Tropisetron


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Cách dùng
Should be taken on an empty stomach. Take in the morning immediately upon rising 1 hr before breakfast.
Hướng dẫn pha thuốc
IV infusion: Dilute in 100 mL of NaCl 0.9%, glucose 5% inj, Ringer’s soln, mannitol 10%, or KCl 0.3% soln.
Chống chỉ định
Pregnancy and lactation.
Thận trọng
Patient w/ cardiac rhythm or conduction disturbances, uncontrolled HTN. Risk of QT interval prolongation, electrolyte disturbances. Childn.
Phản ứng phụ
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.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness or fatigue, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor BP, ECG and electrolyte abnormalities.
Quá liều
Symptoms: Visual hallucinations, increased BP. Management: Symptomatic treatment. Monitor vital signs closely.
Tương tác
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]).
Tác dụng
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).
Đặc tính

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)

Bảo quản
Store below 25°C.
Phân loại MIMS
Phân loại ATC
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.

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