Palonosetron Exhibits Unique Molecular Interactions with the 5-HT3 Receptor

Rojas, Camilo; Stathis, Marigo; Thomas, Ajit G.; Massuda, Edward B.; Alt, Jesse; Zhang, Jie; Rubenstein, E. B.; Sebastiani, Silvia; Cantoreggi, Sergio; Snyder, Solomon H.; Slusher, Barbara S.

doi:10.1213/ane.0b013e318172fa74

Cited by 214 publications

(176 citation statements)

References 21 publications

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“…[13][14][15][16][17] Palonosetron may also have other advantages for perioperative care. For example, a recent study reported by Cho et al 34 found that palonosetron 0.075 mg iv administered before induction of anesthesia reduced injection pain associated with rocuronium administration; the NNT was 2.94.…”

Section: Discussionmentioning

confidence: 99%

“…Méthodes Nous avons effectué une recherche systématique dans les bases de données MEDLINE Ò , EMBASE TM , le Registre central Cochrane des essais cliniques contrô lés et Web of Science Ò pour identifier les essais randomisés contrô lés qui ont abordé la comparaison de l'efficacité antiémétique dans les 24 premières heures suivant une chirurgie, du palonosétron et de l'ondansétron administrés à titre prophylactique. Les principaux critères d'évaluation étaient le pourcentage de participants éprouvant des nausées postopératoires (NPO), des vomissements postopératoires (VPO) ou les deux, dans la période précoce (0-6 heures) ou tardive (6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24) Postoperative nausea and vomiting (PONV), the big ''little problem'', 1 is the most common postoperative medical problem. From the perspective of both patients and healthcare providers, prophylaxis of PONV is equally as important as postoperative analgesia.…”

Section: Résuméunclassified

“…13,14 In addition, Rojas et al [15][16][17] showed features that differentiate palonosetron from other 5-HT 3 RAs: allosteric binding and positive cooperativity with 5-HT 3 R, triggering of 5-HT 3 R internalization and prolonged inhibition of receptor function, and inhibition of substance P (a mediator of emesis)-mediated responses. [15][16][17] Due to these unique characteristics, palonosetron may be a promising agent that could achieve long-lasting efficacy in the prevention of PONV. Importantly, preliminary studies have already shown that palonosetron is safer and more effective than other 5-HT 3 RAs in preventing chemotherapy-induced nausea and vomiting, although this requires more rigorous confirmation.…”

Section: Résumémentioning

confidence: 99%

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Efficacy of palonosetron for preventing postoperative nausea and vomiting: a systematic review and meta-analysis

Xiong

et al. 2015

Can J Anesth/J Can Anesth

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Purpose Palonosetron, a second-generation 5-hydroxytryptamine 3 receptor antagonist (5-HT 3 RA), has unique characteristics relative to first-generation 5-HT 3 RAs such as ondansetron. Nevertheless, it remains unclear if palonosetron is better than ondansetron for the prevention of nausea and vomiting during the first 24 hr after surgery and is thus the focus of this systematic review. RésuméObjectif Le palonosétron est un antagoniste du récepteur de la 5-hydroxytryptamine 3 (5-HT 3 RA) de deuxième génération; il présente des caractéristiques uniques par rapport aux 5-HT 3 RA de première génération tels que l'ondansétron. Néanmoins, il n'est pas certain que le palonosétron est meilleur que l'ondansétron pour la prévention des nausées et vomissements au cours des 24 premières heures suivant une chirurgie et cela est donc l'objet de cette revue systématique. Méthodes Nous avons effectué une recherche systématique dans les bases de données MEDLINE Ò ,

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Section: Discussionmentioning

confidence: 99%

Section: Résuméunclassified

Section: Résumémentioning

confidence: 99%

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Efficacy of palonosetron for preventing postoperative nausea and vomiting: a systematic review and meta-analysis

Xiong

et al. 2015

Can J Anesth/J Can Anesth

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“…Our data indicate that palonosetron shows long-lasting activity that may be related to its longer half-life and its unique interaction with the 5-HT 3 receptor. 35 In fact, palonosetron seems to show positive cooperativity with the 5-HT 3 receptor, and thus the binding affinity increases, as additional palonosetron molecules become bound to the receptor. This characteristic, which is not shared by firstgeneration 5-HT 3 RAs, may partly account for the effective clinical control of CINV observed with palonosetron.…”

Section: Discussionmentioning

confidence: 99%

Palonosetron and dexamethasone for prevention of nausea and vomiting in patients receiving high-dose chemotherapy with auto-SCT

