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  • Absorption: Owing to hepatic first-pass metabolism, its bioavailability is only about 60%.
  • Distribution: Plasma protein binding of ondansetron as measured in vitro was 70% to 76%, over the pharmacologic concentration range of 10 to 500 ng/mL. Circulating drug also distributes into erythrocytes.
  • Metabolism: Ondansetron is extensively metabolized in humans, with approximately 5% of a radiolabeled dose recovered as the parent compound from the urine. The primary metabolic pathway is hydroxylation on the indole ring followed by subsequent glucuronide or sulfate conjugation.
  • Elimination: In adult cancer patients, the mean ondansetron elimination half-life was 4.0 hours, and there was no difference in the multidose pharmacokinetics over a 4-day period.


  • Prevention of nausea and vomiting associated with highly emetogenic chemotherapy, including cisplatin ≥50mg/m2.
  • Prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic chemotherapy.
  • Prevention of nausea and vomiting associated with radiotherapy in patients receiving total body irradiation, single high-dose fraction to the abdomen, or daily fractions to the abdomen.
  • Prevention of post-op nausea and vomiting.
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