pimavanserin NUPLAZID

Class: 5HT2A Receptor Inverse Agonist
FDA Indications: Parkinsons Disease Psychosis
Off-Label Use: Agitation In Alzheimers Disease
Prescribing
Forms: 17mg tablet
Dose Range: 34 mg/day
Starting: 17 mg po bid
Stopping: Taper 6-8 weeks, rapid d/c can lead to rebound psychosis

NAMI drug fact sheet

Precautions
Contraindications: Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Pimavanserin is not approved for the treatment of patients with dementia-related psychosis unrelated to the hallucinations and delusions associated with Parkinson's disease psychosis
Possible Risk of TdP, Drugs to Avoid in Congenital Long QT
Side Effects: confusion, nausea, orthostatic hypotension, peripheral edema
Pharmacodynamics
1° MOA: 5HT2A/2C inverse agonist / antagonist
Target: 5HT2A >> 5HT2C > σ1 (inverse agonism and antagonism)
Pharmacokinetics
t½: 57° TMAX:
Substrate of: 3A4, 3A5; 2J2, 2D6
Inhibits: ∅ ; Induces:
Active Metabolites: AC-279
DDIs
Misc
  • - pimavanserin is the first-ever approved treatment for hallucinations and delusions associated with Parkinson's disease psychosis
  • - since pimavanserin is not dopaminergic, it does not worsen motor symptoms of PD
  • - based on its 5HT2A inverse agonism, it may have potential for treating symptoms associated with the use of hallucinogen drugs and for treating akathisia associated with antipsychotic medications
Special Populations

Category Undefined.—No human data available. No teratogenic effect in animal studies

No data available


All atypicals may increase mortality in elderly patients by 1.7 times greater than placebo.

No dosage adjustment for pimavanserin is needed in patients with mild to moderate renal impairment. Use of pimavanserin is not recommended in patients with severe renal impairment.

Use of pimavanserin is not recommended in patients with hepatic impairment.

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Last updated January 20 2018 15:32:06. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.