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QuickView for Risperidone (compound)


PubChem
Name: Risperidone
PubChem Compound ID: 5073
Description: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.
Molecular formula: C23H27FN4O2
Molecular weight: 410.485 g/mol
Synonyms:
R 64766; AIDS-085404; Risperidone [USAN:BAN:INN]; NCGC00015883-02; NCGC00015883-01; Risperidona [Spanish]; LS-134196; Risperidonum [Latin]; 3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperi-dino]ethyl]-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one; AIDS085404.
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DrugBank
Identification
Name: Risperidone
Name (isomeric): DB00734
Drug Type: small molecule
Description: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.
Synonyms:
Risperidonum [Latin]; risperdone; Risperidona [Spanish]
Brand: Risperidal M-Tab, Sequinan, Rispolin, Rispolept, Risperin, Risperdal, Risperdal M-Tab, Risperdal Consta
Category: Serotonin Antagonists, Dopamine Antagonists, Antipsychotic Agents, Antipsychotics
CAS number: 106266-06-2
Pharmacology
Indication: 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 inappropriate behavior due to aggression and/or psychosis in patients with severe dementia.
Pharmacology:
Risperidone is an atypical antipsychotic medication. It is most often used to treat delusional psychosis (including schizophrenia), but risperidone is also used to treat some forms of bipolar disorder and psychotic depression. It also has shown some success in treating symptoms of Asperger's Syndrome and autism. Risperidone is now the most commonly...
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Mechanism of Action:
Blockade of dopaminergic D2 receptors in the limbic system alleviates positive symptoms of schizophrenia such as hallucinations, delusions, and erratic behavior and speech. Blockade of serotonergic 5-HT2 receptors in the mesocortical tract, causes an excess of dopamine and an increase in dopamine transmission, resulting in an increase in...
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Absorption: Well absorbed. The absolute oral bioavailability of risperidone is 70% (CV=25%). The relative oral bioavailability of risperidone from a tablet is 94% (CV=10%) when compared to a solution.
Protein binding: Risperidone, ~88% bound; 9-hydroxyrisperidone, ~77% bound.
Biotransformation: Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone, which has approximately the same receptor binding affinity as risperidone. Hydroxylation is dependent on debrisoquine 4-hydroxylase and metabolism is sensitive to genetic polymorphisms in debrisoquine 4-hydroxylase. Risperidone also undergoes N-dealkylation to a lesser extent.
Route of elimination: Risperidone is extensively metabolized in the liver.In healthy elderly subjects, renal clearance of both risperidone and 9-hydroxyrisperidone was decreased, and elimination half-lives were prolonged compared to young healthy subjects.
Half Life: 20-24 hours
Toxicity: Symptoms of overdose include drowsiness, sedation, tachycardia, hypotension, and extrapyramidal symptoms. LD50=82.1mg/kg (orally in mice).
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
TetrabenazineMay cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
ParoxetineThe SSRI, paroxetine, increases the effect and toxicity of risperidone.
ItraconazoleIncreases the level of risperidone
LumefantrineAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
DonepezilPossible antagonism of action
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