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. SiteKi (nM)SpeciesRefH19.3Guinea pigH2351Guinea pigH310000+RatM113HumanM242HumanM332HumanM412HumanM535Human5-HT1A517Human5-HT2A1.5Human5-HT2C12Human5-HT32943Human5-HT722HumanD13.8HumanD25.8HumanD32.5HumanD45.3Humanα12.3Ratα21320RatGABAA10000+RatGABAB10000+RatValues 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