuropsychiatr Dis Treat.2017 May 11;13:1281-1302. doi: 10.2147/NDT.S134340. eCollection 2017.
PMID 28553116

Iminodibenzyl class antipsychotics for schizophrenia: a systematic review and meta-analysis of carpipramine, clocapramine, and mosapramine.

Kishi T1, Matsunaga S1, Matsuda Y1, Iwata N1.
Neuropsychiatric disease and treatment.Neuropsychiatr Dis Treat.2014 Dec 10;10:2339-51. doi: 10.2147/NDT.S73464. eCollection 2014.
PMID 25525363

Augmentation of paroxetine with clocapramine in panic disorder.

Saito M, Miyaoka H.
Psychiatry and clinical neurosciences.Psychiatry Clin Neurosci.2007 Aug;61(4):449.
PMID 17610675

Japanese Journal

In Vitro Receptor Binding and In Vivo Receptor Occupancy in Rat and Guinea Pig Brain: Risperidone Compared with Antipsychotics Hitherto Used

SCHOTTE Alain,BONAVENTURE Pascal,JANSSEN Paul F. M.,LEYSEN Josee E.
The Japanese journal of pharmacology 69(4), 399-412, 1995-12-01
… Both in vitro and in vivo, risperidone, 9-OH-risperidone, SM-9018, clozapine and clocapramine showed higher affinity for 5-HT2A- than for D2-receptors, whereas mosapramine, haloperidol, bromperidol and nemonapride had a slight to strong preference for D2- compared to 5-HT2A-receptors. …
NAID 10006063907

精神分裂病に対する抗精神病薬 risperidone の臨床評価-Clocapramine を対照薬とした二重盲検比較試験

工藤義雄
臨床精神医学 22, 233-249, 1994
NAID 50003882326

マウスの移所運動促進効果からみたMethamphetamine反復投与による逆耐性現象とドパミンD2遮断薬Mosapramine(Y-516)の併用効果について

内橋慶隆,森本敏彦,田所作太郎
日本薬理学雑誌 99(3), 153-160, 1992
… and they were compared with those of clocapramine (CCP), bromperidol (BPD) and chlorpromazine (CPZ). …
NAID 130000758765

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リンク元	「クロカプラミン」
拡張検索	「clocapramine hydrochloride」

「クロカプラミン」

Clocapramine
Systematic (IUPAC) name
	1'-[3-(3-chloro-10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)propyl]-1,4'-bipiperidine-4'-carboxamide
Clinical data
Trade names	Clofekton, Padrasen
AHFS/Drugs.com	International Drug Names
Legal status	℞ Prescription only;
Routes	Oral
Identifiers
CAS number	47739-98-0
ATC code	None
PubChem	CID 2793
DrugBank	DB09003
ChemSpider	2691
UNII	6EEL1GB72K
KEGG	D07718
ChEMBL	CHEMBL2104103
Chemical data
Formula	C28H37ClN4O
Molecular mass	481.07 g/mol
	SMILES Clc1ccc3c(c1)N(c2ccccc2CC3)CCCN5CCC(C(=O)N)(N4CCCCC4)CC5;