pimavanserin

Exact mechanism is unknown. May work by acting as an inverse agonist and antagonist primarily at 5-HT^2A receptors and less at 5–HT^2C receptors.

Therapeutic effects:

Reduced frequency and/or severity of hallucinations and delusions in patients with Parkinson's disease psychosis.

Pharmacokinetics ⬆ ⬇

Absorption: Unknown.

Distribution: Extensively distributed to tissues.

Protein Binding: 95%.

Metabolism/Excretion: Mostly metabolized by the liver (CYP3A4 and CYP3A5 isoenzymes) to an active metabolite. Primarily excreted in feces.

Half-Life: 57 hr (pimavanserin); 200 hr (active metabolite).

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	6 hr	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
QT interval prolongation;
Concurrent use of agents that prolong the QT interval, including sotalol, quinidine, disopyramide, procainamide, amiodarone, thioridazine, chlorpromazine, moxifloxacin, and ziprasidone (↑ risk of serious arrhythmias);
History of arrhythmias, including bradycardia;
Hypokalemia or hypomagnesemia (↑ risk of serious arrhythmias);
Congenital long QT syndrome (↑ risk of serious arrhythmias);
Severe renal impairment (CCr <30 mL/min).

Use Cautiously in:

OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children;
Geri: Appears on Beers list. risk of stroke, cognitive decline, and mortality in older adults with dementia. Avoid use in older adults, except for psychosis in Parkinson's disease.

Adv. Reactions/Side Effects ⬆ ⬇

CV: peripheral edema, QT interval prolongation, TORSADES DE POINTES

GI: constipation, nausea

Neuro: confusion, gait disturbance, hallucinations

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of amiodarone, sotalol, quinidine, disopyramide, procainamide, thioridazine, chlorpromazine, moxifloxacin, and ziprasidone↑ the risk of serious ventricular arrhythmias and should be avoided.
Strong CYP3A4 inhibitors, including clarithromycin, itraconazole, and ketoconazole, may ↑ levels; ↓ dose of pimavanserin.
Strong CYP3A4 inducers, including carbamazepine, phenytoin, and rifampin as well as moderate CYP3A4 inducers, including efavirenz, modafinil, nafcillin, and thioridazine may ↓ levels; avoid concurrent use.

Drug-Natural Products:

St. John's wort may ↓ levels; avoid concurrent use.

Route/Dosage ⬆ ⬇

PO (Adults ): 34 mg once daily. Concurrent use of strong CYP3A4 inhibitors: 10 mg once daily.

Availability ⬆ ⬇

(Generic available)

Capsules: 34 mg
Tablets: 10 mg

Assessment ⬆ ⬇

Assess mental status (orientation, mood, behavior) before and periodically during therapy.

Implementation ⬆ ⬇

PO: Administer 2 tablets once daily without regard to food.
- Capsules can be taken whole, or opened and entire contents sprinkled over a tablespoon (15 mL) of applesauce, yogurt, pudding, or a liquid nutritional supplement. Consume immediately without chewing; do not store for future use.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take pimavanserin as directed.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's wort.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