Palonosetron


Full Prescribing Info
Dosage/Direction for Use

Oral
Nausea and vomiting associated with cancer chemotherapy
Adult: 500 mcg 1 hr before chemotherapy.

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.
Special Precautions
Patient w/ history of constipation, intestinal obstruction, history or risk of QT interval prolongation, electrolyte abnormalities. Childn. Pregnancy and lactation. Patient Counselling This drug may cause dizziness, somnolence or fatigue, if affected, do not drive or operate machinery. Monitoring Parameters Monitor for signs and symptoms of serotonin syndrome.
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).
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
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.
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.
Storage
Intravenous: Store between 20-25°C. Protect from light. Oral: 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.
Disclaimer: This information is independently developed by CIMS 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 CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS 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 © 2020 CIMS. All rights reserved. Powered by CIMSAsia.com
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