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 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 (↑ 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.

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 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:

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

Drug-Natural Products:

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

Drug-Food:

Grapefruit juice may ↑ levels and risk of toxicity; 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.
Perform ECG if patient has a history of cardiac disease to monitor for prolong QT interval.
Monitor for hypersensitivity reactions (rash, urticaria, symptoms consistent with angioedema [tongue swelling, circumoral edema, throat tightness, dyspnea]).

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 ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy. Instruct patient to take pimavanserin as directed.
Instruct patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider before taking any new medications, especially St. John's wort.
Advise patient to notify health care provider of palpitations, chest pain, fatigue, or hypersensitivity reactions and to seek immediate medical attention if needed.
Advise patient to avoid grapefruit or grapefruit juice.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