Ondansetron (Zofran) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic. Its effects are thought to be on both peripheral and central nerves. Ondansetron (Zofran) decreases the activity of the vagus nerve, which deactivates the vomiting center in the medulla oblongata, and also inhibits serotonin receptors in the chemoreceptor trigger zone. Ondansetron (Zofran) has little effect on vomiting caused by motion sickness, and does not have any effect on dopamine receptors or muscarinic receptors. The 5-HT3 receptor antagonists are the primary drugs used to treat and prevent chemotherapy-induced nausea and vomiting (CINV). Ondansetron (Zofran) is also effective in controlling post-operative nausea and vomiting (PONV) and post-radiation nausea and vomiting, and is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute gastroenteritis. Although ondansetron is highly effective, the high cost of the brand-name version had limited its use to controlling PONV and CINV.Ondansetron (Zofran) is also used off-label to treat hyperemesis gravidarum in pregnant women, but there is no conclusive data available on its safety in pregnancy, especially during the first trimester. Ondansetron (Zofran) is also used to treat cyclic vomiting syndrome.
Molecular Weight | 293.36 |
Formula | C18H19N3O |
CAS Number | 99614-02-5 |
Solubility (25°C) | DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Allison C Bennett, et al. The role of ondansetron in the treatment of schizophrenia
[3] V Thavaraj, et al. Ondansetron
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