Osetron solution for intravenous and intramuscularly 2 mg ml 4 ml N10
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Active ingredients
Ondansetron
Release form
Solution
Composition
1 ml of ondansetron hydrochloride dihydrate 2.494 mg, which corresponds to the content of ondansetron 2 mg. Excipients: citric acid monohydrate - 0.
Pharmacological effect
Antiemetic drug of central action. Ondansetron is a selective antagonist of serotonin 5HT3 receptors. Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in the level of serotonin, which, by activating vagal afferent fibers containing 5HT3 receptors, causes a gag reflex. Selectively blocks serotonin 5HT3 receptors of neurons of the central and peripheral nervous system, the end of the vagus nerve in the intestine and in the centers of the central nervous system (mainly the bottom of the IV ventricle), which regulate the implementation of gag reflexes. Does not violate the coordination of movements, does not cause a sedative effect and a decrease in performance. It has anxiolytic activity. Does not change the concentration of prolactin in plasma.
Pharmacokinetics
After ingestion, the time to reach Cmax is 1.5 hours. After the intramuscular injection, the time to reach Cmax is 10 minutes. Binding to plasma proteins is 70-76%. Metabolized in the liver with the participation of microsomal enzymes (CYP2D6). The absence of CYP 2D6 enzyme (debrisoquine polymorphism) does not affect the pharmacokinetics of ondansetron. Both after oral administration and after parenteral administration, T1 / 2 is 3 hours. Less than 5% of the administered dose is excreted unchanged in the urine. The pharmacokinetic parameters of ondansetron do not change with its repeated administration. In patients with moderate renal insufficiency (CC 15–60 ml / min), both systemic clearance and Vd are reduced, resulting in a small and clinically insignificant increase in T1 / 2. The pharmacokinetics of ondansetron practically does not change in patients with severe impaired renal function on chronic hemodialysis (the studies were conducted in the intervals between hemodialysis sessions). In patients with severely impaired liver function, the systemic clearance of ondansetron sharply decreases, resulting in an increase in T1 / 2 to 15-20 hours. The T1 / 2 of ondansetron does not depend on the method of administration. In elderly patients after oral administration or parenteral administration, T1 / 2 may increase up to 5 hours.
Indications
- prevention and elimination of nausea and vomiting caused by cytotoxic chemotherapy or radiotherapy - prevention and elimination of nausea and vomiting in the postoperative period.
Contraindications
- pregnancy - lactation period (breastfeeding) - children under 2 years old - hypersensitivity to ondansetron or other components of the drug.
Use during pregnancy and lactation
The safety of using ondansetron during pregnancy has not been established. The use of the drug Osetron during pregnancy and lactation is contraindicated.
Dosage and administration
Nausea and vomiting caused by cytotoxic therapy The choice of dosing regimen is determined by the emethogenicity of antitumor therapy. For adults, the daily dose of Osetron averages 8-32 mg. For moderately emethogenic chemotherapy or radiotherapy, 8 mg of ondansetron is administered orally for 1-2 hours before the initiation of primary therapy, followed by another 8 mg every 12 hours, or 8 mg IV slowly or intramuscularly immediately before the start of therapy. With highly chemotherapy, 24 mg of Osetron is administered orally at the same time as 12 mg of dexamethasone 1-2 hours before the start of chemotherapy. For the prevention of late or prolonged vomiting that occurs after 24 hours, you should continue taking ondansetron at a dose of 8 mg 2 times / day for 5 days. For parenteral administration, the following regimens are recommended: - 8 mg IV bolus slowly immediately before the start of chemotherapy, and then another 2 IV flux doses of 8 mg, each of which takes 2-4 hours; - continuous 24-hour infusion of the drug in a dose of 24 mg at a rate of 1 mg / h; - 16-32 mg, diluted in 50-100 ml of the appropriate infusion solution, in the form of a 15-minute infusion, immediately before the start of chemotherapy. The effectiveness of