Risperidone
- Atc Codes:N05AX08
- CAS Codes:106266-06-2
- PHARMGKB ID:106266-06-2
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Aleptan, RisPel, Risperdal, Risperidon, Risperihex, Risperinorm, Risperipharm; Belgium: Risperdal, Risperidone; Bulgaria: Neorisp, Resperon, Ridonex, Rileptid, Rispen, Risperidon, Risperidone, Rispolept, Rispolux, Rissar, Risset, Speridan, Torendo-Q; Cyprus: Eperon, Rispelyt, Risperdal, Risperidone; Czech Republic: Apo-Risper, Medorisper, Ridoner, Rigenin, Rileptid, Risepro, Rispalan, Rispemar, Rispen, Rispera, Risperdal, Risperidon, Risperigamma, Risperstad, Rispimed, Rispolux, Risset, Torendo, Unispera; Denmark: Risperanne, Risperdal, Risperidon, Rispolept; Estonia: Aleptolan, Medorisper, Rigenin, Rispen, Risperidon, Risperidone, Rispolept, Risset, Ristad, Rixon, Torendo-Q; Finland: Risperdal, Risperidon, Risperidone; France: Risperdal, Risperidone; Germany: Aceperidon, Belivon, Delperal, Midason, Psycharisp, Rehablit, Risocon, Rispacarm, Rispas, Rispastedt, Rispcon, Rispe-Q, RispeCare, Risperac, Risperdal, Risperdoc, Risperidon, Risperigamma; Greece: Axelabron, Belasperdal-S, Capulton, Deteron, Dixine, Evitrat, Helposper, Isipredon, Lassen, Leterzin, Linipon, Lucipral, Muistin, Natibo, Psychordal, Ribex, Ridoron, Rifocus, Ripepral, Risenar, Risidral, Rispelen, Risperascol, Risperdal, Risperidone, Risperom, Risperoprol, Rispersan, Rispenet, Rispogen, Rubrum, Speralax, Wisperdon, Zafitral; Hungary: Hunperdal, Perdox, Perigen, Prospera, Rileptid, Ripedon, Risperdal, Risperidon, Rispimed, Rispolux, Rispons, Rosipin, Stadarisp, Torendo-Q, Ziperid; Ireland: Perdamel, Resdal, Risdone, Rispal, Rispatal, Risperdal, Risperger, Risperidone, Rispeva; Italy: Belivon, Risperdal, Risperidone; Latvia: Aleptolan, Medorisper, Rigenin, Rileptid, Rispaxol, Risperidon, Risperidone, Risperigamma, Rispolept, Risset, Ristad, Rixon, Torendo-Q; Lithuania: Aleptolan, Medorisper, Rigenin, Rileptid, Rispen, Risperidon, Risperidone, Rispolept, Rispolept, Risset, Ristad, Rixon, Torendo; Luxembourg: Risperdal; Malta: Nodiril, Risperdal, Risperidone; Netherlands: Risperdal, Risperidon, Rispimed, Torendo; Poland: Apo-Risperid, Disaperid, Doresol, Galperinon, Lioxam, Mepharis, Nodir, Orizon, Ranperidon, Ridonex, Rileptid, Rinter, Risnia, Rispen, Risperat, Risperatio, Risperidon, Risperidone, Risperiwin, Risperon, Rispimed, Rispofren, Rispolept, Rispolux, Risset, Ryspolit, Speridan, Stadarisp, Symperid, Torendo, Ziperid; Portugal: Lergitec, Neclav, Perdin, Risperdal, Risperidona, Zoridal; Romania: Essens, Ridonex, Rileptid, Rison, Rispemar, Rispen, Risperidona, Risperidone, Rispolept, Risset, Spring, Torendo, Xenoma; Slovakia: Medorisper, Risepro, Rispen, Risperdal, Risperidon, Risperidone, Rispimed, Rispolux, Risset, Stadarisp, Torendo, Unispera; Slovenia: Risperdal, Risperidon, Risperigamma, Rispolux, Rispons, Risset, Torendo; Spain: Arketin, Diaforín, Risperdal, Risperidona; Sweden: Ridalux, Rinarisp, Rispalan, Risperat, Rispercol, Risperdal, Risperidon, Risperoc; UK: Risperdal, Risperidone.
North America
Canada: Risperdal, Risperidone; USA: Risperdal.
