QuickView for Risperidone (compound)

Summary
General Info

PubChem

PubChem Compound 5073

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. show more » 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; Risperdal; Rispolept; SPBio_003078; Risperidone; Rispolin; 106266-06-2; Risperin; R-64766; Sequinan; Risperidal M-Tab; CAS-106266-06-2; Belivon; 4H-Pyrido(1,2-a)pyrimidin-4-one, 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-6,7,8,9-tetrahydro-2-methyl-; 4H-Pyrido(1,2-a)pyrimidin-4-one, 6,7,8,9-tetrahydro-3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-2-methyl-; D00426; 3-(2-(4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidino)ethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido(1,2-a)pyrimidin-4-one; Risperdal Consta; Risperdal (TN); EU-0101074; Lopac-R-118; 4H-Pyrido[1,2-a]pyrimidin-4-one, 3-[2-[4-(6-fluoro-1,2-benz-isoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-; Risperidone (JAN/USAN); Prestwick0_001029; Prestwick1_001029; BRN 4891881; Risperdal M-Tab show less «

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... show more » 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 prescribed antipsychotic medication in the United States. show less «
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... show more » 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 dopamine transmission and an elimination of core negative symptoms. Dopamine receptors in the nigrostriatal pathway are not affected by risperidone and extrapyramidal effects are avoided. Like other 5-HT₂ antagonists, risperidone also binds at alpha(1)-adrenergic receptors and, to a lesser extent, at histamine H1 and alpha(2)-adrenergic receptors. show less «
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:

Tetrabenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Paroxetine	The SSRI, paroxetine, increases the effect and toxicity of risperidone.
Itraconazole	Increases the level of risperidone
Lumefantrine	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Donepezil	Possible antagonism of action

Tetrabenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Paroxetine	The SSRI, paroxetine, increases the effect and toxicity of risperidone.
Itraconazole	Increases the level of risperidone
Lumefantrine	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Donepezil	Possible antagonism of action
Terbinafine	Terbinafine may reduce the metabolism and clearance of Risperidone. Consider alternate therapy or monitor for therapeutic/adverse effects of Risperidone if Terbinafine is initiated, discontinued or dose changed.
Zuclopenthixol	Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Indinavir	Increased risk of extrapyramidal symptoms
Fluoxetine	The SSRI, fluoxetine, increases the effect and toxicity of risperidone.
Divalproex sodium	Risperidone increases the effect and toxicity of valproic acid
Triprolidine	Triprolidine and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Trospium	Trospium and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Carbamazepine	Decreases the effect of risperidone
Tacrine	The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Risperidone, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
Thiothixene	May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
Trimethobenzamide	Trimethobenzamide and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Galantamine	Possible antagonism of action
Ziprasidone	Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
Artemether	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Tacrolimus	Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Toremifene	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
Trimipramine	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Paliperidone	Paliperidone is the active metabolite of risperidone, 9-OH-risperidone. Concomitant therapy may increase the adverse effects of paliperidone due to additive paliperidone exposure. Consider alternate therapy.
Voriconazole	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).