Risperidone

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H301：Giftig bei Verschlucken.

• Sicherheit

  P301+P310：BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

Risperidone Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R25:Giftig beim Verschlucken.

• S-Sätze 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 möglich, dieses Etikett vorzeigen).

• Beschreibung

  Risperidone is a novel antipsychotic introduced for the treatment of acute and chronic schizophrenia. It has a balanced serotonin 5-HT₂ and dopamine D₂ receptor antagonist activity. While the anti-D₂ activity may relate to the antipsychotic potency of neuroleptic agents, an antidepressive efficacy of substances with anti-5-HT₂ 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 D₂ antagonist antipsychotics. It also has potential for management of alcohol withdrawal and cocaine addiction.

• Chemische Eigenschaften

  Crystalline Solid

• Originator

  Janssen (U.S.A.)

• Verwenden

  For the treatment of schizophrenia in adults and in adolescents, ages 13 to 17, and for the short-term treatment of manic or mixed episodes of bipolar I disorder in children and adolescents ages 10 to 17. May also be used to manage symptoms of inappropria

• Verwenden

  neuroprotectant, inhibitory neurotransmitter, GABA agonist

• Verwenden

  A combined serotonin (5-HT2) and dopamine (D2) receptor antagonist

• 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.

• Trademarks

  Risperdal (Janssen).

• 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-HT₂–D₂ 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.

• Allgemeine Beschreibung

  Risperidone, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2]pyrimidin-4-one (Risperdal), is awhite to slightly beige powder that is essentially insoluble inwater. Risperidone is also available as a 1-mg/mL oral solutionand as orally disintegrating tablets (Risperdal M-Tab).Risperidone is well absorbed, and peak levels occur about 1hour after administration. The absorption of risperidone is notaffected by food. Risperidone is about 90% bound to albuminand 1-acid glycoprotein, whereas its metabolite 9-hydroxyrisperidoneis bound about 77%. Risperidone is primarilymetabolized in humans to the active metabolite 9-hydroxyrisperidone..The major side effects associated with risperidonetherapy are orthostatic hypotension, dose-related hyperprolactinemia,mild weight gain, EPS, and insomnia.Athigher doses (6 mg/day), risperidone is the atypical antipsychoticthat most closely resembles conventional agents. APET study in a group of individuals with schizophreniashowed that D₂ receptor occupancy was dose dependent. Ifthe dose was increased such that D₂ receptor occupancy was79% to 85%, the majority of patients developed EPS.Risperidone is associated with increased mortality in elderlypatients with dementia-related psychosis and is not recommendedfor these individuals.23 Risperidone binds with highaffinity at 5-HT_2A, 5-HT₇, D₂, 1, 2, and H1 receptors. Theantipsychotic action of risperidone has been proposed tobe the result of D₂ and 5-HT_2A antagonism.

• Biologische Aktivität

  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).

• Biochem/physiol Actions

  Risperidone is an antipsychotic; serotonin-dopamine antagonist.

• Clinical Use

  
  Schizophrenia
  Psychoses
  Mania
  Persistent aggression in Alzheimer’s dementia

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Anaesthetics: enhanced hypotensive effect.
  Analgesics: increased risk of convulsions with tramadol; enhanced hypotensive and sedative effects with opioids; increased risk of ventricular arrhythmias with methadone - avoid.
  Antidepressants: concentration increased by fluoxetine and possibly paroxetine; concentration of tricyclics possibly increased.
  Antiepileptics: antagonism, convulsive threshold may be lowered; metabolism accelerated by carbamazepine.
  Antimalarials: avoid with artemether with lumefantrine; possible increased risk of ventricular arrhythmias with mefloquine and quinine.
  Antipsychotics: possible increased risk of ventricular arrhythmias with other antipsychotics that prolong the QT interval; avoid concomitant use of depot formulations with clozapine (cannot be withdrawn quickly if neutropenia occurs).
  Antivirals: ritonavir may increase concentration of risperidone.
  Anxiolytics and hypnotics: enhanced sedative effects.
  Atomoxetine: increased risk of ventricular arrhythmias.
  Beta blockers: possible increased risk of ventricular arrhythmias with sotalol.
  Cytotoxics: increased risk of ventricular arrhythmias with arsenic trioxide.
  Lithium: increased risk of extra-pyramidal side effects and possible neurotoxicity.

• Stoffwechsel

  Risperidone is metabolised in the liver by CYP 2D6 to its main active metabolite, 9-hydroxy-risperidone (paliperidone), which has a similar pharmacological activity as risperidone. This hydroxylation is subject to genetic polymorphism. Oxidative N-dealkylation is a minor metabolic pathway.
  Excretion is mainly in the urine and, to a lesser extent, in the faeces.

• Lager

  +4°C

Risperidone Upstream-Materialien And Downstream Produkte

Risperidone Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(573)Suppliers

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