Palonosetron

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Palonosetron.jpg

[edit] MECHANISM OF ACTION

Palonosetron is an antinauseant and antiemetic agent. It acts as a selective serotonin 5-HT3 receptor antagonist.

Cancer chemotherapy may be associated with a high incidence of nausea and vomiting, particularly when certain agents, such as cisplatin, are used. 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine and that the released serotonin then activates 5-HT3 receptors located on vagal afferents to initiate the vomiting reflex.

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

[edit] INDICATIONS

Injection:

  • Prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately or highly emetogenic cancer chemotherapy
  • Prevention of postoperative nausea and vomiting for up to 24 hours following surgery

Capsules:

  • Capsules are indicated in adults for the prevention of acute nausea and vomiting associated with moderately emetogenic cancer chemotherapy

[edit] DOSAGE

  • Chemotherapy-induced nausea and vomiting:
    • Adult dosage:
      • Injection: A single 0.25 mg I.V. dose administered over 30 seconds, approximately 30 minutes before the start of chemotherapy.
      • Capsule: One 0.5 mg capsule administered approximately one hour prior to the start of chemotherapy
  • Postoperative Nausea and Vomiting
    • Adult dosage: a single 0.075 mg I.V. dose administered over 10 seconds immediately before the induction of anesthesia.

[edit] DOSAGE FORMS AND STRENGTHS

  • 0.25 mg/5 mL single-use vial
  • 0.075 mg/1.5 mL single-use vial
  • 0.5 mg Capsules

[edit] CONTRAINDICATIONS

Hypersensitivity to the drug

[edit] WARNINGS AND PRECAUTIONS

  • Hypersensitivity reactions, including anaphylaxis, have been reported with or without known hypersensitivity to other selective 5-HT3 receptor antagonists

[edit] INTERACTIONS

The potential for clinically significant drug interactions with Palonosetron appears to be low

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US)
  • In nursing mothers a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother

[edit] 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.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

http://www.aloxi.com/common/downloads/PI-FINAL.pdf

[edit] REFERENCES

Antiemetics
5-HT3 receptor antagonists Dolasetron   Granisetron   Ondansetron   Palonosetron   Tropisetron
Dopamine antagonists Alizapride   Bromopride   Clebopride   Domperidone   Metoclopramide   Prochlorperazine   Thiethylperazine
H1 antagonists Dimenhydrinate   Meclizine
NK1 receptor antagonists‎ Aprepitant   Fosaprepitant   Maropitant
Motion sickness‎ Cinnarizine   Dimenhydrinate   Meclizine   Meclizine/Pyridoxine   Scopolamine (Patch)
Pregnancy Meclizine/Pyridoxine   Ondansetron
Veterinary Maropitant