Abstract

Pungsh Tadar, Manikanta Murahari and Mohammad Azamthulla*

ABSTRACT

5-HT3 receptor antagonist have major role play in the management of neuro psychiatric and GIT disorders. Palonosetron is a newly generated 2nd generation of 5HT3 receptor antagonist. FDA first approved Palonosetron in 2003 for prevention of acute nausea and vomiting associated with chemotherapy and used as antiemetic agent. It also used in pediatric patients to control sickness. The first generation of 5-HT3 receptor antagonist such as ondansetron, granisetron, dolasetron and tropisetron are found to have similar efficacies in preventing acute cancer induced nausea and vomiting. Palonosetron hydrochloride is white to grayish, non-hygroscopic, glasslike powder, uninhibitedly dissolvable in water and dissolvable in methanol. It has two chiral focuses while the dynamic substance in the item comprises of a solitary stereoisomer. Palonosetron hydrochloride is known to show polymorphism. Its chemical name is (3aS)- 2-[(3S)- 1-azabicyclo[2.2.2]oct-3-l]- 2,3,3a,4,5,6-hexahydro-1H-benz[de]-isoquinolin-1-one hydrochloride relating to the atomic equation C19H24N2O·HCl and has an overall sub-atomic mass of 332.87g/mol. The pharmacokinetics of Palonosetron have half-life around 40 hours and shows to be broadly appropriated in the body, bound to plasma proteins at an extent of 62%, processed by cytochrome P450 compounds, basically CYP2D6, with minor commitments from CYP1A2 and CYP3A4 and eliminates through urine. This review highlights the therapeutic, pharma kinetic and pharmacological properties of palonosetron that have been reported since 2003 and also displays the gaps in our knowledge about both the compounds and its characteristic limitations which deserves more exploration.