World Library  
Flag as Inappropriate
Email this Article


Article Id: WHEBN0028884053
Reproduction Date:

Title: Clocapramine  
Author: World Heritage Encyclopedia
Language: English
Subject: Gevotroline, Desmethylclozapine, Clorotepine, Blonanserin, Sarizotan
Publisher: World Heritage Encyclopedia


Systematic (IUPAC) name
Clinical data
Trade names Clofekton, Padrasen
Legal status
  • Prescription only
Routes Oral
CAS number
ATC code None
Chemical data
Formula C28H37ClN4O 
Mol. mass 481.07 g/mol

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-HT2A, 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-HT2A 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]

See also


  1. ^ David J. Triggle (1997). Dictionary of pharmacological agents. London: Chapman & Hall.  
  2. ^ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. p. 1932.  
  3. ^ Sittig, Marshall (1988). Pharmaceutical manufacturing encyclopedia. Park Ridge, N.J., U.S.A: Noyes Publications. p. 1756.  
  4. ^ 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.  
  5. ^ 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.  
  6. ^ Saito M, Miyaoka H (August 2007). "Augmentation of paroxetine with clocapramine in panic disorder". Psychiatry and Clinical Neurosciences 61 (4): 449.  
  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.  
  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.  
  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.  
  10. ^ 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.  
  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.  
  12. ^ Yamagami S (1985). "A crossover study of clocapramine and haloperidol in chronic schizophrenia". The Journal of International Medical Research 13 (6): 301–10.  
  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.  
  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.  
  15. ^ 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.  
This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.

Copyright © World Library Foundation. All rights reserved. eBooks from Project Gutenberg are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.