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Medicines > generic: None & classes : Neuroleptic or Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism)

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generic: (Click arrow to add another value)
brand:
Nuplazid (1)
classes: (Click arrow to add another value)
mechanism:
Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (1)
uses:
Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1)
starting dose:
34 mg PO once daily (1)
preparations:
10 mg, 34 mg capsules/tablets (1)
fda max:
34 mg/d (1)
routes:
Oral (1)
onset:
Benefit over weeks of dosing (1)
duration:
Daily dosing (1)
halflife:
~57 hours (parent), ~200 h (active metabolite) (1)
bioavailability:
Not characterized; oral dosing once daily (1)
pregnancy:
Limited data; avoid (1)
legal:
Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1)

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