Adults. Prevention and inhibition of nausea and vomiting caused by chemotherapy or radiotherapy of tumors. Prevention and treatment of nausea and vomiting in the postoperative period.Children and youth. Prevention and suppression of nausea and vomiting induced by cancer chemotherapy in children ≥6 months.
A strong and selective antagonist of 5-HT serotonin receptors3 in neurons located both in the peripheral and in o.u.n. By blocking these receptors (peripheral and central), it inhibits the gag reflex resulting from their stimulation by serotonin released by ionizing radiation and cytostatics. Thus, it strongly inhibits nausea and vomiting caused by chemotherapy and radiotherapy. Ondansetron does not affect the concentration of prolactin in the blood. Following oral administration, ondansetron is completely absorbed from the gastrointestinal tract and undergoes a "first pass" effect: after a dose of 8 mg, the maximum concentration in the blood occurs after about 1.5 hours. The presence of food causes a slight reduction in bioavailability.0,5 is about 3 hours. Ondansetron binds to 70-76% plasma proteins. It is metabolized in the liver. Less than 5% of the absorbed dose is excreted in the urine in unchanged form. The pharmacokinetic properties of ondansetron do not change during repeated administration of the drug. Studies conducted in healthy elderly volunteers showed clinically insignificant, age-related, increased bioavailability of the drug (up to 65%) and an increase in half-life (up to 5 hours). In patients with impaired renal function (creatinine clearance 15-60 ml / min) there is a reduction in both the total clearance and volume of drug distribution, resulting in a slight, clinically unimportant increase in half-life (up to 5.4 hours). In patients with severe hepatic impairment, there is a significant reduction in the clearance of ondansetron, an increase in half-life (up to 15-32 h) and an increase in bioavailability of up to 100% (due to the reduction of the "first pass" effect).
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Concomitant use with apomorphine (risk of deep hypotension and unconsciousness).
Precautions:
Carefully use in patients with sub-acute intestinal obstruction (ondansetron may increase intestinal transit time) and in patients with moderate or severe hepatic impairment. Special care should be taken in patients with arrhythmias or conduction disorders, in patients taking anti-arrhythmic or adrenergic blockers ß, and in patients with electrolyte disturbances. Hypersensitivity reactions may occur in patients who have been hypersensitive to other selective inhibitors of 5-HT serotonin receptors3. In patients after adenotomy and tonsillectomy, ondansetron may mask latent bleeding. Children receiving ondansetron together with hepatotoxic chemotherapeutics should be closely monitored for liver dysfunction. Due to the lactose content, the drug should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.
Pregnancy and lactation:
Pregnancy is not recommended. In animals, it has been shown that ondansetron is excreted in milk, therefore it is recommended that mothers receiving ondansetron do not breastfeed.
Side effects:
Very common: headache. Common: a feeling of heat, redness of the face and a feeling of blood clashing to the head, constipation. Uncommon: convulsions, movement disorders (including extrapyramidal reactions such as dystonic, forced upward look, dyskinesia), arrhythmia, chest pain with depression of the ST in the ECG or not, bradycardia, hypotension, hiccups, asymptomatic increase in activity liver enzymes (often in patients receiving cisplatin). Rare: sudden hypersensitivity reactions (sometimes severe, including anaphylactic shock), dizziness (mostly during rapid administration)Lv.), transient visual disturbances (e.g. blurred vision, primarily during administrationi.v.), prolongation of the QTc interval (including ventricular tachycardiatorsade de pointes). Very rare: temporary disappearance of vision (especially during administrationLv .; most of these incidents resolved to 20 min; the majority of patients who have experienced this symptom have taken chemotherapy, including cisplatin; in some cases, transient visual loss was reported as a cortical symptom). The profile of side effects in children and adolescents is consistent with that described in adults.
