Pimavanserin

Products

Pimavanserin was approved in the United States in 2016 in tablet form (Nuplazid). It has not yet been registered in many countries.

Structure and properties

Pimavanserin (C25H34FN3O2, Mr = 427.6 g/mol) is present in the drug as pimavanserine tartrate, which is highly soluble in water. It is a urea, fluorobenzyl, and piperidine derivative.

Effects

Pimavanserin (ATC N05AX17) has antipsychotic properties. The effects are due to inverse agonism/antagonism at the serotonin 5-HT2A receptor. Unlike other neuroleptics, it is selective for this receptor and is therefore potentially better tolerated. It does not interact with dopamine receptors, muscarinic receptors, histamine receptors, adrenergic receptors, or calcium channels. Pimavanserin has an active metabolite (AC-279) and a long half-life of 57 hours (metabolite: 200 hours).

Indications

For the treatment of hallucinations and delusions associated with psychosis in Parkinson’s disease.

Dosage

According to the SmPC. Tablets are taken once daily, independent of meals.

Contraindications

Pimavanserin is contraindicated in case of hypersensitivity. Full precautions can be found in the drug label.

Interactions

Pimavanserin is metabolized predominantly by CYP3A4 and by CYP3A5, and corresponding drug-drug interactions are possible. Pimavanserin should not be combined with other agents that prolong the QT interval.

Adverse Effects

The most common possible adverse effects include peripheral edema and confusion. Pimavanserin prolongs the QT interval.