The product is indicated for use in adults to: prevent acute nausea and vomiting due to antineoplastic chemotherapy with severe vomiting; prevention of nausea and vomiting associated with moderate-antitumor chemotherapy.
Composition:
1 ml of solution contains 50 μg of palonosetron (as hydrochloride). 5 ml of solution contains 250 μg of palonosetron (as hydrochloride).
Action:
Palonosetron is an antiemetic medicine and against nausea. The drug is a selective, high affinity 5-HT receptor antagonist3. The antiemetic effect was observed between 0-24 h, 24-120 h and 0-120 h. In healthy people and patients with cancer Cmax and AUC vary in a dose-proportional manner for doses in the range 0.3 - 90 μg / kg. Palonosetron used in the recommended dose is subject to wide distribution in the body - the volume of distribution is about 6.9-7.9 l / kg. Approx. 62% of palonosetron is bound to plasma proteins. Elimination of the drug occurs in two ways: about 40% of the drug is excreted through the kidneys, and about 50% is converted to 2 major metabolites, showing less than 1% of 5-HT receptor antagonist activity3. In researchin vitro it was found that palonosetron metabolism is mediated by CYP2D6 and, to a lesser extent, CYP3A4 and CYP1A2 isoenzymes. After a single intravenous injection in adults, the total clearance of palonosetron was 173 ± 73 ml / min and the renal clearance was 53 ± 29 ml / min. Due to low total clearance and high volume of distribution, total plasma T0,5 the elimination phase is approx. 40 h. In 10% of patients the average T0,5 the elimination phase is greater than 100 h.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients.
Precautions:
Palonosetron can prolong the time of intestinal transit; Patients with a history of constipation or signs of subacute intestinal obstruction should be monitored. Caution should be exercised when palonosetron is combined with agents that prolong the QT interval in patients with or with a higher risk of QT prolongation. Due to the lack of sufficient data, it is not recommended for use in children and adolescents under 18 years of age.
Pregnancy and lactation:
Due to the lack of data, the preparation is not recommended in pregnant women and during breast-feeding.
Intravenously. The drug should only be used before administration of chemotherapy. The preparation should be administered by medical personnel under appropriate medical supervision. Adults: palonosetron 250 μg administered as a single intravenous bolus injection 30 min before the start of chemotherapy. The preparation should be injected for 30 seconds. The effectiveness of the preparation in the prevention of nausea and vomiting induced by high-emetic chemotherapy may be increased by adding a corticosteroid before starting chemotherapy.No dose adjustment is necessary in the elderly, in patients with impaired hepatic function, or in patients with impaired renal function. Lack of information on hemodialyzed patients in the final stage of renal failure.
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