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化疗止吐药帕洛诺司琼与昂丹司琼哪个好?

Author: Medicalhalo
Release time: 2025-10-19 11:44:20

Chemotherapy antiemetics palonosetron and ondansetron both have good efficacy. There is no clinical opinion about which drug is better. If necessary, patients can choose the medication under the guidance of a doctor.

Palonosetron, available in oral and intravenous (IV) formulations, is a fixed-dose combination of the neurokinin 1 (NK1) receptor antagonist nepitant (or the prodrug fosnetupitant in IV formulations) and the second-generation serotonin 3 (5-HT3) receptor antagonist palonostrone. Nepitant/palonosetron single dose (in combination with dexamethasone) is indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) in adults.

In clinical trials, (fos)nepitant/palonosetron plus dexamethasone was associated with high complete response rates (no emesis and no rescue medication) in the acute, delayed and overall phases in patients receiving highly or moderately emetogenic chemotherapy, and efficacy was maintained across multiple cycles. In addition, oral nepitant/palonosetron was found to be superior to palonosetron and not inferior to aprepitant plus granisetron in preventing CINV in individual trials. Both oral and intravenous formulations of this drug combination were well tolerated. The fixed-dose combination is consistent with guideline recommendations and provides a simple and convenient option for the prevention of acute and delayed CINV in patients receiving highly or moderately emetogenic chemotherapy.

Chemotherapy-induced nausea and vomiting (CINV) is a common problem during cancer treatment. Palonosetron (NEPA); Akynzeo® is a fixed-dose combination of two drugs that target two different signaling pathways that induce vomiting.

In clinical trials, a high proportion of patients who received nepitant/palonosetron (in combination with the corticosteroid dexamethasone) before chemotherapy experienced no vomiting, no need for rescue medications, and no significant nausea within 5 days of chemotherapy. Both oral and intravenous formulations of this drug combination were well tolerated.

In summary, nepitant/palonosetron is a simple, convenient and effective drug combination.

Ondansetron is a potent and highly selective serotonin 5-HT3 receptor antagonist with important antiemetic activity and good tolerability in the prevention of chemotherapy-induced nausea and vomiting. Ondansetron is completely and rapidly absorbed from the gastrointestinal tract after oral administration and does not accumulate due to repeated oral administration.

Due to hepatic first-pass metabolism, ondansetron's bioavailability is only approximately 60% when infused over 15 minutes. Bioavailability is slightly increased when administered after a standard meal and is not affected by coadministration of antacids. Slightly enhanced bioavailability was observed in cancer patients. Since the drug reaches peak concentration 0.5-2 hours after oral administration, it should be administered at least 30 minutes before chemotherapy.

Possible other modes of administration of ondansetron include intramuscular, subcutaneous, and rectal administration and oral controlled-release formulations. Ondansetron is widely distributed (distribution volume approximately 160L), has moderate binding to plasma proteins (70 - 76%), and has an average elimination half-life of approximately 3.8±1 hours. Clearance occurs by hepatic metabolism (95%) rather than renal excretion. Metabolites do not play a role in drug activity, and there is no evidence of genetically polymorphic metabolism.

Although aging is associated with decreased clearance and increased bioavailability, dose adjustments are not required in the elderly and may only be required in patients with severe hepatic impairment.

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