奈妥吡坦的注意事项是什么？

It is a second-generation 5-hydroxytryptamine 3 (5-HT;) receptor antagonist. Compared with the first-generation drugs, it has a higher receptor affinity for 5-HT and a longer plasma clearance half-life. After administration, it can selectively inhibit 5-HT and receptor excitability, block the vagus nerve endings in the intestine, making it difficult for signals to be transmitted to the 5-HT and receptor trigger areas, thereby preventing the occurrence of nausea and vomiting and reducing its occurrence. Due to its long half-life, Netupitant is not only effective against acute vomiting caused by chemotherapy, but also has a good effect on delayed vomiting, which is helpful in reducing the occurrence of nausea and vomiting. However, the following matters need to be paid attention to when using Netupitant:

1. Hypersensitivity reaction

Hypersensitivity reactions, including anaphylaxis, have been reported in patients treated with palonosetron (an ingredient of AKYNZEO), with or without known hypersensitivity to other 5-HT3 receptor antagonists.

2. Serotonin syndrome

5-HT3 receptor antagonists have been reported to cause serotonin syndrome. Most reports have been related to the concomitant use of serotonergic drugs (e.g., selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors, mirtazapine, fentanyl, lithium, tramadol, and intravenous methylene blue). Some reported cases have been fatal. Serotonin syndrome has also been reported with overdose of another 5-HT3 receptor antagonist alone. Most reports of serotonin syndrome associated with the use of 5-HT3 receptor antagonists have occurred in postanesthesia care units or infusion centers.

3. Others

Symptoms associated with serotonin syndrome may include a combination of the following signs and symptoms: mental status changes (e.g., agitation, hallucinations, delirium, and coma), autonomic instability (e.g., tachycardia, unstable blood pressure, dizziness, diaphoresis, flushing, and hyperthermia), neuromuscular symptoms (e.g., tremor, rigidity, myoclonus, hyperreflexia, and incoordination), seizures, with or without gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea). Patients should be monitored for the emergence of serotonin syndrome, particularly when AKYNZEO is used concomitantly with other serotonergic drugs. If symptoms of serotonin syndrome occur, discontinue AKYNZEO and initiate supportive treatment. Patients should be informed of the increased risk of serotonin syndrome, particularly when AKYNZEO is used concomitantly with other serotonergic drugs.

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