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| Clinical data | |
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| Pregnancy category |
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| Routes of administration | Oral and extended-release intramuscular injection |
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| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | 70% (oral) |
| Metabolism | Hepatic (CYP2D6-mediated) |
| Elimination half-life | 3–20 hours |
| Excretion | Urinary |
| Identifiers | |
IUPAC name
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.114.705  |
| Chemical and physical data | |
| Formula | C23H27FN4O2 |
| Molar mass | 410.485 g/mol g·mol |
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, obsessive-compulsive disorder 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.
Risperidone is now the most commonly prescribed antipsychotic medication in the United States.
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 such as retrograde ejaculation.
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.
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.
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.
References
- "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
- "FDA Approves the First Drug to Treat Irritability Associated with Autism, Risperdal" (Press release). FDA. October 2 2006. Retrieved 2006-10-02.
{{cite press release}}: Check date values in:|date=(help) - Szarfman A, Tonning J, Levine J, Doraiswamy P (2006). "Atypical antipsychotics and pituitary tumors: a pharmacovigilance study". Pharmacotherapy. 26 (6): 748–58. PMID 16716128.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - "FDA Warning Letter" (Press release). FDA. April 19 2004. Retrieved 2006-10-02.
{{cite press release}}: Check date values in:|date=(help)
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.