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Zofran

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Zafron (ondansetron) is a medication used to prevent nausea and vomiting caused by cancer chemotherapy, radiation therapy, or surgery.

How does it work?

The main ingredient of the drug is ondansetron, an antagonist of 5-hydroxytryptamine membrane receptors that are mediators of the hormone serotonin. The effect of the drug is not fully understood. Ondansetron is believed to have an inhibitory effect on serotonin receptors, thereby eliminating the urge to vomit. Its effect extends to the peripheral and central nervous systems.

It should be noted that ondansetron does not interact with dopamine receptors; therefore, it is not effective for motion sickness. At the same time, the drug does not entail sleep disturbances and does not affect the level of lactotropic prolactin in the blood.

The drug has good absorption in the digestive tract and reaches a maximum concentration in the blood after 1.5 hours after oral administration. Metabolism passes in the liver, excretion occurs through the kidneys. The digestibility of the drug increases with the use of the drug with food and can be 100%.
Indications

Prevention and elimination of nausea and vomiting caused by cytostatic chemo- or radiotherapy.

Dosage and administration

The tablets should be swallowed whole, washed down with a sufficient amount of water. The duration of treatment is determined by the attending physician.

Adult patients who undergo chemical therapy and radiation and experience the urge to vomit usually take 8 mg of the drug 2 hours before the procedure and 8 mg after 12 hours. The drug must be taken for 5 days after the procedure of chemical therapy and radiation. When conducting chemotherapy in large doses, it is recommended to increase the dosage of the drug to 24 mg. In this case, the use of the drug should be combined with 12 mg of dexamethasone phosphate and sodium salt 2 hours before the start of the chemical therapy procedure.

Children usually take 4 mg of the drug 2 times a day.

The maximum dose for patients with impaired liver function is 8 mg.

Contraindications

Do not take Zofran tablets if you have any of the following conditions/diseases:

  • hypersensitivity to any component of the drug;
  • pregnancy;
  • lactation;
  • age under 2 years.

Side effects

In some cases, the drug can cause the following adverse effects:

  • upset stool;
  • nausea;
  • vomiting
  • dry mouth;
  • hiccups;
  • an increase in liver enzymes;
  • burning in the anus (with the use of suppositories);
  • cramps;
  • dizziness;
  • headache;
  • arrhythmia;
  • a decrease in blood pressure;
  • bradycardia;
  • cardialgia;
  • skin rash;
  • swelling;
  • itching;
  • visual impairment;
  • anaphylactic shock.

Pregnancy and breastfeeding

The use of Zofran during pregnancy can be prescribed by the attending physician if necessary. To date, there is no data on the safety of ondansetron for the fetus. In case of urgent need to take the drug during lactation, breastfeeding should be interrupted for the time of therapy with ondansetron.

Drug interaction

There is no evidence that ondansetron induces or inhibits the metabolism of other drugs,.

Ondansetron is metabolized by several enzymes of the cytochrome P450 system (CYP3A4, CYP2D6 and CYP1A2). Inhibition or decrease in the activity of one of the enzymes is usually normally compensated by others, and therefore a significant decrease in the overall clearance of ondansetron is unlikely.

However, caution is required when Zofran is used together with:

  • P450 enzymatic inducers (CYP2D6 and CYP1A2) – barbiturates, carbamazepine, carisoprodol, glutethimide, griseofulvin, nitrous oxide, papaverine, phenylbutazone, phenytoin;
  • inhibitors of P450 enzymes (CYP2D6 and CYP1A2) – allopurinol, macrolide antibiotics, MAO-inhibitors, antidepressants, chloramphenicol, cimetidine, oral contraceptives containing estrogen, diltiazem, disulfiram, valproic acid, sodium valproate, erythromycin, fluconazole, fluoroquinolones, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil.

Special studies have shown that ondansetron does not interact with alcohol, temazepam, furosemide, tramadol, and propofol.

Overdose

In most cases, the symptoms of an overdose are similar to adverse reactions when using the drug in recommended doses. There is limited experience with an overdose of ondansetron.

There is no specific antidote for Zofran, therefore, if an overdose occurs, symptomatic and supportive therapy is recommended.