Palonosetron

Intravenous
Nausea and vomiting associated with cancer chemotherapy

Intravenous
Prophylaxis of postoperative nausea and vomiting

Oral
Nausea and vomiting associated with cancer chemotherapy

Patient w/ history of constipation, intestinal obstruction, history or risk of QT interval prolongation, electrolyte abnormalities. Childn. Pregnancy and lactation.

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

This drug may cause dizziness, somnolence or fatigue, if affected, do not drive or operate machinery.

Monitor for signs and symptoms of serotonin syndrome.

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].

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.

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

Store between 20-25°C. Protect from light.

Antiemetics / Supportive Care Therapy

A04AA05 - palonosetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.

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.