Risperidone Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R25:Giftig beim Verschlucken.
S-S?tze Betriebsanweisung:
S28:Bei Berührung mit der Haut sofort abwaschen mit viel . . . (vom Hersteller anzugeben).
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn m?glich, dieses Etikett vorzeigen).
Beschreibung
Risperidone is a novel antipsychotic introduced for the treatment of acute and chronic
schizophrenia. It has a balanced serotonin 5-HT
2 and dopamine D
2 receptor antagonist
activity. While the anti-D
2 activity may relate to the antipsychotic potency of neuroleptic
agents, an antidepressive efficacy of substances with anti-5-HT
2 activity has been
suggested. Risperidone, therefore, has therapeutic action on both positive and negative
symptoms of schizophrenia and produces significantly fewer side effects especially
extrapyramidal symptoms compared with commonly used pure D
2 antagonist antipsychotics.
It also has potential for management of alcohol withdrawal and cocaine addiction.
Chemische Eigenschaften
Crystalline Solid
Verwenden
Risperidone has been used:
- to study its effects on bone formation and differentiation
- to investigate the relationship between risperidone (RIS) dosages and RIS plasma levels in autism spectrum disorder (ASD) pediatric patients
- to reverse induced schizophrenia-like behavior in mice
Definition
ChEBI: A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.
Allgemeine Beschreibung
Risperidone (Risperdal, a benzisoxazole)has the structural features of a hybrid molecule between abutyrophenone antipsychotic and a trazodone-like antidepressant.Its superior side effects profile (compared withhaloperidol) at dosage of 6 mg/d or less and the lower riskof tardive dyskinesia have contributed to its very widespreaduse. It benefited refractory psychotic patients, withparkinsonism controlled at one tenth the dose of antiparkinsoniandrugs used with haloperidol.Coexisting anxietyand depressive syndromes were also lessened. It is reportedto decrease the negative (e.g., withdrawal, apathy) as well asthe positive (e.g., delusions, hallucinations) symptoms ofschizophrenia. This is reportedly a consequence of the compound’scombination 5-HT
2–D
2 receptor antagonistic properties.Overall, the reasons for the decreased EPS and effectiveness against negative symptom are still under investigation.It is an important atypical antipsychotic.Risperidone is metabolized in the liver by CYP2D6 to anactive metabolite, 9-hydroxyrisperidone. Because thismetabolite and risperidone are nearly equipotent, the clinicalefficacy of the drug reflects both compounds.
Biologische Aktivit?t
Atypical antipsychotic agent that displays 5-HT 2A receptor antagonism. Also displays high affinity at D 2 receptors (K i values are 0.4 and 3.13 nM for 5-HT 2A and D 2 receptors respectively).
Risperidone Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Kaliumiodid
Isoxazol
1H-Pyrimidin-4-on
1,3-Difluorbenzol
885706-66-1
Risperidal iMpurity B
3-(2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride
3-[2-[4-[(Z)-(2,4-Difluorophenyl)(hydroxyiMino)Methyl]-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-Methyl-4H-pyrido[1,2-a]pyriMidin-4-one
Risperidone E-Oxime
2,4-Difluorophenyl-(4-piperidinyl)methanoneoxime
2,4-Difluorophenyl-(4-piperidinyl)methanone oxime hydrochloride
6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole
Ethylentetracarbonitril
Downstream Produkte
