Palonosetron, Indications, Dosage, Side Effect, Interactions, Pregnancy

Palonosetron
If this article seems to be helpful ,please rate us & share to others









User Review


5
(2 votes)


Palonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is the most effective of the 5-HT3 antagonists in controlling delayed CINV nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy and is the only drug of its class approved for this use by the U.S. Food and Drug Administration. As of 2008, it is the most recent 5-HT3 antagonist to enter clinical uses

Mechanism of Action of Palonosetron

Palonosetron is a selective serotonin 5-HT3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors, in turn, inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. Alternative mechanisms appear to be primarily responsible for delayed nausea and vomiting induced by emetogenic chemotherapy, since similar temporal relationships between serotonin and emesis beyond the first day after a dose have not been established, and 5-HT3 receptor antagonists generally have not appeared to be effective alone in preventing or ameliorating delayed effects. It has been hypothesized that palonosetron’s potency and long plasma half-life may contribute to its observed efficacy in preventing delayed nausea and vomiting caused by moderately emetogenic cancer chemotherapy.

Indications of Palonosetron

  • Prophylaxis against postoperative nausea and vomiting
  • Delayed chemotherapy-induced nausea and vomiting
  • Prophylaxis of acute chemotherapy-induced nausea and vomiting
  • Highly emetogenic cancer chemotherapy
  • Palonosetron Hospira is indicated in adults for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy, the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron Hospira is indicated in pediatric patients 1 month of age and older for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy and prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron Accord is indicated in adults for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy, the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron Accord is indicated in pediatric patients 1 month of age and older for.
  • The prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy and prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron is indicated in adults for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy, the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron is indicated in pediatric patients 1 month of age and older for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy and prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.

Contra Indications of Palonosetron

Dosage of Palonosetron

Strengths: 0.25 mg/5 mL; 0.075 mg/1.5 mL

Chemotherapy Induce Nausea/Vomiting 

  • Oral: 0.5 mg orally administered approximately 1 hour prior to the start of chemotherapy
  • Parenteral: 0.25 mg IV as a single dose 30 minutes before the start of chemotherapy

 Postoperative Nausea/Vomiting 

  • Parenteral: 0.075 mg IV as a single dose immediately before induction of anesthesia

 Chemotherapy Induce Nausea/Vomiting – Pediatric

  • Parenteral: 20 mcg/kg IV (maximum 1.5 mg x 1) infused over 15 minutes beginning 30 minutes before the start of chemotherapy

Side Effects of Palonosetron

The most common

Common

Rare

Drug Interactions of Palonosetron

Palonosetron may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Palonosetron

 FDA pregnancy risk category B

Pregnancy

Palonosetron is listed in FDA pregnancy risk category B. Animal-based teratology studies have not revealed evidence of impaired fertility or harm to the fetus due to palonosetron. There are, however, no adequate and well-controlled studies in pregnant women. Animal reproduction studies are not always predictive of human response. The effects of palonosetron on labor and delivery are not known.

Lactation

It is not known if palonosetron is excreted in human milk. Many drugs are excreted in human milk and may increase the potential for serious adverse reactions in the breastfeeding infant. The manufacturer warns against the use of palonosetron in breast-feeding women due to the possible risks to the infant.

    1. https://pubchem.ncbi.nlm.nih.gov

    2. https://chealth.canoe.com/drug/getdrug/sporanox-capsules

 

palonosetron

Print Friendly, PDF & Email

Sharing to Spread to the World

Leave a Reply

Your email address will not be published.