Cyamemazine
Antipsychotic medication
From Wikipedia, the free encyclopedia
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]
administrationOral, IM, IV
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| Clinical data | |
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| Trade names | Tercian |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral, IM, IV |
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| Pharmacokinetic data | |
| Bioavailability | 10-70% |
| Metabolism | Hepatic |
| Elimination half-life | 10 hours |
| Excretion | Urine |
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| ECHA InfoCard | 100.020.541 |
| Chemical and physical data | |
| Formula | C19H21N3S |
| Molar mass | 323.46 g·mol−1 |
| 3D model (JSmol) | |
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Medical use
It is used for the treatment of schizophrenia and, especially, for psychosis-associated anxiety, due to its unique anxiolytic efficacy.[5][6]
It is also used to reduce anxiety associated with benzodiazepine withdrawal syndrome and anxiety in depression with suicidal tendency.[7]
Side effects
Here are some of the most common side effects and related incidence:[8]
- 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,[9] it additionally produces potent blockade of several serotonin receptors, including 5-HT2A, 5-HT2C, and 5-HT7.[9][10][11][12] These actions have been implicated in cyamemazine's anxiolytic effects (5-HT2C) and lack of extrapyramidal side effects (5-HT2A),[9][10] and despite being classified as a typical antipsychotic, it actually behaves like an atypical antipsychotic.[13]
| Site | Ki (nM) | Species | Ref |
|---|---|---|---|
| H1 | 9.3 | Guinea pig | [14] |
| H2 | 351 | Guinea pig | [14] |
| H3 | 10000+ | Rat | [14] |
| M1 | 13 | Human | [14] |
| M2 | 42 | Human | [14] |
| M3 | 32 | Human | [14] |
| M4 | 12 | Human | [14] |
| M5 | 35 | Human | [14] |
| 5-HT1A | 517 | Human | [14] |
| 5-HT2A | 1.5 | Human | [14] |
| 5-HT2C | 12 | Human | [14] |
| 5-HT3 | 2943 | Human | [14] |
| 5-HT7 | 22 | Human | [14] |
| D1 | 3.8 | Human | [14] |
| D2 | 5.8 | Human | [14] |
| D3 | 2.5 | Human | [14] |
| D4 | 5.3 | Human | [14] |
| α1 | 2.3 | Rat | [14] |
| α2 | 1320 | Rat | [14] |
| GABAA | 10000+ | Rat | [14] |
| GABAB | 10000+ | Rat | [14] |
| Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. | |||
