Definition
Description
Top Gene Interactions
Related Pathways
General Information
- Metabolism: 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
- Uses/Sources: 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.
- Symptoms: Symptoms of overdose include drowsiness, sedation, tachycardia, hypotension, and extrapyramidal symptoms.
- Treatment: In case of acute overdosage, establish and maintain an airway and ensure adequate oxygenation and ventilation. Gastric lavage (after intubation, if patient is unconscious) and administration of activated charcoal together with a laxative should be considered. The possibility of obtundation, seizures, or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis. Cardiovascular monitoring should commence immediately and should include continuous electrocardiographic monitoring to detect possible arrhythmias. If antiarrhythmic therapy is administered, disopyramide, procainamide, and quinidine carry a theoretical hazard of QT-prolonging effects that might be additive to those of risperidone. Similarly, it is reasonable to expect that the alpha-blocking properties of bretylium might be additive to those of risperidone, resulting in problematic hypotension. There is no specific antidote to Risperidone. (L1712)
- Route of Exposure: 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.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD<sub>50</sub>=82.1mg/kg (orally in mice).
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Potassium voltage-gated channel subfamily H member 2 Muscarinic acetylcholine receptor M1 Muscarinic acetylcholine receptor M2 Muscarinic acetylcholine receptor M3 Muscarinic acetylcholine receptor M4 5-hydroxytryptamine receptor 2C 5-hydroxytryptamine receptor 1A 5-hydroxytryptamine receptor 2B Sodium-dependent serotonin transporter Alpha-2A adrenergic receptor 5-hydroxytryptamine receptor 7 D(3) dopamine receptor D(4) dopamine receptor 5-hydroxytryptamine receptor 1B 5-hydroxytryptamine receptor 1D 5-hydroxytryptamine receptor 1F D(1A) dopamine receptor Sigma non-opioid intracellular receptor 1 Alpha-2B adrenergic receptor D(1B) dopamine receptor 5-hydroxytryptamine receptor 6 Alpha-2C adrenergic receptor 5-hydroxytryptamine receptor 1E Solute carrier family 22 member 2 Multidrug and toxin extrusion protein 1 Multidrug and toxin extrusion protein 2 |
10227113 14998318 7531353 18448342 9430133 11170639 14642972 12873512 7861418 19072656 8997630 19110341 15771415 8822531 20719507 9876110 11132243 15324906 8632342 12190308 18595716 20827463 7520908 15992090 15745831 23241029 10991983 1346637 7898773 8935801 8522988 15907153 |
|
5-hydroxytryptamine receptor 2A Alpha-1A adrenergic receptor D(2) dopamine receptor Histamine H1 receptor Alpha-1B adrenergic receptor Beta-1 adrenergic receptor |
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. |
10227113 15664832 14998318 17111172 16513859 11170639 7861418 8997630 14530903 15771415 23043306 8813537 11132243 8632342 8925876 17316700 19910723 18595716 16314884 17016423 17059881 7520908 15992090 12176106 14610521 16730699 7691623 11752352 17311076 15140279 17139284 8935801 9197279 |
Risperidone Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Cocaine dependence | 22.65 |
|
Schizophrenia | 20.31 |
|
Amphetamine-Related Disorders | 19.44 | |
Bipolar disorder | 15.42 |
|
Pheochromocytoma | 15.38 |
|
Parkinson's disease | 14.76 |
|
Alzheimer's Disease | 14.04 |
|
Obesity | 13.52 |
|
Autism | 12.1 |
|
Reperfusion Injury | 10.79 |
|
Diabetes Mellitus, Type 2 | 10.06 |
|
Hepatocellular carcinoma | 9.45 |
|
Muscular Atrophy | 9.3 |
|
Metabolic Syndrome X | 8.85 |
|
Basal Ganglia Diseases | 8.84 |
|
Metabolic Diseases | 8.84 |
|
Familial Testotoxicosis | 8.81 |
|
Infertility, Female | 8.8 |
|
Heroin Dependence | 8.68 |
|
Anorexia nervosa | 8.46 |
|