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Risperidone is a new generation of antipsychotic drugs. Its active ingredient, risperidone, is a selective monoaminergic antagonist with unique properties, which binds with high affinity to 5-hydroxytryptaminergic 5-HT2 receptors and dopamine D2 receptors. Risperidone also binds to α1-adrenergic receptors and with lower affinity to H1-histaminergic and α2-adrenergic receptors. Risperidone does not bind to cholinergic receptors.
Uses and functions of Risperidone.
For the treatment of acute and chronic schizophrenia and various other psychotic states with marked positive symptoms (e.g., hallucinations, fantasies, disturbed thinking, hostility, scepticism) and marked negative symptoms (e.g., unresponsiveness, emotional and social apathy, and hypotonia).
Emotional symptoms associated with schizophrenia (e.g., depression, guilt, anxiety) may also be reduced.
In patients for whom acute-phase treatment is effective, Visteon may continue to be clinically effective in the maintenance phase of treatment.
Drug interactions of Risperidone.
1. This product may antagonise the effects of levodopa and other dopamine agonists.
2. Amimidazole and other hepatic enzyme inducers decrease the plasma concentration of the active ingredient of this product. Once amimidazole or other hepatic enzyme inducers have been discontinued, the dosage of this product should be re-determined and, if necessary, reduced.
3. Phenothiazines, tricyclic antidepressants and some beta-blockers increase the blood concentration of this product, but not that of the antipsychotic active ingredient.
4. When taken with other highly protein-bound drugs, there is no clinically significant reciprocal displacement of plasma proteins.
Product Method of Bulk Risperidone Powder.
4-Carbonyl chloride-1-acetylpiperidine and m-difluorobenzene were acylated under the catalysis of aluminium trichloride, and then hydrolyzed with hydrochloric acid to remove the acetyl group on the piperidine ring, and reacted with hydroxylamine and then base-catalyzed cyclo-combination to obtain a benzisoxazole derivative.4.4 parts of this isoxazole derivative, 5.3 parts of 3-chloroethyl-2-methyl-4H-pyrido[1,2-α]pyrimidin-4-one hydrochloride, 8 parts of sodium carbonate and 0.1 parts of potassium iodide in dimethylformamide, heated at 85-90 °C to give risperidone in 46% yield.
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