Latin America
Argentina: Dozic-Raffo, Dropicine, Edalen, Restelea, Riatul, Risper 1, Risperdal, Risperidona, Risperin, Rispex, Roxodyn, Sequinan; Brazil: Respidon, Risperdal, Risperidon, Risperidona, Risperix, Viverdal, Zargus; Mexico: Reskizof, Risperdal, Rispolux.
Asia
Japan: Risperdal, Risperidone.
Drug combinations
Chemistry
Risperidone: C~23~H~27~FN~4~O~2~. Mw: 410.48. (1) 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-; (2) 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. CAS-106266-06-2 (1989).
Pharmacologic Category
Atypical Antipsychotics. Antimanic Agent. (ATC-Code: N05AX08).
Mechanism of action
A benzisoxazole atypical antipsychotic with mixed serotonin-dopamine antagonist activity which binds to 5-HT~2~-receptors in CNS and periphery with very high affinity. This antagonism is thought to improve negative symptoms of psychoses and reduce incidence of extrapyramidal side-effects. α~1~-, α~2~-adrenergic, and histaminergic receptors also antagonized with high affinity. Risperidone has low to moderate affinity for 5-HT~1C~, 5-HT~1D~, and 5-HT~1A~ receptors, weak affinity for D~1~ and no affinity for muscarinics or β~1~ and β~2~ receptors.
Therapeutic use
Treatment of schizophrenia. Treatment of acute mania or mixed episodes associated with bipolar I disorder (as monotherapy in children or adults, or in combination with lithium or valproate in adults). Treatment of irritability/aggression associated with autistic disorder.
Pregnancy and lactiation implications
Animal studies indicate increase in fetal mortality. Reversible EPS symptoms noted in neonates following use of risperidone during last trimester. Agenesis of corpus callosum also noted in one case report. There are no adequate, well-controlled studies in pregnant women. Risperidone may cause hyperprolactinemia (may decrease reproductive function in males and females). Not recommended in nursing women.
Unlabeled use
Treatment of Tourette’s disorder. Treatment of pervasive developmental disorder. Psychosis/agitation related to Alzheimer’s dementia.
Contraindications
Hypersensitivity to risperidone or any component of the formulation.
Warnings and precautions
Risperidone may alter cardiac conduction. Life-threatening arrhythmias occurred. Use caution with history of conduction abnormalities. Relative to other neuroleptics, risperidone has low risk of arrhythmias. May cause anticholinergic effects (confusion, agitation, constipation, xerostomia, blurred vision, urinary retention). Use with caution in decreased gastrointestinal motility, urinary retention, BPH, xerostomia, or visual problems. Relative to other neuroleptics, risperidone has low potency of cholinergic blockade. Antipsychotic use associated with esophageal dysmotility and aspiration (use with caution in risk of pneumonia (e.g. Alzheimer’s disease)). May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of these reactions generally much lower relative to typical/conventional antipsychotics). Risk of dystonia (and probably other EPS) may be greater with increased doses, use of conventional antipsychotics, males, and younger patients. Atypical antipsychotics associated with development of hyperglycemia (in some cases, may be extreme and associated with ketoacidosis, hyperosmolar coma, or death). Use with caution in diabetes or other disorders of glucose regulation. Use may be associated with neuroleptic malignant syndrome (risk may be increased in Parkinson’s disease or Lewy body dementia). May cause orthostatic hypotension. Use caution with history of cerebrovascular or cardiovascular disease (MI, heart failure, or ischemic disease). Rare cases of priapism reported. May be low-to-moderately sedating. Possibility of suicide attempt inherent in psychotic illness or bipolar disorder (use with caution in high-risk patients during initiation of therapy). Impaired core body temperature regulation may occur. Significant weight gain observed with antipsychotic therapy. Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at increased risk of death compared to placebo. An increased incidence of cerebrovascular adverse events (including fatalities) reported in elderly patients with dementia-related psychosis. Risperidone not approved for treatment of dementia-related psychosis. Use with caution in narrow-angle glaucoma (may be exacerbated by cholinergic blockade), and in hepatic disease or impairment. Elevates prolactin levels (effects seen in adults and children). Use with caution in breast cancer or other prolactin-dependent tumors, in myasthenia gravis (may be exacerbated by cholinergic blockade), in Parkinson’s disease, and in patients with renal disease; dosage reduction recommended. Use with caution in risk of seizures, including patients with history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. Elderly patients may be at increased risk of seizures due to increased prevalence of predisposing factors. May mask toxicity of other drugs or conditions (e.g. intestinal obstruction, Reye’s syndrome, brain tumor) due to antiemetic effects.