PubMed · 13695290
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A H COONS. 1960. Immunofluorescence.. https://pubmed.ncbi.nlm.nih.gov/13695290/
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BACKGROUND: Palonosetron HCl is a selective 5-HT(3) receptor antagonist used for the prevention of chemotherapy-induced nausea and vomiting. Palonosetron HCl may be diluted in an infusion solution for administraton. Consequently, stability information is needed for palonosetron HCl admixed in common infusion solutions. OBJECTIVE: To evaluate the physical and chemical stability of palonosetron HCl in concentrations of 5 and 30 microg/mL in dextrose 5% injection, NaCl 0.9% injection, dextrose 5% in NaCl 0.45% injection, and dextrose 5% in lactated Ringer's injection. METHODS: Triplicate test samples of palonosetron HCl at each concentration in each diluent were tested. Samples were stored and evaluated at appropriate intervals for up to 48 hours at room temperature ( approximately 23 degrees C) and 14 days under refrigeration (4 degrees C). Physical stability was assessed using turbidimetric and particulate measurement, as well as visual inspection. Chemical stability was assessed by HPLC. RESULTS: All of the admixtures were initially clear and colorless when viewed in normal fluorescent room light and with a Tyndall beam. Measured turbidity and particulate content were low initially and remained low throughout the study. The drug concentration was unchanged in any of the samples at either temperature throughout the study. CONCLUSIONS: Palonosetron HCl is physically and chemically stable in all 4 common infusion solutions for at least 48 hours at room temperature and 14 days under refrigeration.
OBJECTIVE: To review the currently available literature on the efficacy of the 5-HT(3) receptor antagonists in the prevention of late acute-onset chemotherapy-induced nausea and vomiting (12-24 h after cytotoxic treatment). DATA SOURCES: Primary articles were identified by PubMed search (performed in March 2004) and through secondary sources. Search terms included granisetron, ondansetron, tropisetron, dolasetron, acute, chemotherapy, nausea, and vomiting (a further search was performed for palonosetron in March 2004). STUDY SELECTION AND DATA EXTRACTION: All studies that performed regular assessments (every 2-6 h) of antiemetic control over the first 24 hours with 5-HT(3) receptor antagonists were evaluated. DATA SYNTHESIS: Current guidelines recommend the use of 5-HT(3) receptor antagonists for the control of chemotherapy-induced nausea and vomiting but do not differentiate between the available agents. However, there is variability in the pharmacokinetic and pharmacodynamic profiles of these agents, and this has implications for dosing regimen, safety, efficacy, and potential drug-drug interactions. Cytotoxic agents vary in the time profile of their emetic effect; this must be considered when choosing an appropriate 5-HT(3) receptor antagonist. The optimal agent should be simple to administer and provide safe and effective antiemetic protection over the whole 24-hour period. CONCLUSIONS: The differences between the 5-HT(3) receptor antagonists have important consequences for their dosing and efficacy in the control of late acute-onset chemotherapy-induced nausea and vomiting.
Significant progress has been made in the development of effective, convenient, and well-tolerated means to prevent nausea and vomiting associated with cancer chemotherapy (CINV). Nevertheless, a substantial minority of patients continues to have suboptimal antiemetic control, and additional treatment approaches are needed. One avenue of investigation being pursued involves the evaluation of a new 5-HT(3) receptor antagonist (palonosetron) that differs from available serotonin antagonists in its markedly longer half-life (40 h) and greater binding affinity for the type-three serotonin receptor. Analysis of available clinical data demonstrates that palonosetron is an active and well tolerated new 5-HT(3) antagonist. Additional studies incorporating dexamethasone and repetitive-day conventional 5-HT(3) antagonist dosing will be necessary to definitively determine the relative efficacy of palonosetron compared to available agents. Another very promising area that moves beyond serotonin focuses on Substance P as a therapeutic target. Substance P is a tachykinin found in neurons in the brainstem. It is the preferred ligand for the neurokinin-1 (NK-1) receptor. Preclinical studies with selective NK-1 antagonists have demonstrated promising antiemetic activity. Subsequent clinical trials with selective NK-1 antagonists for the prevention of CINV have validated the preclinical promise demonstrated with these agents. One agent in this new therapeutic class (aprepitant) recently received regulatory approval in the United States for use in combination with a 5-HT(3) antagonist and dexamethasone, defining a new standard of care for highly-emetogenic chemotherapy.