Cyamemazine

Cyamemazine (Tercian), also known as cyamepromazine, is a typical antipsychotic drug of the phenothiazine class which was introduced by Theraplix in France in 1972 and later in Portugal as well.[1][2][3][4] It is used for the treatment of schizophrenia and, especially, for psychosis-associated anxiety, due to its unique anxiolytic efficacy.[5][6]


Cyamemazine
Clinical data
Trade namesTercian
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral, IM, IV
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability10-70%
MetabolismHepatic
Elimination half-life10 hours
ExcretionUrine
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard100.020.541
Chemical and physical data
FormulaC19H21N3S
Molar mass323.46 g·mol−1
3D model (JSmol)
 NY (what is this?)  (verify)

Cyamemazine differs from other phenothiazine neuroleptics in that aside from the usual profile of dopamine, α1-adrenergic, H1, and mACh receptor antagonism,[7] it additionally produces potent blockade of several serotonin receptors, including 5-HT2A, 5-HT2C, and 5-HT7.[7][8][9][10] These actions have been implicated in cyamemazine's anxiolytic effects (5-HT2C) and lack of extrapyramidal side effects (5-HT2A),[7][8] and despite being classified as a typical antipsychotic, it actually behaves like an atypical antipsychotic.[11]

Site Ki (nM) Species Ref
H1 9.3 Guinea pig [12]
H2 351 Guinea pig [12]
H3 >10,000 Rat [12]
M1 13 Human [12]
M2 42 Human [12]
M3 32 Human [12]
M4 12 Human [12]
M5 35 Human [12]
5-HT1A 517 Human [12]
5-HT2A 1.5 Human [12]
5-HT2C 12 Human [12]
5-HT3 2943 Human [12]
5-HT7 22 Human [12]
D1 3.8 Human [12]
D2 5.8 Human [12]
D3 2.5 Human [12]
D4 5.3 Human [12]
α1 2.3 Rat [12]
α2 1320 Rat [12]
GABAA >10,000 Rat [12]
GABAB >10,000 Rat [12]
Values are Ki (nM). The smaller the value,

the more strongly the drug binds to the site.


References
  1. Index nominum, international drug ... - Google Books. 2000. ISBN 9783887630751.
  2. David J. Triggle (1996). Dictionary of Pharmacological Agents. Boca Raton: Chapman & Hall/CRC. p. 534. ISBN 0-412-46630-9.
  3. Sittig, Marshall (January 1988). Pharmaceutical manufacturing ... - Google Books. ISBN 9780815511441.
  4. Bret P, Bret MC, Queuille E (April 2009). "[Prescribing patterns of antipsychotics in 13 French psychiatric hospitals]". L'Encéphale (in French). 35 (2): 129–38. doi:10.1016/j.encep.2008.03.007. PMID 19393381. Archived from the original on 2013-02-13.
  5. "Stahl's Essential Psychopharmacology - Cambridge University Press".
  6. Bourin M, Nic Dhonnchadha BA, Claude Colombel M, Dib M, Hascoët M (September 2001). "Cyamemazine as an anxiolytic drug on the elevated plus maze and light/dark paradigm in mice". Behavioural Brain Research. 124 (1): 87–95. doi:10.1016/S0166-4328(01)00238-8. PMID 11423169.
  7. Hameg A, Bayle F, Nuss P, Dupuis P, Garay RP, Dib M (February 2003). "Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes". Biochemical Pharmacology. 65 (3): 435–40. doi:10.1016/S0006-2952(02)01515-0. PMID 12527336.
  8. Alvarez-Guerra M, d'Alché-Birée F, Wolf WA, Vargas F, Dib M, Garay RP (January 2000). "5-HT3- and 5-HT2C-antagonist properties of cyamemazine: significance for its clinical anxiolytic activity". Psychopharmacology. 147 (4): 412–7. doi:10.1007/s002130050010. PMID 10672635. Archived from the original on 2002-01-12. Retrieved 2010-02-11.
  9. Alvarez-Guerra M, Hameg A, Bayle F, Dib M, Garay RP (November 2002). "5-HT2A receptor antagonist properties of cyamemazine in rat and guinea pig smooth muscle". European Journal of Pharmacology. 454 (2–3): 235–9. doi:10.1016/S0014-2999(02)02489-5. PMID 12421652.
  10. Benyamina A, Arbus C, Nuss P, Garay RP, Neliat G, Hameg A (January 2008). "Affinity of cyamemazine metabolites for serotonin, histamine and dopamine receptor subtypes". European Journal of Pharmacology. 578 (2–3): 142–7. doi:10.1016/j.ejphar.2007.09.025. PMID 17936750.
  11. Peinado J, Hameg A, Garay RP, Bayle F, Nuss P, Dib M (February 2003). "Reduction of extracellular dopamine and metabolite concentrations in rat striatum by low doses of acute cyamemazine". Naunyn-Schmiedeberg's Archives of Pharmacology. 367 (2): 134–9. doi:10.1007/s00210-002-0665-4. PMID 12595954.
  12. Hameg, Ahcène; Bayle, Franck; Nuss, Philippe; Dupuis, Philippe; Garay, Ricardo P.; Dib, Michel (2003-02-01). "Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes". Biochemical Pharmacology. 65 (3): 435–440. doi:10.1016/s0006-2952(02)01515-0. ISSN 0006-2952. PMID 12527336.


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