Pimavanserin: Difference between revisions
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Create Pimavanserin page (Stahl-sourced detail with skepticism) |
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| pregnancy = Limited data; avoid | | pregnancy = Limited data; avoid | ||
| legal = Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) | | legal = Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) | ||
| intro = '''Pimavanserin''' (brand name Nuplazid) is the only FDA-approved | | intro = '''Pimavanserin''' (brand name Nuplazid) is the only FDA-approved medicine for the treatment of hallucinations and delusions in Parkinson's disease psychosis (approved April 2016). Unlike every other approved antipsychotic, it has '''no D2 dopamine receptor activity''' — a critical feature in Parkinson's, where conventional D2 antagonists worsen motor symptoms. Mechanism: selective 5HT2A inverse agonism with weaker 5HT2C inverse agonism. Carries the class black-box warning for increased mortality when used in elderly dementia-related psychosis, though it has been studied in that population and is investigational for dementia psychosis. Also studied as augmentation for major depression with positive preliminary results. | ||
| pharmacodynamics= Selective 5HT2A inverse agonist (Ki ~0.4 nM). Weaker 5HT2C inverse agonism. No significant binding at D2, muscarinic, adrenergic, or histaminergic receptors. The lack of D2 activity preserves dopaminergic function (essential in PD) while reducing the 5HT2A-mediated psychotic symptoms. | | pharmacodynamics= Selective 5HT2A inverse agonist (Ki ~0.4 nM). Weaker 5HT2C inverse agonism. No significant binding at D2, muscarinic, adrenergic, or histaminergic receptors. The lack of D2 activity preserves dopaminergic function (essential in PD) while reducing the 5HT2A-mediated psychotic symptoms. | ||
| effects = Peripheral edema, confusion, nausea, constipation, gait disturbance, hallucinations (paradoxically reported), QT prolongation (avoid combination with other QT-prolonging | | effects = Peripheral edema, confusion, nausea, constipation, gait disturbance, hallucinations (paradoxically reported), QT prolongation (avoid combination with other QT-prolonging medicines). | ||
| interactions = <pharmaInteractions/> | | interactions = <pharmaInteractions/> | ||
}} | }} | ||