Tropisetron


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : IV Prophylaxis of nausea and vomiting associated with cytotoxic therapy 5 mg by slow IV inj over at least 1 min or by IV infusion over 15 min to be given 15 min before chemotherapy on day 1. PO 5 mg once daily before chemotherapy on day 2-6 following IV dose given on day 1. Duration of treatment: 5 days. Treatment and prophylaxis of postoperative nausea and vomiting 2 mg as single dose or once daily by bolus inj over 30 sec or by IV infusion over 15 min w/in 2 hr at the end of anaesth (treatment) or before induction of anaesth (prophylaxis).
Dosage Details
Intravenous
Prophylaxis of nausea and vomiting associated with cytotoxic therapy
Adult: 5 mg by slow IV inj over at least 1 min or by IV infusion over 15 min to be given 15 min before chemotherapy on day 1, followed by oral preparation on day 2-6.
Child: >2 yr 0.2 mg/kg (max: 5 mg) by slow IV inj over at least 1 min or by IV infusion at a concentration of 0.05 mg/ mL over 15 min to be given as a single dose before chemotherapy on day 1. >25 kg: Continue once daily at the same dose up to day 5 of chemotherapy.

Intravenous
Treatment and prophylaxis of postoperative nausea and vomiting
Adult: 2 mg as single dose or once daily by bolus inj over 30 sec or by IV infusion over 15 min w/in 2 hr at the end of anaesth (treatment) or before induction of anaesth (prophylaxis).

Oral
Prophylaxis of nausea and vomiting associated with cytotoxic therapy
Adult: 5 mg once daily before chemotherapy on day 2-6 following IV dose given on day 1. Duration of treatment: 5 days.
Child: >2 yr 0.2 mg/kg once daily before chemotherapy on day 2-6 following IV dose given on day 1. Duration of treatment: 5 days.
Special Patient Group
Patient w/ uncontrolled HTN: Max dose: 10 mg daily.
Administration
Should be taken on an empty stomach. Take in the morning immediately upon rising 1 hr before breakfast.
Reconstitution
IV infusion: Dilute in 100 mL of NaCl 0.9%, glucose 5% inj, Ringer’s soln, mannitol 10%, or KCl 0.3% soln.
Contraindications
Pregnancy and lactation.
Special Precautions
Patient w/ cardiac rhythm or conduction disturbances, uncontrolled HTN. Risk of QT interval prolongation, electrolyte disturbances. Childn.
Adverse Reactions
Significant: QT prolongation. Rarely, hypersensitivity reactions (e.g. anaphylaxis).
Nervous: Headache, constipation, dizziness, fatigue, visual hallucinations, somnolence, syncope.
CV: HTN, hypotension.
GI: Abdominal pain, diarrhoea, anorexia.
Resp: Dyspnoea, acute bronchospasm, chest discomfort.
Dermatologic: Urticaria.
Potentially Fatal: Rarely, collapse and CV arrest.
Patient Counseling Information
This drug may cause dizziness or fatigue, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor BP, ECG and electrolyte abnormalities.
Overdosage
Symptoms: Visual hallucinations, increased BP. Management: Symptomatic treatment. Monitor vital signs closely.
Drug Interactions
Decreased plasma concentration w/ rifampicin or other liver enzyme-inducers (e.g. phenobarbital). Increased risk of conduction abnormalities w/ antiarrhythmics, β-blockers. Risk of serotonin syndrome w/ serotonergic drugs (e.g. serotonin and norepinephrine reuptake inhibitors [SNRIs or SSRIs]).
Action
Description: Tropisetron is a potent and selective serotonin (5-HT3) receptor antagonist. It competitively blocks serotonin peripherally on vagal nerve terminal and centrally in the chemoreceptor trigger zone.
Duration: 24 hr.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Time to peak plasma concentration: W/in 3 hr. Bioavailability: 60%.
Distribution: Volume of distribution: 400-600 L. Plasma protein binding: 71%.
Metabolism: Undergoes hepatic first-pass metabolism by CYP2D6 via hydroxylation of its indole ring and via conjugation to glucuronide/sulfate.
Excretion: Mainly via urine (approx 8%, as unchanged drug; 70%, as metabolites); faeces (15%, as metabolites). Elimination half-life: Approx 8 hr (extensive metabolisers); 45 hr (poor metabolisers).
Chemical Structure

Chemical Structure Image
Tropisetron

Source: National Center for Biotechnology Information. PubChem Database. Tropisetron, CID=656665, https://pubchem.ncbi.nlm.nih.gov/compound/Tropisetron (accessed on Jan. 23, 2020)

Storage
Store below 25°C.
ATC Classification
A04AA03 - tropisetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.
References
AFT Pharmaceuticals Ltd. Tropisetron AFT data sheet May 2017. Medsafe. http://www.medsafe.govt.nz/. Accessed 23/11/2017.

Anon. Tropisetron. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 23/11/2017.

Buckingham R (ed). Tropisetron. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/11/2017.

Disclaimer: This information is independently developed by MIMS based on Tropisetron 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 © 2020 MIMS. All rights reserved. Powered by MIMS.com
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