Palonosetron

Palonosetron (INN) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is used for the control of delayed CINV—nausea and vomiting and there are tentative data to suggest that it may be better than granisetron.

Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy, or as a single oral capsule one hour before chemotherapy. The oral formulation was approved on August 22, 2008 for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV.

Indication:

• Moderately emetogenic cancer chemotherapy – prevention of acute and delayed nausea and vomiting associated with initial and repeat courses

• Highly emetogenic cancer chemotherapy – prevention of acute nausea and vomiting associated with initial and repeat courses

• Prevention of postoperative nausea and vomiting (PONV) for up to 24 hours following surgery. Efficacy beyond 24 hours has not been demonstrated.

Dosage & Administration:
Chemotherapy-Induced Nausea and Vomiting
Dosage for Adults – a single 0.25 mg I.V. dose administered over 30 seconds. Dosing should occur 30 minutes before the start of chemotherapy. Alternatively 0.5 mg tablet approximately 1 hour before the start of chemotherapy. Postoperative Nausea and Vomiting
Dosage for Adults – a single 0.075 mg I.V. dose administered over 10 seconds immediately before the induction of anesthesia. In case of 0.5 mg tablet, dose should be determined by the physician.

Pediatric Use
Safety and effectiveness in patients below the age of 18 years have not been established. However different clinical trial shows Palonosetron is well tolerated and effective from one month of age.

Geriatric Use
Pharmacokinetics analysis did not reveal any differences in Palonosetron pharmacokinetics between patients ≥ 65 years of age and younger patients (18 to 64 years)

Renal Function Impairment
No dosage adjustments are needed with any degree of renal function impairment.

Hepatic Function Impairment
No dosage adjustments are needed with any degree of hepatic function impairment.

Elderly
No dosage adjustments or special monitoring are needed in elderly patients.

Side Effects:
The most common adverse reactions in chemotherapy-induced nausea and vomiting (incidence ≥ 5%) are headache and constipation.
The most common adverse reactions in postoperative nausea and vomiting (incidence ≥ 2%) are QT prolongation, bradycardia, headache, and constipation.
Contraindication:

Palonosetron is contraindicated in patients known to have hypersensitivity to the drug or any of its components

Hypersensitivity reactions may occur in patients who have exhibited hypersensitivity to other selective 5-HT3 receptor antagonists.