Risperidone detailed information

Risperidone detailed information

File:Risperidone.svg
File:Risperdal.gif
Clinical data
Pregnancy category	C
Routes of administration	Oral and extended-release intramuscular injection
ATC code	N05AX08 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	70% (oral)
Metabolism	Hepatic (CYP2D6-mediated)
Elimination half-life	3–20 hours
Excretion	Urinary
Identifiers
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
CAS Number	106266-06-2
PubChem CID	5073
DrugBank	APRD00187
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C23H27FN4O2
Molar mass	410.485 g/mol

Risperdal tablets

Risperidone (pronounced Ris-PER-ǐ-dōn and sold under the trade name Risperdal in the United States, Canada, the United Kingdom, Portugal and several other countries, Risperdal or Ridal in New Zealand, Rispolept in Eastern Europe, and Belivon, or Rispen elsewhere) is an atypical antipsychotic medication developed by Janssen Pharmaceutica. It was approved by the United States Food and Drug Administration (FDA) in 1993 for the treatment of schizophrenia. On Wednesday, August 22, 2007, Risperdal was approved as the only drug agent available for treatment of schizophrenia in children ages 13–18; it was also approved that same day for treatment of bipolar disorder in youths ages 10–18, joining lithium. Risperidone contains the functional groups of benzisoxazole and piperidine as part of its molecular structure. In 2003 the FDA approved risperidone for the short-term treatment of the mixed and manic states associated with bipolar disorder. In 2006 the FDA approved risperidone for the treatment of irritability in children and adolescents with autism. Like other atypical antipsychotics, it has also been used "off-label" for the treatment of anxiety disorders, such as Obsessive-Compulsive disorder; severe, treatment-resistant depression with or without psychotic features; Tourette's disorder; disruptive behavior disorders in children; and eating disorders, among others.

Janssen's patent on Risperdal expires on December 29, 2007, opening the market for cheaper generic versions of the drug from other companies; however, Janssen will continue to have exclusive marketing rights until June 29, 2008, as the result of a pediatric extension.

Risperidone is available as a tablet in 0.25, 0.5, 1, 2, 3 and 4 mg sizes, and as a 25 mg, 37.5 mg or 50 mg ampoule Risperdal Consta, which is a depot injection administered once every two weeks. It is also available as a wafer known in the United States as Risperdal M-Tabs and elsewhere as Risperdal Quicklets.

Side effects

Common side effects include akathisia, anxiety, insomnia, low blood pressure, muscle stiffness, muscle pain, sedation, tremors, increased salivation, and stuffy nose. Risperidone has been associated with minimal to moderate weight gain, with one study finding that 26 to 38 percent of participants on the drug experienced weight gain. 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. Template:Refs

Pharmacology

File:Risperidone-icon.jpg

Risperidone's receptor profile Template:Ifdc

Risperidone is a strong dopamine blocker (antagonist); i.e., it inhibits functioning of postsynaptic dopamine receptors.

Risperidone also acts as a 5-HT_2A antagonist, and can be used to quickly and effectively block the effects of 5-HT_2A agonist drugs such as LSD. However, the use of antipsychotics on people under the influence of LSD is reportedly extremely unpleasant, with some describing it as a "chemical straitjacketTemplate:Citequote". As a result, diazepam is often recommended to reduce the anxiety of a bad trip.

It reaches peak plasma levels quickly regardless of whether it is administered as a liquid or pill. 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.

An intramuscular preparation, marketed as Risperdal Consta, can be given once every two weeks. It is slowly released from the injection site. It can be useful in patients who have difficulty taking oral medication for any reason. Some people prefer a once-every-two-weeks injection to daily pills. It also helps the physician insure compliance. Doses range from 25 to 50 mg given as an intramuscular injection once every two weeks.

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.