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Cyamemazine
Antipsychotic medication
Antipsychotic medication
| Drugs.com =
| elimination_half-life = 10 hours
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.
Medical use
It is used for the treatment of schizophrenia and, especially, for psychosis-associated anxiety, due to its unique anxiolytic efficacy.
It is also used to reduce anxiety associated with benzodiazepine withdrawal syndrome and anxiety in depression with suicidal tendency.
Side effects
Here are some of the most common side effects and related incidence:
- Sedation (20%)
- Vertigo (7.9%)
- Constipation (4%)
- Dyskinesia (4.4%)
- Dryness of mouth (5.9%)
- Hypotension (7.4%)
- Tachycardia (3.2%)
Mechanism
Cyamemazine differs from other phenothiazine neuroleptics in that aside from the usual profile of dopamine, α1-adrenergic, H1, and mACh receptor antagonism, it additionally produces potent blockade of several serotonin receptors, including 5-HT2A, 5-HT2C, and 5-HT7. These actions have been implicated in cyamemazine's anxiolytic effects (5-HT2C) and lack of extrapyramidal side effects (5-HT2A), and despite being classified as a typical antipsychotic, it actually behaves like an atypical antipsychotic.
| Site | Ki (nM) | Species | Ref | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| H1 | 9.3 | Guinea pig | vauthors = Hameg A, Bayle F, Nuss P, Dupuis P, Garay RP, Dib M | title = Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes | journal = Biochemical Pharmacology | volume = 65 | issue = 3 | pages = 435–440 | date = February 2003 | pmid = 12527336 | doi = 10.1016/s0006-2952(02)01515-0 }} |
| H2 | 351 | Guinea pig | |||||||||
| H3 | 10000+ | Rat | |||||||||
| M1 | 13 | Human | |||||||||
| M2 | 42 | Human | |||||||||
| M3 | 32 | Human | |||||||||
| M4 | 12 | Human | |||||||||
| M5 | 35 | Human | |||||||||
| 5-HT1A | 517 | Human | |||||||||
| 5-HT2A | 1.5 | Human | |||||||||
| 5-HT2C | 12 | Human | |||||||||
| 5-HT3 | 2943 | Human | |||||||||
| 5-HT7 | 22 | Human | |||||||||
| D1 | 3.8 | Human | |||||||||
| D2 | 5.8 | Human | |||||||||
| D3 | 2.5 | Human | |||||||||
| D4 | 5.3 | Human | |||||||||
| α1 | 2.3 | Rat | |||||||||
| α2 | 1320 | Rat | |||||||||
| GABAA | 10000+ | Rat | |||||||||
| GABAB | 10000+ | Rat | |||||||||
| Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. |
Synthesis
2-Cyanophenothiazine [38642-74-9] (1) 3-Chloro-2-methylpropyl(dimethyl)amine [23349-86-2] (2)
References
References
- (2000). "Index Nominum, International Drug". Taylor & Francis.
- (1996). "Dictionary of Pharmacological Agents". Chapman & Hall/CRC.
- (January 1988). "Pharmaceutical manufacturing ... - Google Books". Noyes Publications.
- (April 2009). "[Prescribing patterns of antipsychotics in 13 French psychiatric hospitals]". L'Encephale.
- "Stahl's Essential Psychopharmacology". Cambridge University Press.
- (September 2001). "Cyamemazine as an anxiolytic drug on the elevated plus maze and light/dark paradigm in mice". Behavioural Brain Research.
- (July 2012). "Potential role of cortical 5-HT(2A) receptors in the anxiolytic action of cyamemazine in benzodiazepine withdrawal". Elsevier BV.
- (2006-06-07). "Preclinical and clinical pharmacology of cyamemazine: anxiolytic effects and prevention of alcohol and benzodiazepine withdrawal syndrome". Wiley.
- (February 2003). "Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes". Biochemical Pharmacology.
- (January 2000). "5-HT3- and 5-HT2C-antagonist properties of cyamemazine: significance for its clinical anxiolytic activity". Psychopharmacology.
- (November 2002). "5-HT2A receptor antagonist properties of cyamemazine in rat and guinea pig smooth muscle". European Journal of Pharmacology.
- (January 2008). "Affinity of cyamemazine metabolites for serotonin, histamine and dopamine receptor subtypes". European Journal of Pharmacology.
- (February 2003). "Reduction of extracellular dopamine and metabolite concentrations in rat striatum by low doses of acute cyamemazine". Naunyn-Schmiedeberg's Archives of Pharmacology.
- (February 2003). "Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes". Biochemical Pharmacology.
- (1961). "Synthesis of Phenothiazines. VI. Certain 2-Substituted Phenothiazines and Their 10-Aminoalkyl Derivatives". The Journal of Organic Chemistry.
- {{cite patent
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