aripiprazole mech

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MudPhud20XX

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Hi all,

This is not in FA, but was asked in nbme.

The mech of Aripiprazole?

Is the reason you get less of NMS or EPS, is that b/c Aripiprazole is a partial agonist to D2 receptor? Or it reversibly binds to D2?

Many thanks in advance.
 
This is a throwback to my undergrad days in Neuroscience, but I believe it's a dopamine partial agonist. The key to understanding its utility as an antipsychotic is that most schizophrenics have decreased DA neurotransmission in the mesocortical pathway (negative symptoms), but increased DA neurotransmission in the mesolimbic pathway (positive symptoms). Aripiprazole helps mediate both decreased and increased dopaminergic transmission - like adding lukewarm water to an ice bath to warm it up, and lukewarm water to a hot bath to cool it down
 
Dude where do you get all this stuff from ?
I mean the 5HT2a antagonist..
i mean what do you read ?
Dr. Lionel Raymon's pharmacology eCoach.

All atypical antipsychotics share 5HT2a antagonism with variable D2 antagonism.
 
Yeah, the much more important point about atypical antipsychotics is that they are all 5-HT2 antagonists (and 5-HT2 controls DA release in the different dopamine pathways). The relative ration of 5-HT2 receptors to D2 receptors in the different pathways allows 5-HT2 inhibitors (atypicals) to work and also have less side effects.
 
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