Pimavenserin mode of action
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pimavanserin prescribing information mechanism action 5-HT2A inverse agonist
Pimavanserin is a selective serotonin-modulating antipsychotic used for hallucinations and delusions in Parkinson disease psychosis.
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It acts primarily as an inverse agonist and antagonist at serotonin 5-HT2A receptors.
- Antagonism blocks serotonin-driven receptor activation.
- Inverse agonism also reduces the receptor's baseline, constitutive signaling, even when serotonin is not bound.
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It has lower-affinity activity at 5-HT2C receptors.
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It has negligible dopamine D2 receptor affinity, unlike most antipsychotics. Therefore, it is less likely to worsen parkinsonian motor symptoms such as bradykinesia, rigidity, and tremor.
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It also has no appreciable clinically relevant binding to muscarinic, histamine, adrenergic, or 5-HT2B receptors. The FDA notes that the precise clinical mechanism remains unclear, but its effect is thought to result from 5-HT2A inverse agonism/antagonism, with lesser 5-HT2C activity, as described in the FDA prescribing information.
One-line exam answer:
Pimavanserin is a selective 5-HT2A inverse agonist and antagonist with lesser 5-HT2C activity and essentially no D2 blockade, treating Parkinson disease psychosis without worsening motor function.
Pimavanserin is a selective 5-HT2A inverse agonist and antagonist with lesser 5-HT2C activity and essentially no D2 blockade, treating Parkinson disease psychosis without worsening motor function.
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