Asenapine structure

Drug of the Month:
Asenapine (Saphris)

A new sedating dopamine blocker without metabolic harms



Biological mechanism

Asenapine is a dopamine blocker with potent D2 receptor blockade, along with strong antiadrenergic effects.  The D2 blockade is dose dependent, such that at 10-20 mg/d, over 90% of D2 receptors are blocked.  This level of D2 blockade produces extrapyramidal symptoms (EPS) such as akathisia, which appears to be the main clinical problem with this agent, as with the entire dopamine blocker class.

Like all modern dopamine blockers, it also has serotonin-2 receptor blockade, but it seems to have little to no  weight gain.  Asenapine does not have apparent anti-insulin effects,  and thus it does not appear to cause or worsen the metabolic syndrome of diabetes, hypertension, and hyperlipidemia. 

It has moderate anti-alpha adrenergic effects, like risperidone. This effect may be a mechanism for notable...

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