(US Adopted Name, rINNM)
INNs in main languages (French, Latin, Spanish):
Stability. The stability of palonosetron hydrochloride at concentrations of 5 and 30 micrograms/mL was assessed in polyvinyl chloride bags of the following 4 infusion solutions: glucose 5%, sodium chloride 0.9%, glucose 5% in sodium chloride 0.45%, and glucose 5% in lactated Ringer’s solution. All solutions were considered to be physically and chemically stable for at least 48 hours at room temperature exposed to light, and for 14 days under refrigeration.
Palonosetron 50 micrograms/mL was found to be physically and chemically stable during simulated Y-site administration with the following drugs: fentanyl citrate 50 micrograms/mL, hydromor-phone hydrochloride 500 micrograms/mL, morphine sulfate 15 mg/mL, pethidine hydrochloride 10 mg/mL, and sufentanil citrate (12.5 micrograms/mL of sufentanil).
Adverse Effects and Precautions
As for Ondansetron, although no dosage reduction is considered necessary in hepatic impairment. Diarrhoea, fatigue, and abdominal pain may also occur. Patients with a history of constipation or signs of suba-cute intestinal obstruction should be monitored if given palonosetron.
Effects on the cardiovascular system. For a discussion of the effects of 5-HT3 antagonists on the cardiovascular system, see under Ondansetron.
As for Ondansetron.
Palonosetron has a volume of distribution of around 7 to 8 litres/kg plasma protein binding is about 62%. About 50% of a dose is metabolised in the liver by cy-tochrome P450 isoenzymes (notably CYP2D6, but also CYP3A4 and CYP1A2). About 80% of a dose is recovered in the urine within 144 hours, as palonosetron and its metabolites. The mean elimination half-life is reported to be about 40 hours.
Uses and Administration
Palonosetron is a 5-HT3 antagonist used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy and for the prevention of postoperative nausea and vomiting. Palonosetron is given as the hy-drochloride but doses are expressed in terms of the base 280.8 micrograms of palonosetron hydrochloride is equivalent to about 250 micrograms of palonosetron.
For the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately or highly emetogenic cancer chemotherapy, a dose of 250 micrograms is given intravenously over 30 seconds about 30 minutes before chemotherapy. Repeated dosing within 7 days is not recommended.
For the prevention of postoperative nausea and vomiting, for up to 24 hours after surgery a single dose of 75 micrograms is given intravenously over 10 seconds immediately before the induction of anaesthesia. Efficacy beyond 24 hours has not been demonstrated.
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