Dosage:
Orally. NUDGES AND ENTITIES RELEASED BY CHEMOTHERAPY AND RADIOTHERAPY. The route of administration and the dose of ondansetron should be selected individually.aDULTand.Chemotherapy and radiotherapy with moderate vomiting. Ondansetron can be given to the patient orally, intravenously, intramuscularly or rectally. The recommended oral dose is 8 mg for 1-2 hours before the start of chemotherapy. This dose should be repeated after 12 hours. From day 2 to a maximum of 5 days after chemotherapy or radiotherapy with emetic effects, to prevent nausea and delayed or prolonged vomiting, it is recommended to continue to administer ondansetron in oral or rectal forms. The recommended oral dose is 8 mg 2 times a day.Chemotherapy with strong vomiting. On the day of application of a chemotherapeutic with a strong vomiting, eg high doses of Cisplatin, ondansetron can be administered to the patient intravenously, intramuscularly or rectally. From 2 days to a maximum of 5 days after the chemotherapy with strong vomiting, to prevent nausea and delayed or prolonged vomiting, it is recommended to continue to administer ondansetron, in oral or rectal forms. The recommended dose is 8 mg 2 times a day.Children ≥6 months and adolescents. Nausea and vomiting caused by cancer chemotherapy. The dose of ondansetron can be determined either on the body surface or in body weight. Daily doses are higher when converted to body weight than when converted to body surface. Ondansetron solution for injection should be diluted with 5% Glucose or 0.9% sodium chloride solution for intravenous infusion or other compatible infusion solution and infused into a vein over a period of not less than 15 min. There are no data from controlled clinical trials regarding the use of ondansetron in the prevention of delayed or prolonged nausea or vomiting induced by chemotherapy and the use of ondansetron in children in case of nausea and vomiting induced by radiotherapy.Dosage based on body surface area. Ondansetron should be administered intravenously, at a single dose of 5 mg / m2 pc, immediately before the start of chemotherapy. A single dose administered intravenously can not exceed 8 mg. After 12 h, you can start using ondansetron orally and continue it for 5 days. The total daily dose can not be greater than the adult dose, i.e. 32 mg. Children on pc <0.6 m2: day 1 - 5 mg / m2 pc.i.v. + 2 mg in syrup or tablet after 12 hours, days 2 - 6. - 2 mg in syrup every 12 hours. Children with pc. > 0.6 m2: day 1 - 5 mg / m2 pc.i.v. + 4 mg in syrup or tablet after 12 hours, days 2 - 6. - 4 mg in syrup or tablet every 12 hours.Dose calculated based on body weight. Ondansetron should be administered intravenously, in a single dose of 0.15 mg / kg, immediately before chemotherapy. A single dose administered intravenously can not exceed 8 mg. After 12 hours, ondansetron may be started orally and continued for up to 5 days. The total daily dose can not be greater than the adult dose, i.e. 32 mg. Children about the month of ≤10 kg: day 1 - up to 3 doses of 0.15 mg / kgi.v. every 4 hours, days 2 - 6. - 2 mg in syrup every 12 hours. Children about the month > 10 kg: day 1 - up to 3 doses of 0.15 mg / kgi.v. every 4 hours, days 2 - 6. - 4 mg in syrup or tablet every 12 hours.Special groups of patients. In the elderly, the principles of using the drug and the dosage and frequency of administration are not changed. NUDGES AND EVENTS OF THE POST-OPERATING PERIOD.Adults. In the prevention of nausea and vomiting in the postoperative period, ondansetron can be used both intravenously, intramuscularly and orally; orally 16 mg for 1 h before anesthesia. In the treatment of nausea and vomiting in the post-operative period, intravenous or intramuscular administration is recommended.Children ≥1 months and adolescents. Intravenous use.There are no data on the use of the drug in the treatment of post-operative nausea and vomiting in children under 2 years.Special groups of patients. Experience in elderly people is limited, but it is known that ondansetron is well tolerated by these patients. In patients with renal insufficiency and in patients with disturbed metabolism of sparteine and debrisoquine, no dosage adjustment is necessary. In patients with moderate or severe hepatic impairment, the maximum daily dose is 8 mg.
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