It has long been recognized that delayed emesis can be difficult to control. As many as 90% of patients receiving high-dose cisplatin regimens ( 120 mg/m2) are reported to experience delayed nausea or vomiting despite antiemetic prophylaxis with high-dose metoclopramide and dexamethasone on the day of cisplatin treatment. The incidence of symptoms is greatest between 48 and 72 hours after cispl...

BACKGROUND Cisplatin (CDDP) is one of the most active chemotherapeutic agents but is among the most emetogenic drugs. The emetic side-effects of CDDP-containing intraarterial chemotherapy have not been evaluated in a prospective randomized trial and the efficacy of serotonin antagonists in preventing the emesis associated with this method of CDDP administration has not been assessed. METHODS ...

PURPOSE Hyperemesis gravidarum is the third leading cause of hospitalization during pregnancy. 5-HT3-receptor antagonists are the most effective against chemotherapy-induced nausea and vomiting and radiation. This randomized study aimed to compare and evaluate the efficacies of granisetron and promethazine for controlling nausea and vomiting of pregnancy. METHODS The included patients were ad...

Crystal structures can identify ligand-receptor interactions and assist the development of novel therapeutics, but experimental challenges sometimes necessitate the use of homologous proteins. Tropisetron is an orthosteric ligand at both 5-HT3 and α7 nACh receptors and its binding orientation has been determined in the structural homologue AChBP (pdbid: 2WNC). Co-crystallisation with a structur...

Background and aim: Uremic pruritus is a relatively common and distressing problem for patients with chronic renal failure. Serotonin and histamine have been reported as possible mediators of uremic pruritus. Granisetron, a potent and selective inhibitor of 5-HT3 receptors was developed for relief of chemotherapy induced nausea. There are some studies about effect of Ondansetron in uremic...

PURPOSE This analysis was undertaken to review published reports of the comparative efficacy and safety of 5-hydroxytryptamine-3 (5-HT3) receptor antagonists in the prophylaxis of acute chemotherapy-induced emesis. METHODS Comparison data used are the preclinical pharmacology as well as the design and results of clinical trials. Seven comparative studies that used granisetron, ondansetron, or...

Palonosetron is the only 5-HT(3) receptor antagonist approved for the treatment of delayed chemotherapy-induced nausea and vomiting (CINV) in moderately emetogenic chemotherapy. Accumulating evidence suggests that substance P (SP), the endogenous ligand acting preferentially on neurokinin-1 (NK-1) receptors, not serotonin (5-HT), is the dominant mediator of delayed emesis. However, palonosetron...

BACKGROUND Regulatory concern about potential QT-interval prolongation by serotonin-receptor antagonist antiemetics prompted product-label changes. The first-generation serotonin-receptor antagonist granisetron is available in oral (PO), intravenous (IV), and transdermal formulations. APF530 is a formulation that provides sustained release of granisetron when administered as a single subcutaneo...

BACKGROUND Pediatric strabismus surgery is commonly associated with higher incidence of postoperative nausea and vomiting (PONV). Mixtures of different classes of antiemetics have been used successfully to decrease the incidence of PONV but there was no agreement on the optimal combination. The aim of this study was to investigate the effect of granisetron, ondansetron, midazolam combination wi...

BACKGROUND AND OBJECTIVES Reducing pain on injection of anesthetic drugs is of importance to every anesthesiologist. In this study we pursued to define if pretreatment by granisetron reduces the pain on injection of etomidate similar to lidocaine. METHODS Thirty patients aged between 18 and 50 years of American Society of Anesthesiologists physical status class I or II, whom were candidates f...