Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0042963 (vomiting)
 31,883 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Palonosetron (Aloxi) is a 5-HT(3)-receptor antagonist antiemetic indicated for the prevention of acute and delayed nausea and vomiting following moderately emetogenic chemotherapy and for acute nausea and vomiting following highly emetogenic chemotherapy. Although it is the fourth member of this class to enter the US market, palonosetron is distinguished by distinct pharmacological characteristics. It has a higher binding affinity for the 5-HT(3 )receptor and a terminal serum half-life at least four times greater than any other available agent of this class (approximately 40 h). The high affinity and long half-life may explain the persistence of antiemetic effect throughout the delayed emesis risk period. The indications for palonosetron are supported by one dose-ranging study and three large, randomised, Phase III studies that all demonstrated at least equivalent activity (and in some cases, superior activity) compared to other 5-HT(3)-receptor antagonists. In spite of the pharmacological differences, the side effect profile of palonosetron is comparable to that of other 5-HT(3)-receptor antagonists. Palonosetron may prove valuable in combination therapy for delayed emesis and may be an appropriate agent for clinical settings, such as multiple-day chemotherapy, where acute emesis is repeatedly induced. Palonosetron provides a convenience advantage if multiple-day 5-HT(3)-receptor antagonist therapy is anticipated and is a unique addition to the antiemetic armamentarium.
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PMID:Palonosetron: a unique 5-HT3-receptor antagonist for the prevention of chemotherapy-induced emesis. 1464 Sep 28

Nausea and vomiting are considered to be among the most distressing consequences of cytotoxic chemotherapies. Currently, there are several novel 5-HT(3) receptor antagonists for the treatment of chemotherapy-induced nausea and vomiting (CINV), including ondansetron, granisetron, and dolasetron. These agents provide significant improvement in the management of acute emesis but are ineffective at preventing delayed emesis. In 2003, a new 5-HT(3) receptor antagonist, palonosetron HCL (Aloxi), was introduced to the U.S. market. Palonosetron was found to be effective in preventing delayed CINV. Indeed, palonosetron was the first and only 5-HT(3) receptor antagonist approved by the FDA for the prevention of both acute and delayed CINV. More recently, studies on the role of substance P in the emetic process led to the development of aprepitant (Emend) for the prevention of delayed emesis in combination with 5-HT(3) receptor antagonists. Despite these major advances, CINV remains uncontrolled in some patients. Current efforts are focused on treating refractory emesis and include both the clinical evaluation of compounds marketed for other indications and the preclinical evaluation of novel molecules targeting other transmitters in the emetic pathway. Ongoing work in pharmacogenomics has postulated several candidate genes that could be involved in emetic sensitivity and responsiveness to antiemetic therapy. Investigations into the pharmacogenomics of CINV may someday be able to aid in the identification of high risk patients and patients unlikely to respond to conventional therapies.
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PMID:New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations. 1703 70

Chemotherapy-induced nausea and vomiting (CINV) remains an important and common toxicity of cancer treatment. Recent guideline revisions have classified chemotherapeutic agents into four categories of emesis risk without the use of preventive agents: high (> 90%), moderate (30%--90%), low (10%-30%), and minimal (< 10%). Currently available antiemetic agents, including corticosteroids, 5-hydroxytryptamine (HT)3 receptor antagonists, and neurokinin (NK)-1 antagonists are used alone or in combination depending on the level of emetogenic potential as prophylaxis against the development of CINVduring the acute period (up to 24 hours after chemotherapy) and the delayed period (up to 5 days after treatment). Newer agents, including the second-generation 5-HT3 receptor antagonist palonosetron (Aloxi) and the NK-1 antagonist aprepitant (Emend), offer additional clinical benefit in highly and moderately emetogenic therapy. However, delayed nausea and vomiting continue to occur frequently in many patients and have an impact on quality of life. Other classes of agents including the benzodiazepines and cannabinoids offer the potential for additional protective benefit. Continued research with new drugs and combinations is necessary to meet this significant unmet need of cancer patients.
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PMID:Chemotherapy-induced nausea and vomiting: which antiemetic for which therapy? 1771 96

The current study aimed to evaluate the efficacy and safety of palonosetron hydrochloride injection for preventing chemotherapy-induced moderate and severe nausea and vomiting. A multi-centered, randomly stratified, double-blind, double-dummy, parallel-group and positive-controlled trial was performed. A total of 240 patients who underwent chemotherapy treatment which induced moderate or severe vomiting were divided into the experimental and control groups. Half an hour before chemotherapy, the experimental group received a 0.25-mg palonosetron hydrochloride injection, whereas the control group received a 3-mg granisetron injection. The acute vomiting complete remission rate (CRR) of the experimental group was not significantly different compared with that of the control group (P=0.35). The delayed vomiting CRR of the experimental group was significantly higher compared with that of the control group (P=0.002). No difference in full course vomiting CRR, vomiting control time, treatment failure time or acute nausea CRR was identified between the two groups. No significant differences in adverse events were observed between the experimental group and the control group. No significant differences in adverse reactions occurred between the experimental group and the control group (12.50%). Palonosetron hydrochloride injection had a better effect on delayed vomiting CRR than granisetron hydrochloride injection. The two injections exhibited similar effects on acute vomiting CRR, full course vomiting CRR, vomiting control time, treatment failure time (days), acute nausea CRR and adverse events.
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PMID:The effect of palonosetron hydrochloride in the prevention of chemotherapy-induced moderate and severe nausea and vomiting. 2373 92

Palonosetron hydrochloride is a longer-acting, selective 5-HT3 receptor antagonist that has been approved for prevention of chemotherapy-induced nausea and vomiting and is being evaluated for prevention of postoperative nause and vomiting. The objective of this study was to evaluate the physical and chemical stablity of palonosetron hydrochloride 50 mcg/mL when mixed with undiluted propofol 1% during simulated Y-site administation. Duplicate samples of this mixture were tested. Samples were stored and evaluated for up to 4 hours at room temperature. Physical stability was assessed by visual inspection. Chemical stability was assessed by high-performance liquid chromatographic analysis. All of the admixtures were opaque white when viewed in normal fluorescent room light and when viewed with a Tyndall beam. After centrifugation, no evidence of precipitation was found. The drug concentrations were essentially unchanged in all of the samples throughout the study. Palonosetron hydrochloride is physically and chemically stable when mixed with propofol as undiluted injections during simulated Y-site administration over 4 hours at ambient room temperature.
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PMID:Compatibility and stability of palonosetron hydrochloride and propofol during simulated y-site administration. 2396 67