Tiapride
 |
|
| Clinical data | |
|---|---|
| Trade names | Tiapridal |
| Routes of administration |
Oral (tablets), IM, IV |
| ATC code | |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | ~75% (oral) (Tmax = 1 hour) |
| Protein binding | Negligible |
| Biological half-life | 2.9–3.6 hours |
| Excretion | Urine (70% as unchanged tiapride) |
| Identifiers | |
|
|
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEMBL | |
| ECHA InfoCard | 100.051.717 |
| Chemical and physical data | |
| Formula | C15H24N2O4S |
| Molar mass | 328.427 g/mol |
| 3D model (Jmol) | |
|
|
Tiapride is a drug that selectively blocks D2 and D3dopamine receptors in the brain. It is used to treat a variety of neurological and psychiatric disorders including dyskinesia, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly. A derivative of benzamide, tiapride is chemically and functionally similar to other benzamide antipsychotics such as sulpiride and amisulpride known for their dopamine antagonist effects.
Research in animal models and clinical studies in alcoholic patients have found that tiapride has anxiolytic effects. Dopamine hyperactivity has been linked with alcohol withdrawal syndrome (AWS), suggesting that tiapride's antidopaminergic effects are the most likely mechanism for its clinical efficacy, although others believe some other mechanism might be involved. Alcoholic patients treated with tiapride at a dosage of 300 mg/day reported reduced psychological distress and improved abstinence from alcohol. In another study in which alcoholic patients were given titrated doses up to 800 mg/day, subjects showed significant improvements in ratings of withdrawal, craving, psychiatric symptoms and quality of life.
While tiapride does not affect positive symptoms of psychosis such as hallucinosis or delirium sometimes manifested in alcohol withdrawal syndrome, if combined with a drug such as carbamazepine that addresses those symptoms, it is ideal for treating alcohol dependency because its metabolism does not depend on liver function and it has low potential for abuse. This sets it apart from the benzodiazepines, which are contraindicated with alcohol and can be addictive. Moreover, tiapride's rapid onset makes intravenous or intramuscular injection prior to or during withdrawal episodes particularly effective.
...
Wikipedia