Tropisetron

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Navoban; Belgium: Novaban; Bulgaria: Navoban; Denmark: Navoban; Estonia: Navoban; Finland: Navoban; France: Navoban; Germany: Navoban; Greece: Navoban; Hungary: Navoban; Italy: Navoban; Latvia: Navoban; Lithuania: Navoban; Luxembourg: Navoban; Netherlands: Novaban; Poland: Navoban; Portugal: Navoban; Slovenia: Navoban; Spain: Navoban; Sweden: Navoban.

Latin America

Mexico: Navoban.

Asia

Japan: Navoban.

Drug combinations

Chemistry

Tropisetron: C~17~H~20~N~2~O~2~. Mw: 284.35. 1αH,5αH-Tropan-3α-yl indole-3-carboxylate. CAS-89565-68-4.

Pharmacologic Category

Antiemetics; 5-HT~3~ Receptor Antagonists. (ATC-Code: A04AA03).

Mechanism of action

A highly potent and selective competitive antagonist of 5-HT~3~ receptor, a subclass of serotonin receptors located on peripheral neurons and within CNS. Tropisetron selectively blocks excitation of presynaptic 5-HT~3~ receptors of peripheral neurons in this reflex, and may exert additional direct actions within CNS on 5-HT~3~ receptors mediating actions of vagal input to area postrema. These effects are considered to be the underlying mechanism of action of the anti-emetic effect of tropisetron.

Therapeutic use

Prevention of cancer-chemotherapy-induced nausea and vomiting. Treatment of post-operative nausea and vomiting.

Pregnancy and lactiation implications

Must not be given to pregnant women. Unknown whether tropisetron is excreted into human milk.

Unlabeled use

Contraindications

Known hypersensitivity to tropisetron, other 5-HT~3~ receptor antagonists, or any other components of the formulation.

Warnings and precautions

In poor metabolizers of sparteine/debrisoquine (about 8% of the Caucasian population) the elimination half-life of tropisetron is prolonged (4-5 times longer than in extensive metabolizers). Studies indicate that, for 6-day courses in patients with poor metabolism, the usual daily dose of 5 mg does not need to be reduced. No change in the pharmacokinetics of tropisetron occurs in acute hepatitis or fatty liver disease. In contrast, liver cirrhosis or impaired kidney function may have plasma concentrations up to 50% higher than those found in healthy volunteers belonging to the group of extensive metabolizers of sparteine/debrisoquine. Nevertheless, no dosage reduction is necessary in such patients when recommended 6-day courses of 5 mg tropiseron per day are given. In uncontrolled hypertension, daily doses of tropiseron higher than 10 mg should be avoided, since they may cause further increase in blood pressure. Caution should be exercised in cardiac rhythm or conduction disturbances, or in patients treated with anti-arrhythmic or β-adrenergic-blocking agents, since in these patient groups limited experience is available with concurrent use of tropiseron and anesthetics.

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