Palonosetron Hydrochloride
Generic Name: palonosetron hydrochloride
Brand Names:
Palonosetron Hydrochloride
11 DESCRIPTION Palonosetron hydrochloride injection contains palonosetron as palonosetron HCl, an antiemetic and antinauseant agent. It is a serotonin-3 (5-HT 3 ) receptor antagonist with a strong binding affinity for this receptor. Chemically, palonosetron hydrochloride is: (3a S )-2-[( S )-1-Azabicyclo [2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1-oxo-1 H benz[ de ]isoquinoline hydrochloride. The molecular formula is C 19 H 24 N 2 O•HCl, with a molecular weight of 332.87.
Overview
11 DESCRIPTION Palonosetron hydrochloride injection contains palonosetron as palonosetron HCl, an antiemetic and antinauseant agent. It is a serotonin-3 (5-HT 3 ) receptor antagonist with a strong binding affinity for this receptor. Chemically, palonosetron hydrochloride is: (3a S )-2-[( S )-1-Azabicyclo [2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1-oxo-1 H benz[ de ]isoquinoline hydrochloride. The molecular formula is C 19 H 24 N 2 O•HCl, with a molecular weight of 332.87.
Uses
1 INDICATIONS AND USAGE Palonosetron hydrochloride injection is indicated in adults for prevention of: acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC). acute nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC). postoperative nausea and vomiting (PONV) for up to 24 hours following surgery. Efficacy beyond 24 hours has not been demonstrated. As with other antiemetics, routine prophylaxis is not recommended in patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively.
Dosage
2 DOSAGE AND ADMINISTRATION Chemotherapy-Induced Nausea and Vomiting ( 2.1 ) Age Dose * Infusion Time Adults 0.25 mg as a single-dose Infuse over 30 seconds beginning approximately 30 minutes before the start of chemotherapy Pediatrics (1 month to less than 17 years) 20 micrograms per kilogram (maximum 1.5 mg) as a single-dose Infuse over 15 minutes beginning approximately 30 minutes before the start of chemotherapy *Note different dosing units in pediatrics Postoperative Nausea and Vomiting ( 2.1 ) The recommended adult dosage is 0.075 mg as a single intravenous dose administered over 10 seconds immediately before the induction of anesthesia.
Side Effects
6 ADVERSE REACTIONS Serious or otherwise clinically significant adverse reactions reported in other sections of labeling: Hypersensitivity Reactions [see Warnings and Precautions (5.1) ] Serotonin Syndrome [see Warnings and Precautions (5.2) ] Most common adverse reactions in chemotherapy-induced nausea and vomiting in adults (≥5%) are: headache and constipation ( 6.1 ) postoperative nausea and vomiting (≥ 2%) are: QT prolongation, bradycardia, headache, and constipation ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Eugia US LLC at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
Interactions
7 DRUG INTERACTIONS Serotonergic Drugs: Monitor for serotonin syndrome; if symptoms occur, discontinue palonosetron and initiate supportive treatment. ( 7.1 ) 7.1 Serotonergic Drugs Serotonin syndrome (including altered mental status, autonomic instability, and neuromuscular symptoms) has been described following the concomitant use of 5-HT 3 receptor antagonists and other serotonergic drugs, including selective serotonin reuptake inhibitors (SSRIs) and serotonin and noradrenaline reuptake inhibitors (SNRIs). Monitor for the emergence of serotonin syndrome. If symptoms occur, discontinue palonosetron and initiate supportive treatment [see Warnings and Precautions (5.2) ].
Warnings
5 WARNINGS AND PRECAUTIONS Hypersensitivity reactions, including anaphylaxis, and anaphylactic shock : reported in patients with or without known hypersensitivity to other selective 5-HT 3 receptor antagonists. If symptoms occur, discontinue palonosetron and initiate appropriate medical treatment. (5.1) Serotonin syndrome : reported with 5-HT 3 receptor antagonists alone, but particularly with concomitant use of serotonergic drugs. ( 5.2 , 7.1 ) 5.1 Hypersensitivity Reactions Hypersensitivity reactions, including anaphylaxis and anaphylactic shock, have been reported with administration of palonosetron [see Adverse Reactions (6.2) ]. These reactions occurred in patients with or without known hypersensitivity to other 5-HT 3 receptor antagonists. 4 CONTRAINDICATIONS Palonosetron hydrochloride injection is contraindicated in patients known to have hypersensitivity to palonosetron [see Warnings and Precautions (5.1) ]. Hypersensitivity to palonosetron or any of its components ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary There are no available data on palonosetron HCl use in pregnant women to inform a drug-associated risk. In animal reproduction studies, no effects on embryo-fetal development were observed with the administration of oral palonosetron HCl during the period of organogenesis at doses up to 1,894 and 3,789 times the recommended human intravenous dose in rats and rabbits, respectively (see Data). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING Palonosetron hydrochloride injection is a sterile, clear, colorless, non pyrogenic, isotonic, buffered solution free from visible particles for intravenous administration available in glass vials packaged as follows.
Frequently Asked Questions
What is Palonosetron Hydrochloride used for?▼
1 INDICATIONS AND USAGE Palonosetron hydrochloride injection is indicated in adults for prevention of: acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC). acute nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC). postoperative nausea and vomiting (PONV) for up to 24 hours following surgery. Efficacy beyond 24 hours has not been demonstrated. As with other antiemetics, routine prophylaxis is not recommended in patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively.
What are the side effects of Palonosetron Hydrochloride?▼
6 ADVERSE REACTIONS Serious or otherwise clinically significant adverse reactions reported in other sections of labeling: Hypersensitivity Reactions [see Warnings and Precautions (5.1) ] Serotonin Syndrome [see Warnings and Precautions (5.2) ] Most common adverse reactions in chemotherapy-induced nausea and vomiting in adults (≥5%) are: headache and constipation ( 6.1 ) postoperative nausea and vomiting (≥ 2%) are: QT prolongation, bradycardia, headache, and constipation ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Eugia US LLC at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
Can I take Palonosetron Hydrochloride during pregnancy?▼
8.1 Pregnancy Risk Summary There are no available data on palonosetron HCl use in pregnant women to inform a drug-associated risk. In animal reproduction studies, no effects on embryo-fetal development were observed with the administration of oral palonosetron HCl during the period of organogenesis at doses up to 1,894 and 3,789 times the recommended human intravenous dose in rats and rabbits, respectively (see Data). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown.
What are the important warnings for Palonosetron Hydrochloride?▼
5 WARNINGS AND PRECAUTIONS Hypersensitivity reactions, including anaphylaxis, and anaphylactic shock : reported in patients with or without known hypersensitivity to other selective 5-HT 3 receptor antagonists. If symptoms occur, discontinue palonosetron and initiate appropriate medical treatment. (5.1) Serotonin syndrome : reported with 5-HT 3 receptor antagonists alone, but particularly with concomitant use of serotonergic drugs. ( 5.2 , 7.1 ) 5.1 Hypersensitivity Reactions Hypersensitivity reactions, including anaphylaxis and anaphylactic shock, have been reported with administration of palonosetron [see Adverse Reactions (6.2) ]. These reactions occurred in patients with or without known hypersensitivity to other 5-HT 3 receptor antagonists. 4 CONTRAINDICATIONS Palonosetron hydrochloride injection is contraindicated in patients known to have hypersensitivity to palonosetron [see Warnings and Precautions (5.1) ]. Hypersensitivity to palonosetron or any of its components ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.