Fluanxol Research Paper
• History and background :
- Fluanxol is a thioxanthene derivative which contains flupentixol as active substances. It belongs to group of medicines known as antidepressants drugs which act on nerve pathway in specific areas of the brain and help in correcting some chemical imbalances that cause the symptoms of this illness.
- Its International Non-proprietary Name (INN) is flupentixol , but its British Approved Name (BAN) is flupenthixol and it is known in the market under the name of Fluanxol and Depixol.
- In the United States , it isn’t approved for use but it is approved in UK , Canada , Australia , NewZealand and South Africa.
• Uses :
- Fluanxol is used to treat schizophrenia and other psychotic diseases in adults. It also …show more content…
Its exact mechanism hasn’t been established but its effects resemble to those of phenothiazines and fluphenazine , so that it belongs to the antipsychotic drugs that cause sedation and hypotension but have a great ability to produce extrapyramidal reactions.
- Fluanxol depot has alerting , antipsychotic and anxiolytic effects. This antipsychotic effect of neuroleptics is related to their dopamine receptor blocking effects which seems to release a chain reaction such as other influenced transmitter systems.
- Flupenthixol is metabolized by dealkylation , sulfoxidation and conjucation to glucuronic acid.
- The metabolites of flupenthixol doesn’t contain any psychopharmacological activity.
- For example : in rats Flupentixol dihydrochloride is metabolized in the liver to sulphoxide and glucuronide derivatives.
- In the feces , it is found mainly in the unchanged state. But in the urine , it is found as the unchanged drug with the sulphoxide and glucuronide derivatives.
Structure activity relationship ( SAR ) :
- Its SAR is extremely related to that of phenothiazine :
1- Any substitution at C1 will decrease