Risperidone
From Wikipedia, the free encyclopedia
| |
| Risperidone
| |
| Systematic (IUPAC) name | |
| 4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)- 1-piperidyl]ethyl]-3-methyl- 2,6-diazabicyclo[4.4.0]deca-1,3-dien-5-one | |
| Identifiers | |
| CAS number | 106266-06-2 |
| ATC code | N05AX08 |
| PubChem | 5073 |
| DrugBank | APRD00187 |
| Chemical data | |
| Formula | C23H27N4FO2 |
| Mol. weight | 410.485 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 70% (oral) |
| Metabolism | Hepatic (CYP2D6-mediated) |
| Half life | 3–20 hours |
| Excretion | Urinary |
| Therapeutic considerations | |
| Pregnancy cat. |
C |
| Legal status |
℞ Prescription only |
| Routes | Oral and extended-release intramuscular injection |
Risperidone (Belivon®, Rispen®, Risperdal® in the United States) is an atypical antipsychotic medication developed by Janssen Pharmaceutica. It was approved by the United States Food and Drug Administration (FDA) in 1993. It is most often used to treat delusional psychosis (including schizophrenia), but risperidone (like other atypical antipsychotics) is also used to treat some forms of bipolar disorder, psychotic depression and Tourette syndrome.
Generally lower doses are used for autistic spectrum disorders than are used for schizophrenia and other forms of psychosis; risperidone has received approval from the Food and Drug Administration (FDA) for symptomatic treatment of irritability in autistic children and adolescents.<ref name="Samuel Curtis">FDA (October 2 2006). FDA Approves the First Drug to Treat Irritability Associated with Autism, Risperdal. Press release. Retrieved on 2006-10-02.</ref>
Risperidone is now the most commonly prescribed antipsychotic medication in the United States.
Contents |
[edit] Side effects
Common side effects include nausea, anxiety, dizziness, insomnia, low blood pressure, muscle stiffness, muscle pain, sedation, tremors, increased salivation and weight gain (it is not uncommon for patients taking risperidone over long periods to gain upwards of 50 pounds or even more). It has also been known to cause sexual dysfunction.
Occasionally breast tenderness and eventually lactation in both genders may occur. Many antipsychotics are known to increase prolactin because they inhibit dopamine. However, Risperidone is known to increase prolactin to a greater extent than most other antipsychotics, such as quetiapine. It is thought that once Risperidone raises prolactin, it may cause tumors in the pituitary gland. This may recur even if the patient has switched to a different antipsychotic.<ref name="Szarfman2006">Szarfman A, Tonning J, Levine J, Doraiswamy P (2006). "Atypical antipsychotics and pituitary tumors: a pharmacovigilance study.". Pharmacotherapy 26 (6): 748-58. PMID 16716128.</ref>
Like all antipsychotics, Risperidone can potentially cause tardive dyskinesia (TD), extrapyramidal symptoms (EPS), and neuroleptic malignant syndrome (NMS), although the risk is generally less than for the older typical antipsychotics.
Also, like all atypical antipsychotics, risperidone can trigger diabetes and more serious conditions of glucose metabolism, including ketoacidosis and hyperosmolar coma.<ref name="warning">FDA (April 19 2004). FDA Warning Letter. Press release. Retrieved on 2006-10-02.</ref>
[edit] Pharmacology
Risperidone is a very strong dopamine blocker (antagonist); i.e., it inhibits functioning of postsynaptic dopamine receptors.
Risperidone also acts as a 5-HT2A antagonist, and can be used to quickly and effectively block the effects of 5-HT2A agonist drugs such as LSD.
It reaches peak plasma levels quickly regardless of whether it is administered as a liquid or pills. The strong dopamine-blocking reaction is known to make some people feel nauseated if they do things that normally trigger the dopamine response, such as eat a pleasing meal or experience orgasm. Risperidone is metabolised fairly quickly so this potential for nausea subsides usually in two to three hours.
[edit] References
[edit] External links
- Drugs.com Professional information on Risperidone
- Drugs.com Consumer information on Risperidone
- Janssen L.P. official web site on Risperdal (Risperidone)
- PubChem Substance Summary: Risperidone National Center for Biotechnology Information.
fr:Rispéridone nl:Risperidon ja:リスペリドン ru:Рисперидон fi:Risperidoni sv:Risperidon zh:利培酮
