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Re: low dose risperdal as dopamine agonist?

Posted by Phillipa on October 2, 2007, at 13:31:34

In reply to low dose risperdal as dopamine agonist?, posted by nellie7 on October 2, 2007, at 8:35:51

Here's some more info. Phillipa

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Systematic (IUPAC) name
CAS number 106266-06-2
ATC code N05AX08
PubChem 5073
DrugBank APRD00187
Chemical data
Formula C23H27FN4O2
Mol. mass 410.485 g/mol
Pharmacokinetic data
Bioavailability 70% (oral)
Metabolism Hepatic (CYP2D6-mediated)
Half life 320 hours
Excretion Urinary
Therapeutic considerations
Pregnancy cat. C

Legal status ℞ Prescription only

Routes Oral and extended-release intramuscular injection

Risperdal tabletsRisperidone (pronounced Ris-PER-ǐ-dōn and sold under the trade name Risperdal in the United States, Canada, the United Kingdom 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[1] 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 1318; it was also approved that same day for treatment of bipolar disorder in youths ages 1018, 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.[2]

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 Risperdal Quicklets.

Contents [hide]
1 Side effects
2 Pharmacology
3 References
4 External links

[edit] 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.[3] 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.[4]

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.[5]

[edit] Pharmacology

Risperidone's receptor profile

The image above is proposed for deletion. See images and media for deletion to help reach a consensus on what to do.Risperidone is a 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. However, the use of antipsychotics on people under the influence of LSD is reportedly extremely unpleasant, with some describing it as a "chemical straitjacket[cite this quote]". As a result, diazepam is often recommended to reduce the anxiety of a bad trip.[citation needed]

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.




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