Improved prophylaxis of postoperative nausea vomiting: Palonosetron a novel antiemetic

Abstract

Many anti-emetics are used in clinical practice. Palonosetron hydrochloride is one of them. It is a novel, centrally acting antiemetic, and anti-nausea agent. This drug is an antagonist of serotonin receptor subtype 3 (5-HT3). This drug has longer duration of action which makes it useful in the prevention and treatment of acute and delayed onset of nausea and vomiting. This drug was initially used for chemotherapy induced nausea and vomiting. Federal drug agency (FDA) has approved it for prevention and treatment of post-operative nausea and vomiting. The literature search for this article was done using Google scholar and Pubmed using the terms “Palonosetron,” “longer duration of action,” “nausea,” “vomiting,” and “postoperative”.

Effects of palonosetron for prophylaxis of postoperative nausea and vomiting in high-risk patients undergoing total knee arthroplasty: A prospective, randomized, double-blind, placebo-controlled study

“…Along with the overall incidence of PONV, the incidences of both nausea and vomiting, respectively, were lower in the palonosetron group during the first 48 h postoperatively, notably during the 2–24 h. This concurs with reports that palonosetron is effective at preventing PONV compared with placebo [ 12 , 16 , 17 ], ondansetron [ 13 , 18 ], dexamethasone [ 19 ], and granisetron [ 18 ]. Palonosetron, a recently developed second-generation 5-HT 3 receptor antagonist, has greater binding affinity to the 5-HT 3 receptor more than 30-fold higher than that of ondansetron or ramosetron [ 20 ]. Palonosetron has a specific ternary ring moiety attached to the quinuclidine ring, therefore can bind more tightly to the receptor and multiple palonosetron molecules bind to a single receptor [ 20 ].…”

“…Palonosetron, a recently developed second-generation 5-HT 3 receptor antagonist, has greater binding affinity to the 5-HT 3 receptor more than 30-fold higher than that of ondansetron or ramosetron [ 20 ]. Palonosetron has a specific ternary ring moiety attached to the quinuclidine ring, therefore can bind more tightly to the receptor and multiple palonosetron molecules bind to a single receptor [ 20 ]. This allosteric binding and positive cooperativity, which are structurally distinct from the first-generation drugs, lead to effective treatment [ 21 ].…”