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Zofran is used for preventing nausea and vomiting due to cancer chemotherapy or surgery. It may also be used for other conditions as determined by your doctor.

Brand: Ondansetron

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: May 2024
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Zofran 8 mg
270 pills - 8 mg
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180 pills - 8 mg
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120 pills - 8 mg
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90 pills - 8 mg $82.91 $0.92 $30.94 Add to cart
60 pills - 8 mg $59.97 $1.00 $15.93 Add to cart
30 pills - 8 mg $37.95 $1.27 No Add to cart
Zofran 4 mg
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Product description

Drug Title

Zofran (Ondansetron)

Pharmacological action

Antiemetic drug, selective serotonin 5HT3-receptor antagonist.

Ondansetron is a potent, highly selective 5HT3 receptor antagonist. The mechanism of nausea and vomiting suppression is not exactly known. Radiation therapy and chemotherapy drugs may release serotonin (5NT) in the small intestine, causing the gag reflex through activation of 5NT3 receptors and excitation of afferent vagus nerve endings. Ondansetron blocks initiation of this reflex. Activation of vagus nerve afferents, in turn, can cause release of 5NT in the posterior field of the floor of the fourth ventricle (area postrema) and, therefore, trigger the gag reflex through a central mechanism. Thus, the action of ondansetron to suppress nausea and vomiting provoked by cytotoxic chemotherapy and radiotherapy appears to be due to its antagonistic effect on 5HT3 receptor neurons located both in the periphery and in the CNS.

The mechanism of action of the drug in relief of postoperative nausea and vomiting is unclear, probably it is similar to that in relief of chemo- and radio-induced nausea and vomiting.

Ondansetron has no effect on plasma prolactin concentration.



After oral administration ondansetron is completely absorbed from gastrointestinal tract and undergoes "first pass" effect through liver. Cmax is reached approximately 1.5 hours after intake. Bioavailability is slightly increased with concomitant food intake, but does not change when taking antacids.

After rectal administration ondansetron is determined in plasma after 15-60 minutes. The concentration of the active substance increases linearly, Cmax is reached approximately 6 hours after administration and is 20-30 ng/ml. Plasma concentrations decrease at a slower rate than after oral administration (due to ongoing absorption). Absolute bioavailability is 60% and does not depend on gender.


The distribution of ondansetron is the same when administered orally, v/m and intravenously; Vd at equilibrium is about 140 l. Binding to plasma proteins is 70-76%.

Pharmacokinetic parameters of ondansetron do not change when administered repeatedly orally, parenterally or rectally.


Ondansetron is eliminated from systemic blood flow mainly as a result of metabolism in liver with the participation of several enzyme systems.

When administered in doses exceeding 8 mg, blood content of ondansetron increases disproportionately since when administered in high oral doses, its metabolism may be decreased during "first passage" through the liver.

The absence of CYP2D6 enzyme (debrisokvin polymorphism) does not affect ondansetron pharmacokinetics.


Less than 5% of the administered dose is excreted unchanged in the urine. T1/2 after oral, IM and IV administration is approximately 3 hours.

T1/2 after rectal administration is 6 hours.

Pharmacokinetics in special clinical cases

Distribution of ondansetron depends on sex of patients. Thus, in women, when taking the drug orally, a higher rate and degree of absorption of ondansetron and a decrease in systemic clearance and Vd are noted.

In patients with an IQ of 15-60 ml/min both systemic clearance and Vd of ondansetron are decreased, which results in a small and clinically insignificant increase of T1/2 (up to 5.4 h). Pharmacokinetics of ondansetron is virtually unchanged in patients with severe renal impairment who are on hemodialysis.

In patients with severe hepatic impairment systemic clearance of ondansetron decreases sharply, as a result its T1/2 is increased (up to 15-32 h), and bioavailability in per oral administration reaches 100% due to the decrease of presystemic metabolism.

Studies in healthy elderly volunteers have shown a slight, clinically insignificant, age-dependent increase in bioavailability and T1/2, which can be up to 5 h.

