Expiration date: 06/2025
Group affiliation:
Anti-emetic - serotonin antagonist
Description of the active substance (INN):
Ondansetron
Description trade names:
Ondansetron-Teva
Dosage form:
lozenges, solution for intravenous injection, syrup, coated tablets, rectal suppositories, solution for intravenous and intramuscular injection, solution for injections, tablets film-coated
Pharmacological action:
Antiemetic. Drugs for cytotoxic chemotherapy and radiation therapy can cause an increase in serotonin, which by activation of afferent fibers of the vagus nerve containing the serotonin 5-HT3-receptors, causing a gag reflex. Selectively blocks the serotonin 5-HT3-receptor neurons of the Central (vomiting center) and peripheral (gastrointestinal) nervous system, reguliruemoe gag reflex. Not violate the coordination of movements, does not cause sedation and reduce efficiency. Does not change the concentration of prolactin in plasma.
Indications:
Nausea and vomiting due to cytotoxic chemotherapy or radiotherapy, postoperative nausea and vomiting - prevention and treatment. Symptomatic treatment of alcohol withdrawal syndrome mild and moderate severity (only Latran).
Contraindications:
Hypersensitivity, pregnancy, lactation.
Side effects:
Allergic reactions: urticaria, bronchospasm, laryngospasm, angioedema, anaphylaxis. Local reactions: redness, pain, a burning sensation at the injection site. From the digestive system: hiccups, dry mucous membranes of the mouth, constipation or diarrhea, asymptomatic transient elevation of transaminases in blood serum. From the CCC: chest pain, in some cases, depressed S-T, arrhythmia, bradycardia, decrease in blood pressure. From the nervous system: headache, dizziness, spontaneous movement disorders and seizures. Other: the "tide" of blood to the skin, hot flashes, temporary violation of visual acuity, hypokalemia, gipercreatininemia.
Method of application and dose:
The choice of dosage regimen is determined by the severity emetogenic actions carried out by anti-cancer therapies. For adults, the daily dose is 8-32 mg/day, we recommend the following modes. At a moderate intensity emetogenic action of chemotherapy or radiotherapy - 8 mg/bolus or slow/m, just before the beginning of therapy. When a significant expression emetogenic action of chemotherapy: administered in/jet slowly to 8 mg immediately before chemotherapy and then/jet - 8 mg every 2-4 h or in/to drip continuously at a rate of 1 mg/h for 24 hours, or drip directly before the start of chemotherapy at a dose of 16-32 mg diluted in 50-100 ml of appropriate infusion solution for 15 min. odansetron Efficiency can be increased by single I/V administration of corticosteroids (e.g. 20 mg of dexamethasone) before beginning of chemotherapy. To prevent delayed vomiting that occurs after 24 hours from the start of chemotherapy or radiotherapy - at both high and moderate severity emetogenic action of the therapy recommended taking the drug in pill form. For oral administration: adults, to prevent nausea and vomiting on the background of chemo or radiotherapy, ondansetron administered at 8 mg 1-2 h before the start of antitumor therapy followed the methods of another 8 mg orally after 12 h. To prevent late (24 h) or prolonged vomiting, should continue to receive 8 mg 2 times a day for 5 days after the end of the course of anticancer therapy. To enhance the effect the dose can be increased to 24 mg and appointed simultaneously with 12 mg of dexamethasone phosphate (in the form of sodium salt) for 1-2 hours before start of chemotherapy. Children over 2 years:/in a dose of 5 mg/sq m body surface immediately before chemotherapy, followed by ingestion at a dose of 4 mg over 12 h After completion of chemotherapy should continue to receive ondansetron in a dose of 4 mg 2 times a day for 5 days. Prevention of postoperative nausea and vomiting: Adults: administered during the period of induction of General anesthesia, in/m or/in (slowly) in the dose of 4 mg. To treat the arising of nausea and vomiting in the recommended/m or/in the slow introduction of 4 mg of the drug. I/m in the same part of the body of ondansetron may be administered at a dose not exceeding 4 mg. Children to prevent postoperative nausea and vomiting, ondansetron is used exclusively parenterally in a single dose of 0.1 mg/kg (maximum 4 mg) slow I/before or after anesthesia. Developed for the treatment of postoperative nausea and vomiting in children is recommended medlenee in/with the introduction of a single dose of 0.1 mg/kg (maximum 4 mg). With regard to the prevention and treatment of posleoperazionny nausea and vomiting in children under 2 years not enough experience. When kidney disease and in elderly patients correction normal daily dose and frequency of drug administration is not required. When liver disease substantially reduces the clearance of ondansetron, increases T1/2 from plasma and require dose reduction to 8 mg/day.
Special instructions:
Patients who previously had allergic reactions to other selective blockers of 5-HT3 receptors, have an increased risk of their development against the background of the ondansetron. Ondansetron may slow down the motility of the colon, in connection with his appointment of patients with symptoms of intestinal obstruction requires special monitoring. The infusion solution is prepared immediately before use. If necessary it can be stored for 24 hours at 2-8 deg.With under normal light. During the infusion of protection from light is not required, diluted injectable solution retains its stability for at least for 24 h under natural light or normal lighting. For preparing an infusion solution can be used: 0.9% NaCl solution, 5% dextrose, 10% solution, mannitol, ringer solution, 0.3% KCl solution and 0.9% NaCl solution, a solution of 0.3% KCl and 5% dextrose. Lingual tablets contain aspartame, this should be considered when assigning patients with phenylketonuria.
Interaction:
Caution is required if joint application: with inducers of isoenzymes CYP2D6 and CYP3A - barbiturates, carbamazepine, carisoprodol, glutethimide, griseofulvin, dinitrogen oxide, papaverine, phenylbutazone, phenytoin (probably, etc. hydantoins), rifampin, tolbutamide, inhibitors of the isoenzyme CYP2D6 and CYP3A - allopurinol, macrolide antibiotics, antidepressants (MAO inhibitors), chloramphenicol, cimetidine, estrogensoderjaschie oral contraceptives, diltiazem, disulfiram, valproic acid and its salts, erythromycin, fluconazole, fluoroquinolones, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil. Ondansetron in the concentration of 16-160 ug/ml pharmaceutically compatible and can be administered via a Y-shaped injector/drip in conjunction with the following drugs: cisplatin (in concentrations up to 0.48 mg/ml) for 1-8 h, fluorouracil (at a concentration of up to 0.8 mg/ml at a rate of 20 ml/h higher concentrations can cause precipitation of ondansetron), carboplatin (at a concentration of 0.18-9.9 mg/ml for 10-60 min), etoposide (at a concentration of 0.14-0.25 mg/ml for 30-60 min), ceftazidime (dose 0.25-2 g, in/in the bolus injection for 5 min), cyclophosphamide (at a dose of 0.1-1 g, in/in the bolus injection for 5 min), doxorubicin (at a dose of 10-100 mg, in/in the bolus injection for 5 min), dexamethasone: possible in/with the introduction of 20 mg dexamethasone sodium phosphate slowly over 2-5 min. BOS can be entered using one dropper in the solution concentration of dexamethasone sodium phosphate can range from 32 to 2500 µg/ml, ondansetron - from 8 to 100 µg/ml.
