Palonosetron


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Nausea and vomiting associated w/ cancer chemotherapy 500 mcg 1 hr before therapy. IV Nausea and vomiting associated w/ cancer chemotherapy 250 mcg over 30 sec approx 30 min before therapy. Prophylaxis of postoperative nausea and vomiting 75 mcg over 10 sec before induction of anaesthesia.
Dosage Details
Intravenous
Nausea and vomiting associated with cancer chemotherapy
Adult: 250 mcg by bolus inj over 30 sec to be given approx 30 min before chemotherapy.
Child: 1 mth to 17 yr 20 mcg/kg (max: 1,500 mcg) by infusion over 15 min to be given approx 30 min before chemotherapy.

Intravenous
Prophylaxis of postoperative nausea and vomiting
Adult: 75 mcg by bolus inj over 10 sec immediately before induction of anaesthesia.

Oral
Nausea and vomiting associated with cancer chemotherapy
Adult: 500 mcg 1 hr before chemotherapy.
Special Precautions
Patient w/ history of constipation, intestinal obstruction, history or risk of QT interval prolongation, electrolyte abnormalities. Childn. Pregnancy and lactation.
Adverse Reactions
Significant: QT prolongation, bradycardia, hypersensitivity reactions (e.g. anaphylaxis).
Nervous: Headache, dizziness, somnolence, fatigue, weakness, anxiety, vertigo, flu-like symptoms, insomnia, paresthesia.
CV: Nonsustained tachycardia, hypotension, HTN, MI, hot flush.
GI: Constipation, diarrhoea, abdominal pain, dyspepsia, dry mouth, hiccups, flatulence, anorexia.
Hepatic: Increased serum ALT/AST, bilirubin.
Genitourinary: Urinary retention.
Endocrine: Hyperkalaemia, electrolyte fluctuations, hyperglycaemia, metabolic acidosis, glycosuria.
Musculoskeletal: Arthralgia.
Ophthalmologic: Amblyopia.
Otic: Tinnitus.
Dermatologic: Pruritus, rash, allergic dermatitis.
Others: Inj site reaction.
Potentially Fatal: Rarely, serotonin syndrome (e.g. altered mental status, autonomic instability, neuromuscular symptoms).
IV/Parenteral/PO: B
Patient Counseling Information
This drug may cause dizziness, somnolence or fatigue, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor for signs and symptoms of serotonin syndrome.
Drug Interactions
Decreased therapeutic effect of tramadol.
Potentially Fatal: Increased risk of serotonin syndrome w/ serotonergic agents [e.g. SSRI, serotonin and norepinephrine reuptake inhibitors (SNRIs), MAOIs, mirtazapine].
Action
Description: Palonosetron is a selective high-affinity receptor antagonist of 5-HT3 receptor w/ little or no affinity for other serotonin receptors. It blocks serotonin peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Absolute bioavailability: 97% (oral). Time to peak plasma concentration: Approx 5 hr (oral).
Distribution: Volume of distribution: Approx 7-8 L/kg. Plasma protein binding: Approx 62%.
Metabolism: Metabolised by CYP to inactive metabolite, N-oxide-palonosetron and 6-S-hydroxy-palonosetron.
Excretion: Mainly via urine (80%; 40%, as unchanged drug); faeces (5-8%). Elimination half-life: Approx 40 hr.
Chemical Structure

Chemical Structure Image
Palonosetron

Source: National Center for Biotechnology Information. PubChem Database. Palonosetron, CID=6337614, https://pubchem.ncbi.nlm.nih.gov/compound/Palonosetron (accessed on Jan. 22, 2020)

Storage
Store between 20-25°C. Protect from light.
ATC Classification
A04AA05 - palonosetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.
References
Aloxi Palonosetron Hydrochloride Injection (Eisai Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/09/2017.

Anon. Palonosetron. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/09/2017.

Buckingham R (ed). Palonosetron Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/09/2017.

Joint Formulary Committee. Palonosetron. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/09/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Palonosetron Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 20/09/2017.

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