While studying the action of ondansetron in children, the absolute clearance and Vd values were decreased after a single injection of 2 mg (children aged 3-7 years) or 4 mg (children aged 8-12 years), and the magnitude of the change depended on the age. Thus, children aged 12 years had a clearance of 300 ml/min, and children aged 3 years had a clearance of 100 ml/min, Vd of 75 L and 17 L, respectively. Adjustment of the dose to patients' body weight (0.1 mg/kg, up to a maximum of 4 mg) compensates for these changes and normalizes the systemic exposure of ondansetron in children.

The experience of using Zofran in elderly patients and patients with renal insufficiency is limited by the IV and oral routes of administration, but it can be assumed that when using the drug in suppository form, the T1/2 in such patients will not differ from the T1/2 in healthy volunteers, since the excretion rate of ondansetron when suppositories are given does not depend on systemic clearance.

Contraindications to use

  • pregnancy;
  • Lactation (breast-feeding);
  • Childhood under 6 months;
  • Concomitant use with apomorphine;
  • Hypersensitivity to the drug components.

Caution should be exercised when using the drug in patients with cardiac rhythm and conduction disorders, patients receiving antiarrhythmic agents and beta-adrenoblockers and patients with significant electrolyte disturbances; with the risk of developing or already existing prolonged QT interval; congenital prolonged QT interval syndrome; patients taking other drugs that lead to QT interval prolongation; with hypersensitivity reaction to other 5HT3-receptor antagonists.

Administration during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breast-feeding).

Administration if liver function abnormalities

When administering this drug to patients with hepatic impairment, the daily dose should not exceed 8 mg.

Administration in renal impairment

No special adjustment of the dosage, the frequency of administration or the method of application is required in case of renal failure.

Administration in children

Contraindicated in children under 6 months of age.

It is possible to use in children older than 6 months according to the dosage regimen.

Administration in elderly patients

Regardless the method of administration, in elderly patients a change of dosage regimen is not required.

Indications of Zofran

Prevention and relief of nausea and vomiting caused by cytostatic chemotherapy or radiotherapy;

Prevention and relief of nausea and vomiting during postoperative period.

Dosing regimen

Nausea and vomiting during cytostatic chemotherapy or radiation therapy


The choice of dosing regimen is determined by the emetogenicity of antitumor therapy.

In moderate emetogenic chemotherapy or radiotherapy, the drug is prescribed in a dose of 8 mg (10 ml syrup) 1-2 hours before the start of basic therapy, followed by another 8 mg 12 hours later.

In high-emetogenic chemotherapy (e.g., high-dose cisplatin), the recommended dose is 24 mg (30 ml syrup) concomitantly with an oral dose of dexamethasone sodium phosphate 12 mg 1-2 hours before the start of chemotherapy.

To prevent late or prolonged vomiting that occurs 24 hours after chemotherapy or radiation therapy, Zofran should be continued in a dose of 8 mg (10 ml) 2 times daily for 5 days.

Children and adolescents aged 6 months to 17 years

The dose of Zofran in children and adolescents is calculated based on surface area or body weight.

Zofran is usually administered as a solution for injection once intravenously just before the start of chemotherapy followed by oral administration of Zofran® in the form of syrup 12 hours later. Zofran® syrup should be continued for 5 days after chemotherapy.

Nausea and vomiting in the postoperative period

In adults for prevention of nausea and vomiting during postoperative period it is recommended to administer Zofran® in dose 16 mg (20 ml syrup) 1 hour before nausea. For relief of postoperative nausea and vomiting Zofran® in the form of solution for injection is used (the use of this dosage form is determined by the patient's state during the postoperative period).

In children aged 6 months to 17 years old for prevention and relief of postoperative nausea and vomiting Zofran® is administered by intravenous injection (application of this dosage form is determined by the patient's condition during postoperative period).

Other categories of patients

Dosage adjustment is not required for elderly patients.

Patients with impaired renal function do not require dose adjustment of Zofran.

In patients with moderate to severe hepatic impairment the clearance of ondansetron is significantly decreased, T1/2 is increased. The daily dose of the drug should not exceed 8 mg (10 mg syrup).

Patients with delayed metabolism of sparteine/debrisoquine do not require adjustment of the daily dose or frequency of ondansetron administration.