Paloron® 0.5 mg Tablet: Each film-coated tablet contains 0.5 mg of Palonosetron as Palonosetron Hydrochloride INN. Paloron® 0.25 mg Injection: Each 5 ml vial contains 0.25 mg of Palonosetron as Palonosetron Hydrochloride INN. Paloron® 0.075 mg Injection: Each 1.5 ml vial contains 0.075 mg of Palonosetron as Palonosetron Hydrochloride INN.

Palonosetron (Paloron®) is a highly potent, selective, second generation Serotonin sub-type 3 (5-HT3) receptor antagonist with a 5-HT3 receptor binding affinity that is _ 100 fold higher than other 5-HT3 recptor antagonists.

Palonosetron is contra-indicated in patients known to have hypersensitivity to the drug or any of its components.

Indications:
Acute and delayed nausea and vomiting; Uncontrolled nausea and vomiting; Chemotherapy-induced nausea and vomiting (CINV): Acute CINV resulting in on the day of treatment with certain types of chemotherapy; Delayed CINV resulting in on days later with certain types of chemotherapy; Radiotherapy-induced nausea and vomiting (RINV); Post-operative & Post-discharge nausea and vomiting (PONV & PDNV).

Usual dosage: Adult tablet dosage: 0.5 mg (01 tablet) daily.
Adult IV dosage: A single IV dose of 0.075 mg should be administered over 10 seconds. Chemotherapy-induced nausea and vomiting: Adult tablet dosage: 0.5 mg (01 tablet) administered approximately 1 hour prior to the start of chemotherapy.
Adult IV dosage: A single IV dose of 0.25 mg should be administered over 30 seconds approximately 30 minutes before the start of chemotherapy.
Radiotherapy-induced nausea and vomiting: A single IV dose of 0.25 mg should be administered over 30 seconds approximately 30 minutes before each week of radiation fraction.
Post-operative nausea and vomiting: A single IV dose of 0.075 mg should be administered over 10 seconds immediately before induction of anesthesia.
Children dosage: (1 month to 17 years): A single IV dose at 20 mcg/kg body weight. Which maximum dose is 1.5 mg

The most common adverse reactions are headache and constipation.
Drug Interactions: In controlled clinical trials, Palonosetron injection has been safely administered with corticosteroids, analgesics, antiemetics/antinauseants, antispasmodics and anticholinergic agents. Palonosetron did not inhibit the antitumor activity of cisplatin, cyclophosphamide, cytarabine, doxorubicin and mitomycin C in murine tumor models. Concomitant administration of Palonosetron and metoclopramide has no significant pharmacokinetic interactions. In vitro studies indicated that palonosetron is not inhibitor of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2D6, CYP2E1 & CYP3A4/5 (CYP2C19 was not investigated) nor does it induce the activity of CYP1A2, CYP2D6 or CYP3A4/5. Therefore, the potential for clinically significant drug interactions with Palonosetron appears to be low.

Pregnancy category 'B'. It is not known whether Palonosetron is excreted in breast milk.
Use in elderly patients: No dosage adjustment is recommended in elderly patients _ 65 years of age.
Use in Children: (1 month to 17 years): A single IV dose at 20 mcg/kg body weight. Which maximum dose is 1.5 mg.
Use in patients with impaired renal and hepatic function: No dosage adjustment is recommended in patients with renal and hepatic dysfunction.

Paloron® 0.5 mg Tablet: Each box contains 2x10's tablets in Alu-Alu blister pack.
Paloron® 0.25 mg Injection: Each box contains 4 vials of 5 ml each in separate inner carton.
Paloron® 0.075 mg Injection: Each box contains 4 vials of 1.5 ml each in separate inner carton.

Palonosetron exhibits linear dose-proportional pharmacokinetics over the dose-range 1-90 µg/kg in healthy subjects and in patients with cancer. In cancer patients receiving single intravenous doses of Palonosetron in this dose range, the mean maximum plasma concentration (Cmax) ranges from 0.89 to 336 ng/ml and the area under the plasma concentration-time curve from zero to infinity (AUC0- ) ranges from 13.8 to 957 ng.h/ml. Palonosetron has a volume of distribution of approximately 6.9-7.9 L/kg, with approximately 62% bound to plasma proteins. Approximately 50% of Palonosetron is metabolized into two inactive metabolites that exhibit <1% of the 5-HT3 receptor antagonist activity. Approximately 40% of the drug is metabolised via kidney, 50% by liver CYP2D6 (mainly), CYP3A4 and CYP1A2 isoenzymes. About 50% of the drug goes under metabolism. After a single intravenous dose, approximately 40% is excreted as unchanged drug in the urine after 144 hours. Total body clearance of Palonosetron is 160±35 ml/h/kg, and renal clearance is 66.5±18.2 ml/h/kg in healthy subjects. Palonosetron exhibits a longer half-life (40 hours) and has a greater 5-HT3 receptor binding affinity.

Storage:
Store in a cool & dry place, protected from light.