Palonosetron

Intravenous
Prophylaxis of chemotherapy-induced nausea and vomiting

Intravenous
Prophylaxis of postoperative nausea and vomiting

Oral
Prophylaxis of chemotherapy-induced nausea and vomiting

Patient with history of constipation, signs of subacute intestinal obstruction; known or susceptibility to QT prolongation (e.g. history of QT prolongation, electrolyte abnormalities, CHF, bradyarrhythmia, conduction disturbances, patients taking antiarrhythmics or agents that cause QT prolongation or electrolyte abnormalities). Children. Pregnancy and lactation.

Significant: Hypersensitivity reaction, including anaphylaxis and anaphylactic shock; increased ECG intervals (dose-dependent) such as PR, QT/QTc, QRS duration, and JT intervals; reduced heart rate, increased large bowel transit time.
Cardiac disorders: Tachycardia, sinus bradycardia.
Eye disorders: Eye swelling (oral); eye irritation (IV).
Gastrointestinal disorders: Constipation, diarrhoea, flatulence, abdominal pain.
General disorders and administration site conditions: Asthenia, fatigue. Rarely, inj/infusion site reactions including pain, discomfort, burning sensation, and induration (IV).
Investigations: Increased AST or ALT.
Metabolism and nutrition disorders: Hyperkalaemia.
Musculoskeletal and connective tissue disorders: Myalgia (oral); arthralgia (IV).
Nervous system disorders: Headache, dizziness, somnolence.
Psychiatric disorders: Anxiety, insomnia.
Renal and urinary disorders: Urinary retention.
Skin and subcutaneous tissue disorders: Pruritus, rash.
Vascular disorders: Hypotension.
Potentially Fatal: Serotonin syndrome.

IV/Parenteral/PO: B

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

Correct hypokalaemia and hypomagnesaemia prior to administration. Evaluate allergy history for 5-HT₃ receptor antagonist before administration. Monitor for signs and symptoms of serotonin syndrome.

Potentially Fatal: Increased risk of serotonin syndrome when used with other 5-HT3-antagonists, and other serotonergic agents including SSRIs, selective norepinephrine reuptake inhibitors (SNRIs), MAOIs, mirtazapine, fentanyl, lithium, tramadol and methylthioninium chloride.

Description:
Mechanism of Action: Palonosetron is a selective high-affinity 5-HT₃ receptor antagonist. It inhibits serotonin on vagal nerve terminals in the periphery and centrally in the chemoreceptor trigger zone.
Pharmacokinetics:
Absorption: Well absorbed (oral). Absolute bioavailability: 97% (oral). Time to peak plasma concentration: 5.1 ± 5.9 hours (oral).
Distribution: Widely distributed in the body. Plasma protein binding: Approx 62%. Volume of distribution: 8.3 ± 2.5 L/kg.
Metabolism: Metabolised in the liver (approx 50%) mainly by CYP2D6 and to a lesser extent by CYP3A4 and CYP1A2 isoenzymes into N-oxide-palonosetron and 6-S-hydroxy-palonosetron (inactive metabolites).
Excretion: IV: Via urine (approx 80%; approx 40% as unchanged drug). Oral: Via urine (85-93%; approx 40% as unchanged drug); faeces (5-8%). Terminal elimination half-life: Approx 40 hours.

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

Cap: Store between 15-30°C. Solution for inj: Store between 15-30°C. Do not freeze. Protect from light.

Thuốc chống nôn / Trị liệu chăm sóc nâng đỡ

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

Aloxi 500 micrograms Soft Capsules (Helsinn Birex Pharmaceuticals Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 02/03/2022.

Aloxi 500 micrograms Soft Capsules (Mundipharma Pharmaceuticals Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/03/2022.

Aloxi Capsule (Helsinn Therapeutics [U.S.], Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/03/2022.

Aloxi Injection (Helsinn Therapeutics [U.S.], Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/03/2022.

Aloxi Solution for Injection 50 mcg/mL (Mundipharma Pharmaceuticals Pte Ltd). MIMS Singapore. http://www.mims.com/singapore. Accessed 02/03/2022.

Anon. Palonosetron Hydrochloride. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 02/03/2022.

Anon. Palonosetron. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/03/2022.

Buckingham R (ed). Palonosetron Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/03/2022.

Joint Formulary Committee. Palonosetron. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/03/2022.

Palonosetron 250 micrograms Solution for Injection (Seacross Pharmaceuticals Limited). MHRA. https://products.mhra.gov.uk. Accessed 02/03/2022.