Tropisetron

pharmacological · digestive · nervous · Oral · IV

Tropisetron. Serotonin 5-HT3 receptor antagonist used as an antiemetic; CYP2D6 activity contributes to variability in its exposure. Oral half-life 5.7 h.

Serotonin 5-HT3 receptor antagonist used as an antiemetic; CYP2D6 activity contributes to variability in its exposure.

PK: The 5.7-hour half-life and mean 0.60 oral bioavailability come from PMID:11736884, an 18-volunteer single-dose crossover study. Individual bioavailability varied widely. The study dose is not represented as a general dosing recommendation. MASS: PubChem CID 656665, free compound, molecular weight 284.35 g/mol; salt forms may differ. PK: PMID:11736884 reports IV half-life 5.6 h and volume 678 L following 2 mg IV. Oral and IV data share a crossover study; oral absorption rate remains unauthored.

Pharmacokinetics

• Oral — t½ 5.7 h · F 60%
• IV — t½ 5.6 h · F 100% · Vd 678 L

Sources: PMID:11736884, PMID:12728290, PMID:7661573, PMID:9196997