奈妥吡坦/帕洛诺司琼的作用与效果？

It is a new type of long-acting antiemetic drug. Clinical studies have shown that the antiemetic effect of palonosetron can last for about 10 hours. The blood concentration will gradually increase from 15 minutes to 30 minutes after taking the drug, usually reaching the highest concentration within 5 hours, and then gradually decrease.

Netupitant/palonosetron mechanism of action

Palonosetron (Akynzeo) is a 5-HT3 receptor antagonist with strong binding affinity for this receptor and almost no affinity for other receptors. Cancer chemotherapy may be associated with a high incidence of nausea and vomiting, especially when certain drugs such as cisplatin are used. 5-HT3 receptors are located peripherally and centrally in the vagus nerve terminals, in the chemoreceptor triggering zone of the area postrema.

Chemotherapy drugs produce nausea and vomiting by stimulating the release of 5-hydroxytryptamine from enterochromaffin cells in the small intestine. Serotonin activates 5-HT3 receptors on vagus nerve afferents to initiate the vomiting reflex. It is known that the occurrence of acute vomiting depends on 5-hydroxytryptamine, and 5-HT3 receptors can selectively stimulate the vomiting response.

Netupitant/palonosetron effects and indications

In 2003, the FDA approved the second-generation 5-HT(3) receptor antagonist (5-HT(3)RA) palonosetron for the prevention of acute and delayed nausea and vomiting associated with initial and repeated courses of chemotherapy for highly emetogenic cancers in adults. Palonosetron for injection is a compound preparation of palonosetron and fosnetupitant, the prodrug of netupitant. Palonosetron can prevent nausea and vomiting in the acute phase after cancer chemotherapy, and fosnetupitant can prevent nausea and vomiting in the acute phase and delayed phase after cancer chemotherapy.

Netupitant/palonosetron

In a multicenter, multinational, randomized, active-controlled, double-blind, double-dummy, parallel-group, clinical noninferiority study, the efficacy and safety of single-dose oral palonosetron was compared with intravenous palonosetron in cancer patients scheduled to receive highly emetogenic cisplatin (>70 mg/m 2 )-based chemotherapy. A total of 739 patients were included in the study, 370 in the oral palonosetron group and 369 in the intravenous palonosetron group.

In the oral palonosetron group, 89.4% of patients achieved CR in the acute phase compared with 86.2% in the intravenous palonosetron group, a difference of 3.2%. Noninferiority of oral palonosetron compared with intravenous palonosetron was confirmed because the lower limit of the two-sided 99% CI for the difference in the proportion of patients with CR was greater than (i.e., close to zero) the predefined noninferiority margin (set at -15%).

Palonosetron side effects

The most common adverse reactions (≥3%) of palonosetron are headache, fatigue, indigestion, fatigue, constipation and erythema. The more serious adverse reactions are hypersensitivity reactions and serotonin syndrome. The occurrence of serious adverse reactions requires timely and corresponding treatment. If symptoms of serotonin syndrome occur, discontinue palonosetron and initiate supportive treatment.

Palonosetron dosage forms and specifications

1. Palonosetron capsule: 300 mg Netupitant/0.5 mg Palonosetron, a hard gelatin capsule with a white capsule body and a caramel-colored capsule cap, with “HE1” printed on the capsule body.

2. Palonosetron injection: 235 mg fosnetupitant/0.25 mg palonosetron, white to off-white freeze-dried powder, single-dose vial, reconstitute.

3. Palonosetron injection: 235 mg fosnetupitant/0.25 mg palonosetron/20 mL (11.75 mg/0.0125 mg/mL), a clear solution, single-dose vial.

People who need medication need to use the drug under the guidance of a doctor, and pay attention to the occurrence of adverse reactions. If any discomfort occurs during the medication, they should seek medical advice in time.

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