Generic
Pimavanserin
2 brands available in the market
At a glance
Pimavanserin is used for the treatment of hallucinations and delusions associated with Parkinson's disease psychosis. It is a selective serotonin inverse agonist and antagonist that targets 5-HT2A receptors believed to play an important role in psychosis.
Description
The mechanism of action of pimavanserin is not fully understood, but it may work through inverse agonist and antagonist activity at serotonin 5-HT2A receptors and to a lesser extent at 5-HT2C receptors. It helps reduce hallucinations and delusions associated with Parkinson's disease psychosis.
Indications
- Hallucinations and delusions associated with Parkinson's disease psychosis
Therapeutic class
Antiparkinson drugs
Pharmacological class
5-HT2A Receptor Inverse Agonist/Antagonist
Pharmacology
Pimavanserin is a selective serotonin inverse agonist and antagonist that targets 5-HT2A receptors. It works through inverse agonist and antagonist activity at these receptors, helping to reduce hallucinations and delusions associated with Parkinson's disease psychosis.
Mechanism of action
Reduces psychosis symptoms by blocking 5-HT2A receptors.
Dosage
Adult Dose (Oral):
- Parkinson disease psychosis: 34 mg once daily (two 17 mg tablets), without titration
- Hepatic impairment: No dosage adjustment recommended (not recommended)
- With strong CYP3A4 inhibitors: Reduce dose to 17 mg once daily
Administration
- May be taken with or without food
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Side Effects (1-10%):
- Nausea (7%)
- Peripheral edema (7%)
- Confusional state (6%)
- Hallucinations (5%)
- Constipation (4%)
- Gait disturbance (2%)
Precautions & warnings
- Antipsychotic drugs increase all-cause risk of death in elderly patients with dementia-related psychosis
- QT interval prolongation; avoid in known QT prolongation, with Class 1A/3 antiarrhythmics, certain antipsychotics, certain antibiotics
- Avoid in history of cardiac arrhythmias, symptomatic bradycardia, hypokalemia, hypomagnesemia, congenital QT prolongation
- Strong CYP3A4 inhibitors/inducers affect systemic exposure
Contraindications
- Documented hypersensitivity reaction to drug or components (rash, urticaria, angioedema)
Drug interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole): Increase pimavanserin exposure; reduce dose to 17 mg/day
- Strong CYP3A4 inducers: May reduce pimavanserin exposure
- Carbidopa/levodopa: No dose adjustment required
Food interactions
Food does not affect absorption; it is not known whether it is safe to consume alcohol.
Use in pregnancy
Use in Pregnancy: No data for use in pregnant women to assess drug-associated risk; animal studies showed no adverse effects during organogenesis at up to 10-12 times the 34 mg/day MRHD.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if distributed in human breast milk; consider developmental and health benefits, maternal clinical need, and potential adverse effects on the breastfed infant.
Pediatric use
Safety and effectiveness not established in pediatric patients.
Geriatric use
No dose adjustment required for elderly patients.
Renal / hepatic impairment
Renal Impairment: Mild-to-moderate (CrCl ≥30 mL/min): No dose adjustment required; Severe (CrCl <30 mL/min) or end stage renal disease: Use with caution.
Hepatic Impairment: Not recommended in hepatic impairment (not evaluated).
Overdose effects
No overdose information available; consult your doctor if taken in excess.
Storage conditions
Store below 30°C, away from light and moisture; keep out of reach of children.
Chemical structure
Pimavanserin