Palonosetron Hydrochloride Injection
Function and Efficacy
Palonosetron is a selective antagonist of the 5-HT3 receptor with strong affinity, and has no affinity or low affinity for other receptors. The 5-HT3 receptor is located in the vagus nerve endings in the central and peripheral emetic chemotherapy receptor area of the medulla oblongata. Chemotherapy drugs stimulate the release of 5-HT by chromaffin cells in the small intestine, and 5-HT then activates the 5-HT3 receptors of the vagal afferent nerves, producing a vomiting reflex.
Ingredients
The main ingredient of this product is palonosetron hydrochloride, and its chemical name is: 2-[1-azabicyclo(2.2.2)oct-3S-yl]-2,3,3aS,4,5,6-hexahydro-1H-benzo[de]isoquinolin-1-one hydrochloride.
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Palonosetron HydrochlorideIngredients |
Palonosetron is a selective antagonist of the 5-HT3 receptor with strong affinity, and has no affinity or low affinity for other receptors. The 5-HT3 receptor is located in the vagus nerve endings in the central and peripheral emetic chemotherapy receptor area of the medulla oblongata. Chemotherapy drugs stimulate the release of 5-HT by chromaffin cells in the small intestine, and 5-HT then activates the 5-HT3 receptors of the vagal afferent nerves, producing a vomiting reflex. More |
135729-62-3 | 34 |
Appearance
This product is a colorless clear liquid.
Indication
1. Prevent acute nausea and vomiting caused by severe emetogenic chemotherapy; 2. Prevent nausea and vomiting caused by moderate emetogenic chemotherapy.
Usage and Dosage
The recommended dose is a single intravenous injection of 0.25 mg of palonosetron about 30 minutes before chemotherapy, with an injection time of more than 30 seconds. Since the safety and effectiveness of frequent (daily continuous or alternate day) dosing have not been evaluated, repeated use within 7 days is not recommended.
Adverse Reactions
According to foreign clinical research reports: 1,374 adult patients participated in a clinical study of palonosetron to prevent nausea and vomiting caused by moderate or severe emetogenic chemotherapy. The results showed that the incidence and severity of adverse reactions caused by palonosetron were similar to those of ondansetron or dolasetron.
Precautions
Contraindicated in patients with known hypersensitivity to the drug or any of its components.
Drug Interactions
Palonosetron's elimination pathways in vivo include renal secretion and the participation of multiple CYP enzymes. Further in vitro studies have shown that palonosetron is neither an inhibitor of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2D6, CYP2E1, and CYP3A4/5 (CYP2C19 has not been studied), nor does it induce the activity of CYP1A2, CYP2D6, or CYP3A4/5. Therefore, the possibility of significant clinical drug interactions with palonosetron is very low. In a study in which healthy volunteers were given a single intravenous dose of 0.75 mg of palonosetron and oral metoclopramide (10 mg four times a day) during the stable period, no significant pharmacokinetic effects were found. Clinical studies have shown that palonosetron can be safely used with corticosteroids, analgesics, antiemetics, antispasmodics, and anticholinergics. Studies in mouse tumor models showed that palonosetron did not inhibit the anticancer activity of the five chemotherapy drugs studied (cisplatin, cyclophosphamide, cytarabine, doxorubicin, and mitomycin C).
Storage
Keep away from light and store in a sealed container.
Packaging Specification
5ml:0.25mg (based on C19H24N2O)
Manufacturer
Qilu Pharmaceutical (Hainan) Co., Ltd.
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Founded in:
2005-10-18 -
Address:
No. 273-A, Nanhai Avenue, National High-tech Zone, Haikou City -
Tax NO.:
91460000780701210W -
Registered Funds:
40 million yuan -
Website:
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Email: