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Pharmacology of ondansetron (Zofran) ; Mechanism of action, Pharmacokinetics, Uses, Effects
Ondansetron, marketed under the brand name Zofran, is a serotonin 5-HT3 receptor antagonist used primarily to prevent nausea and vomiting caused by chemotherapy, radiation therapy, and surgery.
Mechanism of Action
Ondansetron works by blocking the action of serotonin at the 5-HT3 receptors, which are located in the vagal nerve terminals and chemoreceptor trigger zone in the brain. By inhibiting serotonin from binding to these receptors, it helps prevent nausea and vomiting.
Indications
Chemotherapy-Induced Nausea and Vomiting (CINV): Used to prevent nausea and vomiting associated with highly emetogenic chemotherapy.
Postoperative Nausea and Vomiting (PONV): Administered before anesthesia or immediately after surgery to prevent nausea and vomiting.
Radiation-Induced Nausea and Vomiting (RINV): Used to prevent nausea and vomiting in patients undergoing total body irradiation or single high-dose fraction therapy to the abdomen.
Administration
Oral: Tablets, orally disintegrating tablets (ODT), and oral solution.
Intravenous (IV): Administered as an IV infusion.
Intramuscular (IM): Administered as an IM injection.
Dosage
Chemotherapy-Induced Nausea and Vomiting: 8 mg orally before chemotherapy, followed by 8 mg every 12 hours for 1-2 days.
Postoperative Nausea and Vomiting: 4 mg IV/IM before anesthesia or 16 mg orally 1 hour before anesthesia.
Radiation-Induced Nausea and Vomiting: 8 mg orally 1-2 hours before radiation therapy.
Side Effects
Common: Headache, constipation, and dizziness.
Serious: QT prolongation, which can lead to arrhythmias such as torsade de pointes.
Precautions
QT Prolongation: Patients with a history of QT prolongation or those taking other medications that prolong the QT interval should use ondansetron with caution.
Renal and Hepatic Impairment: Dosage adjustments may be necessary for patients with severe renal or hepatic impairment.
#ondansetron #Zofran

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