Musso

Scalone

Crescimanno

et al. 2009

Bone Marrow Transplant

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The aim of this study was to determine the efficacy of palonosetron combined with dexamethasone in prevention of chemotherapy (CT)-induced nausea and vomiting (CINV) in patients receiving high-dose (HD)-CT with auto-SCT, and the efficacy of a second dose of palonosetron in treating breakthrough emesis. One hundred thirty-four patients treated with HD-CT and auto-SCT for hematologic malignancies received palonosetron as prophylaxis for CINV on the first day of conditioning; patients were also administered dexamethasone throughout the entire period of conditioning. If breakthrough emesis occurred, a second dose of palonosetron was administered at 72 h after the first administration. Complete response and complete protection were observed in 36 and 26% of patients, respectively. One-half of the patients, re-treated with palonosetron for breakthrough emesis, were successfully rescued. Treatment with palonosetron plus dexamethasone seems to be encouraging in terms of prophylaxis of CINV and treatment of breakthrough emesis in the setting of HD-CT.

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“…Palonosetron (Pal), a novel 5-HT3 antagonist, is an effective antiemetic in the setting of PONV that also has advantages in treating PDNV due to its prolonged duration *Address correspondence to this author at the Department of Anesthesiology, NYU Langone Medical Center, 550 1 st Ave RR 605, New York, NY 10016; Tel: 212-263-0667; Fax: 212-263-3211; E-mail: Sorosch.Didehvar@nyumc.org of action. Palonosetron exhibits greater binding affinity and has a longer half-life than older 5-HT3 antagonists, possibly due to its binding of 5HT-3 receptors in an allosteric, positively cooperative manner [5][6][7]. Prior studies have demonstrated the advantages of a multimodal approach to the treatment of PONV, including a reduction in the incidence of PONV in high risk patients with the combination of 5-HT3 receptor antagonists and dexamethasone [8,9].…”

Section: Introductionmentioning

confidence: 99%

A Randomized, Double Blind Study to Evaluate the Efficacy of Palonosetron with Dexamethasone Versus Palonosetron Alone for Prevention of Post-Operative Nausea and Vomiting in Subjects Undergoing Bariatric Surgeries with High Emetogenic Risk

Didehvar

Viola-Blitz²,

Haile³

et al. 2013

TOATJ

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Abstract:Introduction: Postoperative (PONV) and postdischarge (PDNV) nausea and vomiting are common (60-70%) after bariatric surgery. Palonosetron (Pal), a novel 5-HT3 antagonist, is an effective antiemetic with a prolonged duration of action in the setting of PDNV. We hypothesized that combination therapy with Palonosetron (Pal) and dexamethasone (Dex) would improve treatment in comparison to Palonosetron alone in patients at high risk for PONV. Methods:In this study, patients undergoing bariatric laparoscopic surgery under general anesthesia, a subgroup of a larger Phase IV clinical trial of patients who had laparoscopic surgery, were randomized to 8 mg Dex + 0.075mg Pal or saline + 0.075mg Pal. Data was collected postoperatively at 2, 6, 24 and 72 hrs. A Functional Living Index-Emesis (QOL-FLIE) test was administered at 96 hrs. Results:We enrolled 76 ASA 1-2 patients with at least 3 PONV risk factors. Both randomization groups had a low incidence of vomiting in the PACU (Pal, 0.0%; Pal + Dex, 5.4%) as well as at 72 hours (0.0% both groups). Complete response (no vomiting, no rescue medication) was not different between treatment groups at any time intervals. Cumulative success rates over the entire 72 hrs were 60.4% (Pal alone) vs. 60.0% (Pal + Dex). Nausea scores (4 point ordinal scale) were not different between groups for any time intervals. Cumulative success scores for nausea (score = "none"; 0-72 hrs) were 41.9% for the Pal group, and 55.2% for the Pal+ Dex group. The Pal + Dex group showed a trend toward greater satisfaction on the QOL-FLIE scores with the greatest differences in the "nausea domain". Discussion:The combination therapy (Pal + Dex) did not significantly reduce the incidence of PONV or PDNV when compared with Pal alone although a trend was observed indicating the possible increased efficacy of multi-drug therapy. There was no change in comparative efficacy over 72 hrs, possibly due to the low incidence of PDNV in both groups.

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Palonosetron Exhibits Unique Molecular Interactions with the 5-HT3 Receptor

Cited by 214 publications

References 21 publications

Efficacy of palonosetron for preventing postoperative nausea and vomiting: a systematic review and meta-analysis

Efficacy of palonosetron for preventing postoperative nausea and vomiting: a systematic review and meta-analysis

Palonosetron and dexamethasone for prevention of nausea and vomiting in patients receiving high-dose chemotherapy with auto-SCT

A Randomized, Double Blind Study to Evaluate the Efficacy of Palonosetron with Dexamethasone Versus Palonosetron Alone for Prevention of Post-Operative Nausea and Vomiting in Subjects Undergoing Bariatric Surgeries with High Emetogenic Risk

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