Palonosetron

Indications
 Intravenous
Nausea and vomiting associated with cancer chemotherapy
Adult: 250 mcg as a single dose. To be given over 30 sec and 30 minutes before chemotherapy. Do not repeat within 7 days.
Intravenous
Prophylaxis of postoperative nausea and vomiting
Adult: 75 mcg as a single dose immediately before induction of anaesthesia.

Reconstitution: Physically and chemically stable at concentrations of 5 and 30 mcg/ml in glucose 5%, sodium chloride 0.9%, glucose 5% in lactated Ringer's for at least 48 hr at room temperature, exposed to light and for 14 days under refridgeration.
Incompatibility: Y-site incompatibility: Methylprednisolone.
Warnings / Precautions
 Patients with intestinal obstruction or ileus. Rapid inj may lead to temporary visual changes e.g. blurred vision. Patients who have or may develop prolonged QT intervals. Safety and efficacy not established in children <18 yr. Counsel patients who handle skilled tasks e.g. driving may be impaired.
Adverse Reactions
 Headache; flushing; fatigue, dizziness, drowsiness; hiccups; chest pain, tachycardia and bradycardia; diarrhoea, constipation, flatulence; dry mouth; urinary retention; dyspepsia, abdominal pain; changes in BP; asthenia; anxiety, euphoria, paraesthesia, peripheral neuropathy; anorexia; motion sickness; influenza-like symptoms; glycosuria, hyperglycaemia; electrolyte disturbance; arthralgia, eye irritation; amblyopia; tinnitus; rash, pruritus.
Drug Interactions
 May have additive effect on prolonging QT with drugs e.g. moxifloxacin, erythromycin, antipsychotics and TCAs.
See Below for More palonosetron Drug Interactions
Mechanism of Actions
 Palonosetron is a selective 5-HT3 antagonist that is used in the prevention of acute and delayed emesis in emetogenic cancer chemotherapy regimens.
Absorption: Cmax is dose proportional.
Distribution: Volume of distribution: 6.9-7.9 l/kg. Protein binding: Approx 62%.
Metabolism: 40% metabolised via kidney, 50% metabolised by liver CYP2D6 (mainly), CYP3A4 and CYP1A2 isoenzymes. 50% of drug metabolised, <1 % of metabolites have agonist activity on the 5-HT3 receptors.
Excretion: Average terminal half-life: 40 hr.
ATC Classification
 A04AA05 - palonosetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.
Available As
  • Palonosetron 0.25 mg
  • Palonosetron 0.5 mg

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