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Clocapramine

From Wikipedia, the free encyclopedia
Antipsychotic medication
Pharmaceutical compound
Clocapramine
Clinical data
Trade namesClofekton, Padrasen
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral
ATC code
  • None
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • 1-[3-(2-chloro-5,6-dihydrobenzo[b][1]benzazepin-11-yl)propyl]-4-piperidin-1-ylpiperidine-4-carboxamide
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC28H37ClN4O
Molar mass481.08 g·mol−1
3D model (JSmol)
  • Clc1ccc3c(c1)N(c2ccccc2CC3)CCCN5CCC(C(=O)N)(N4CCCCC4)CC5

Clocapramine (Clofekton,Padrasen), also known as3-chlorocarpipramine, is anatypical antipsychotic of theiminostilbene class which was introduced inJapan in 1974 byYoshitomi for the treatment ofschizophrenia.[1][2][3][4][5] In addition topsychosis, clocapramine has also been used to augmentantidepressants in the treatment ofanxiety andpanic.[6]

Clocapramine has been reported to act as anantagonist of theD2,5-HT2A,α1-adrenergic, andα2-adrenergic receptors, and does not inhibit thereuptake of eitherserotonin ornorepinephrine.[4][7][8][9][10] It has also been shown to haveaffinity forSIGMAR1.[11] Clocapramine's affinity for the 5-HT2A receptor is greater than that for the D2 receptor and it has a lower propensity for inducingextrapyramidal symptoms compared totypical antipsychotics, thus underlying itsatypical nature.[4][5][10]

Clinical trials

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In severalclinical trials, clocapramine has been compared to otherneuroleptic agents. Againsthaloperidol, though there was no significant difference in efficacy at the end of the study, clocapramine tended to be superior in alleviatingmotor retardation,alogia, andthought disorder, and also produced fewerside effects.[12] Againstsulpiride, clocapramine demonstrated more favorable effects in the treatment of bothpositive andnegativesymptoms, including motor retardation,delusions,hallucinations, andsocial isolation, though it produced more side effects.[13] Againsttimiperone, clocapramine showed lower efficacy against both positive and negative symptoms and produced more side effects such asdyskinesia,insomnia,constipation, andnausea.[14]

Clocapramine has been implicated in at least one fatality, a suicide in which there were two self-inflicted stab wounds and anoverdose 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]

See also

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References

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  1. ^David J. Triggle (1997).Dictionary of pharmacological agents. London: Chapman & Hall.ISBN 978-0-412-46630-4.
  2. ^Swiss Pharmaceutical Society (2000).Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. p. 1932.ISBN 978-3-88763-075-1.
  3. ^Sittig, Marshall (1988).Pharmaceutical manufacturing encyclopedia. Park Ridge, N.J., U.S.A: Noyes Publications. pp. 1756.ISBN 978-0-8155-1144-1.clocapramine.
  4. ^abcSumiyoshi 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.
  5. ^abOka 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.
  6. ^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.S2CID 38739899.
  7. ^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.doi:10.1159/000468561.PMID 6125486.
  8. ^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.
  9. ^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.
  10. ^abSchotte 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.
  11. ^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.S2CID 19250949.
  12. ^Yamagami S (1985). "A crossover study of clocapramine and haloperidol in chronic schizophrenia".The Journal of International Medical Research.13 (6):301–10.doi:10.1177/030006058501300601.PMID 4076529.S2CID 16157745.
  13. ^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.
  14. ^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.doi:10.1177/030006058301100501.PMID 6139317.S2CID 25624985.
  15. ^abKoreeda 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.
Typical
Disputed
Atypical
Others
α1
Agonists
Antagonists
α2
Agonists
Antagonists
β
Agonists
Antagonists
D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
σ1
σ2
Unsorted
Classes
Antidepressants
(Tricyclic antidepressants(TCAs))
Antihistamines
Antipsychotics
Anticonvulsants
Anticholinergics
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