Palonosetron


Generic Medicine Info
Indications and Dosage
Intravenous
Prophylaxis of chemotherapy-induced nausea and vomiting
Adult: For cases associated with moderately or highly emetogenic cancer chemotherapy: 250 mcg as a single dose via bolus inj over 30 seconds to be given approx 30 minutes before chemotherapy.
Child: ≥1 month to 17 years For cases associated with moderately or highly emetogenic cancer chemotherapy: 20 mcg/kg (Max: 1,500 mcg) as a single dose via infusion over 15 minutes to be given approx 30 minutes before chemotherapy

Intravenous
Prophylaxis of postoperative nausea and vomiting
Adult: 75 mcg as a single dose administered over 10 seconds immediately prior to the induction of anaesthesia.

Oral
Prophylaxis of chemotherapy-induced nausea and vomiting
Adult: For cases associated with moderately emetogenic cancer chemotherapy: 500 mcg approx 1 hour prior to the start of chemotherapy.
Special Precautions
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.
Adverse Reactions
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
Patient Counseling Information
This drug may cause dizziness, somnolence or fatigue; if affected, do not drive or operate machinery.
Monitoring Parameters
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.
Drug Interactions
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.
Action
Description: 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.
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
Cap: Store between 15-30°C. Solution for inj: Store between 15-30°C. Do not freeze. Protect from light.
MIMS Class
Antiemetics / Supportive Care Therapy
ATC Classification
A04AA05 - palonosetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.
References
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.

Disclaimer: This information is independently developed by MIMS based on Palonosetron from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 MIMS. All rights reserved. Powered by MIMS.com
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