ZOFRAN AND DEXTROSE IN PLASTIC CONTAINER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZOFRAN AND DEXTROSE IN PLASTIC CONTAINER (ZOFRAN AND DEXTROSE IN PLASTIC CONTAINER).
Ondansetron is a selective serotonin 5-HT3 receptor antagonist. It blocks the action of serotonin at 5-HT3 receptors in the chemoreceptor trigger zone (CTZ) and gastrointestinal tract, thereby preventing nausea and vomiting. Dextrose provides caloric support.
| Metabolism | Ondansetron is extensively metabolized in the liver via hydroxylation, followed by glucuronide or sulfate conjugation. The major metabolic pathway involves CYP1A2, CYP2D6, and CYP3A4 enzymes. |
| Excretion | Primarily hepatic metabolism (~95%) via CYP1A2, CYP2D6, and CYP3A4; less than 10% excreted unchanged in urine. Fecal excretion accounts for ~20% of metabolites. |
| Half-life | Terminal elimination half-life is approximately 3–4 hours in adults, though may be prolonged to 5–8 hours in severe hepatic impairment (Child-Pugh class C) or elderly patients. |
| Protein binding | Approximately 70–76% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 1.9–2.4 L/kg, indicating extensive extravascular distribution. |
| Bioavailability | Not applicable for IV route; oral bioavailability is approximately 60% (due to first-pass metabolism). |
| Onset of Action | IV: Onset of antiemetic effect occurs within 1–2 minutes following intravenous administration. |
| Duration of Action | Duration of action is typically 4–8 hours, sufficient for prophylaxis of chemotherapy-induced nausea and vomiting for moderate emetogenic regimens. |
4 mg IV or IM every 8 hours as needed; for prevention of chemotherapy-induced nausea and vomiting, 0.15 mg/kg IV up to 16 mg per dose, infused over 15 minutes, given 30 minutes before chemotherapy, then repeat at 4 and 8 hours after first dose, or as a single 32 mg IV dose over 15 minutes immediately before chemotherapy.
| Dosage form | INJECTABLE |
| Renal impairment | No dosage adjustment required for renal impairment; however, patients with severe renal impairment (creatinine clearance < 30 mL/min) have modest increase in half-life, but no adjustment recommended. |
| Liver impairment | For Child-Pugh class A (mild): no adjustment. For Child-Pugh class B or C (moderate to severe): maximum daily dose of 8 mg (IV or oral) due to reduced clearance and increased half-life. |
| Pediatric use | For chemotherapy-induced nausea and vomiting: 0.15 mg/kg IV (maximum 16 mg per dose) given 30 minutes before chemotherapy, then at 4 and 8 hours after first dose. For postoperative nausea and vomiting: children 1 month to 12 years: 0.1 mg/kg IV (maximum 4 mg) as a single dose; children 12 years and older: 4 mg IV as a single dose. |
| Geriatric use | No specific dose adjustment required; pharmacokinetics similar to younger adults. Use caution with electrolyte abnormalities (e.g., hypokalemia, hypomagnesemia) due to potential QT prolongation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ZOFRAN AND DEXTROSE IN PLASTIC CONTAINER (ZOFRAN AND DEXTROSE IN PLASTIC CONTAINER).
| Breastfeeding | Ondansetron is excreted into breast milk in small amounts; infant plasma levels are low. The M/P ratio is approximately 1.0 (mean). No adverse effects reported in breastfed infants. Caution is advised, but compatible with breastfeeding if clinically needed. |
| Teratogenic Risk | First trimester: Limited human data; animal studies show no teratogenicity at clinically relevant doses. Second/third trimesters: No documented fetal abnormalities; use only if clearly needed. No known risk of congenital malformations based on available evidence. |
■ FDA Black Box Warning
No FDA black box warning for this product.
| Serious Effects |
["Hypersensitivity to ondansetron or any component of the formulation","Concomitant use with apomorphine (increased risk of profound hypotension and loss of consciousness)"]
| Precautions | ["Risk of QT prolongation and torsade de pointes, especially with concomitant use of other QT-prolonging drugs or electrolyte abnormalities","Hypersensitivity reactions, including anaphylaxis and bronchospasm","Serotonin syndrome when used with other serotonergic drugs","Masking of progressive ileus or gastric distension after abdominal surgery","Hepatic impairment reduces clearance; dose adjustment may be necessary"] |
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| Fetal Monitoring | Standard maternal monitoring via intravenous infusion rate and fluid balance (dextrose component). Fetal heart rate monitoring not routinely required; observe for maternal cardiac arrhythmias (QT prolongation risk) with ECG monitoring if cofactors present. |
| Fertility Effects | No evidence of impaired fertility or reproductive performance in animal studies. Human data insufficient to assess risk; no known adverse effect on human fertility. |