Risperidone has been classified as a "qualitatively atypical" antipsychotic agent with a relatively low incidence of extrapyramidal side effects (when given at low doses) that has more pronounced serotonin antagonism than dopamine antagonism. Risperidone is unique among most other atypicals in that it has high affinity for the D2 receptor (also known as 'tight binding') whereas most other atypicals have 'loose binding' of the D2 receptor. It has actions at several 5-HT (serotonin) receptor subtypes. These are 5-HT2C, linked to weight gain, 5-HT2A, linked to its antipsychotic action and relief of some of the extrapyramidal side effects experienced with the typical neuroleptics.
- 5-HT1A serotonin receptors antagonist (Ki = 420nM)[24]
- 5-HT1D serotonin receptors antagonist (Ki = 100nM)[25]
- 5-HT2A serotonin receptors antagonist (Ki = 0.16nM)[24]
- 5-HT2C receptors antagonist (Ki = 26nM)[25]
- 5-HT7 irreversible antagonist[26]
- D1 dopaminergic receptors (Ki = 536 nM)[24]
- D1 receptor antagonist
- D5 receptor antagonist
- D2 dopaminergic receptors (Ki = 3.13 nM)
- D2 receptor antagonist
- D3 receptor antagonist
- D4 receptor antagonist
- α1 adrenergic antagonist (Ki = 0.8 nM)
- α1A
- α1B
- α1D subtypes
- α2 adrenergic antagonist (Ki = 7.54 nM)
- α2A
- α2B
- α2C subtypes
- H1 histamine receptor antagonist (Ki = 2.23 nM)
It reaches peak plasma levels quickly, regardless of whether it is administered as a liquid or pill. Risperidone is metabolized fairly quickly, so the potential for nausea subsides usually in two to three hours. However, the active metabolite, 9-hydroxy-risperidone, which has similar pharmacodynamics to risperidone, remains in the body for much longer, and has been developed as an antipsychotic in its own right, called paliperidone.
An intramuscular preparation, marketed as Risperdal Consta, can be given once every two weeks. It is slowly released from the injection site. This method of administration may be used on sanctioned patients who are declining, or consenting patients who may have disorganized thinking and cannot remember to take their daily doses.[27] Doses range from 12.5 to 50 mg given as an intramuscular injection once every two weeks.
I'm looking to ask my shrink for either Adderall XR or Focalin XR. Focalin XR has worked the best for me out of all the stims but will it's effectiveness be blocked by the Risperdone (4mg)?
