ABSTRACT
Pimavanserin is a selective 5-HT2A receptor inverse agonist approved by FDA on April 29, 2016, and it is the first drug for the treatment of hallucinations and delusions associated with Parkinson' s disease. Pimavanserin is with high safety, good toleration and promising clinical efficiency, which is a timely option to resolve the drug shortage in clinic treatment. This paper summarized its pharmacodynamics, pharmacokinetics, clinical studies, adverse reactions and drug interactions.
ABSTRACT
A simple, rapid and sensitive method based on an ultra-performance liquid chromatography–tandem mass spectrometry(UPLC–MS/MS)has been developed and validated for the determination of pimavanserin in rat plasma.The analyte was extracted by protein precipitation with methanol and separated on an ACQUITY BEH C18column(100 mm×2.1 mm,1.7μm;Waters,USA),with an isocratic elution of acetonitrile-water containing 10 mM ammonium acetate (70:30, v/v), at a flow rate of 0.2 mL/min for 2.5 min. The analyte and clarithromycin (the internal standard) were detected and quantified in positive ion mode using multiple reaction monitoring transitions at m/z 428.2 → 223.0 for pimavanserin and m/z 748.5 → 589.5 for clarithromycin. Relative coefficient (r) for the calibration curve was more than 0.9980. The intra-day and inter-day precisions(relative standard deviation,RSD%)were less than 13.3% and 10.5%,respectively,and the accuracy(relative error,RE%)was within ± 11.5%.The analytical method was successfully applied to a routine pharmacokinetic study of pimavanserin in rats after oral administration at the dose of 10 mg/kg.
ABSTRACT
Parkinson’s disease is often associated with hallucinations and psychosis. Till now typical and atypical antipsychotics (Clozapine & Quetiapine) are being used to manage these symptoms. Recently US FDA has approved a new drug Pimavanserin for the treatment of hallucination and delusion associated with parkinson’s disease psychosis in a dose of 34 mg.
ABSTRACT
Pimavanserin(Nuplazid) is a drug of selective targeting 5-HT2A receptor, developed by Acadia Pharmaceuticals. In April 29, 2016, it was approved by FDA for the treatment of Parkinson’s disease (PD) patients experiencing mental symptoms such as hallucinations and delusions. In this paper, we summarize the synthetic methods of pimavanserin published in literature in recent years and their advantages and disadvantages.
ABSTRACT
Pimavanserin(Nuplazid) is a drug of selective targeting 5-HT2A receptor,developed by Acadia Pharmaceuticals. In April 29,2016,it was approved by FDA for the treatment of Parkinson′s disease(PD)patients experiencing mental symptoms such as hallucinations and delusions. In this paper,we summarize the synthetic methods of pimavanserin published in literature in re?cent years and their advantages and disadvantages.