Patron 0.5 mg Tablet

Patron 0.5 mg Tablet 

COMPOSITION

Tablet : Each tablet contains 0.5 mg Palonosetron as

Palonosetron Hydrochloride INN.

Injection 1.5 ml : Each 1.5 ml ampoule contains 0.075 mg of

Palonosetron as Palonosetron Hydrochloride INN.

Injection 5 ml : Each 5 ml ampoule contains 0.25 mg of

Palonosetron as Palonosetron Hydrochloride INN.

MECHANISM OF ACTION

Cancer chemotherapy may be associated with a high incidence of nausea and vomiting, 5-HT3 receptors are located

on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone. It is thought that chemotherapeutic agents release serotonin (5-HT3) from the enterochromaffin cells of the small intestine. The released serotonin then activates 5-HT3 receptors located on vagal afferents to initiate the vomiting response.

Postoperative nausea and vomiting is influenced by multiple patient, surgical and anesthesia related factors and is triggered by release of serotonin (5-HT3) in a cascade of neuronal events involving but the central nervous system and the gastrointestinal tract. The 5-HT3 has been demonstrated to selectively participate in the emetic response.

Palonosetron is a 5-HT3 receptor antagonist with a strong binding affinity for this receptor. As a result serotonin can’t activate 5-HT3 receptors and thus fails to initiate vomiting reflux.

INDICATION

 Moderately emetogenic cancer chemotherapyPrevention 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 AND ADMINISTRATION

Chemotherapy-Induced Nausea and Vomiting:

Dosage for adults : One 0.5 mg tablet administered approximately one hour prior to the start of chemotherapy.

Adult 0.25 mg IV dosage : A single 0.25 mg IV dose administered over 30 seconds. Dosing should occur 30 minutes before the start of chemotherapy. Alternatively 0.5 mg approximately tablet 1 hours before the start of chemotherapy. Postoperative Nausea and Vomiting

Dosage for adults: A single 0.075 mg IV dose administered over 10 seconds immediately before the induction of anesthesia.

OR AS DIRECTED BY PHYSICIAN

GENERAL ADVICE

 For IV administration only. Not for intradermal, subcutaneous or IM administration

 Do not administer if particulate matter, cloudiness, or discoloration is noted

 Discard any unused solution. Do not store unused solution for later administration

 Do not mix with other medications

SIDE EFFECTS

The most common adverse reaction 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 & PRECAUTIONS

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. 

USE IN PREGNANCY & LACTATION

Pregnancy category B.

It is not known whether Palonosetron is excreted in human mmilk.

Paediatric Use :

Safety and effectiveness in patients below the age 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 of 65 years of age and younger patients (18 to 64).

USE OF SPECIAL CASES

Renal Impairment :

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

Hepatic 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.

DRUG INTERACTIONS

In vitro studies indicated that Palonosetron is neither an inhibitor of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2D6,

CYP2E1 and CYP3A4/5 (CYP2C19 was not investigated) nor does it induce the activity of CYP1A2, CYP2D6, or CYP3A4/5.

Therefore, drug interactions with Patron appears to be low. In controlled clinical trials, Palonosetron injection has been safely administered with corticosteroids, analgesics, antiemetics/ anti-nauseants, anti-spasmodics and anticholinergic

drugs.

Palonosetron did not inhibit the antitumor activity of the five chemotherapeutic agents tested (cisplatin, cytarabine, doxorubicin and mitomycin C) in murine tumor models.

SUPPLY

Tablet : Each box contains 2 x 10 tablets in blister strips.

Injection 0.075 mg/1.5 ml : Each box contains 1 ampoule of 1.5 ml solution for IV Injection in blister strip.

Injection 0.25 mg/ 5 ml : Each box contains 3 ampoules of 5 ml solution for IV Injection in blister strip.