ondansetron can be increased by a single intravenous injection of GCS (for example, 20 mg of dexamethasone) before the start of chemotherapy. For children over 2 years old, the drug is prescribed in a dose of 5 mg / m2 of body surface iv, immediately before the start of chemotherapy, followed by ingestion of 4 mg after 12 hours; treatment is recommended to continue at a dose of 4 mg 2 times / day orally for 5 days. Postoperative nausea and vomiting To prevent postoperative nausea and vomiting, adults inject the drug in a single dose of 4 mg IM or IV in a jet (slow) at the onset of anesthesia or give 16 mg orally for 1 hour before general anesthesia begins. For the relief of nausea and vomiting, it is recommended intramuscularly or slow intravenous administration of 4 mg of the drug.V / m in the same area of the body ondansetron can be administered in a dose not exceeding 4 mg! To prevent postoperative nausea and vomiting in children, ondansetron is used exclusively parenterally in a single dose of 0.1 mg / kg (up to a maximum of 4 mg) as a slow intravenous injection before or after anesthesia. For the treatment of developed postoperative nausea and vomiting in children, slow intravenous administration of the drug in a single dose of 0.1 mg / kg (up to a maximum of 4 mg) is recommended. With regard to the prevention and treatment of postoperative nausea and vomiting in children under 2 years of age, there is not enough experience. Elderly patients dosage changes are not required. Patients with impaired renal function to change the usual daily dose and the frequency of administration of the drug is not required. With moderate or severe liver dysfunction, the clearance of ondansetron is significantly reduced, while its T1 / 2 increases, so these patients are not recommended to prescribe ondansetron at a dose of more than 8 mg / day. The following solutions can be used for dilution of the injection solution: 0.9% sodium chloride solution, 5% dextrose solution, Ringer's solution, 0.3% solution of potassium chloride and 0.9% solution of sodium chloride, 0.3% solution of potassium chloride and 5% dextrose solution.
Side effects
Allergic reactions: urticaria, bronchospasm, laryngism, angioedema, anaphylaxis. On the part of the digestive system: hiccups, dry mouth, constipation or diarrhea; sometimes - asymptomatic transient increase in the activity of aminotransferases in the serum. Since the cardiovascular system: pain in the chest, in some cases with depression of the ST segment, arrhythmias, bradycardia, decreased blood pressure. Nervous system disorders: headache, dizziness, spontaneous movement disorders and convulsions. Local reactions: hyperemia, pain, burning at the injection site. Others: rush of blood to the skin of the face, feeling of heat, temporary visual acuity, hypokalemia, hypercreatinemia.
Overdose
In cases of suspected overdose, symptomatic therapy is indicated. The specific antidote is unknown. In case of an overdose of ondansetron, the use of ipecac is not recommended, since It is unlikely that this drug will be effective in the period of the antiemetic effect of ondansetron.
Interaction with other drugs
Sinceondansetron is metabolized by the liver enzyme system (cytochrome P450), caution is required when used together: - with inducers of cytochrome P450 isoenzymes (CYP2D6 and CYP3A) - barbiturates, carbamazepine, carisoprodol, glutethimide, griseofulvin, dinitrogene, nitricogen, carysoprodol, glutethimide, griseofulvin, dinitrogene oxide, nitrohydrin, carcinoprodol, glutethimide, griseofulvin, dinitrogene oxide, nitrohydrin, carcinoprodol, glutethimide, gritofulvin, cytochrome P450 hydantoins), rifampicin, tolbutamide; - with the P450 isoenzymes, Lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil. Ondansetron at a concentration of 16-160 µg / ml is pharmaceutically compatible and can be administered via a Y-shaped injector in / in a drip together with the following drugs: - cisplastin (at a concentration of up to 0.48 mg / ml) for 1-8 hours; - 5-fluorouracil (at a concentration of up to 0.8 mg / ml at a rate of 20 ml / h - higher concentrations may cause ondansetron precipitation); - carboplatin (at a concentration of 0.18-9.9 mg / ml for 10-60 minutes); - etoposide (at a concentration of 0.14-0.25 mg / ml for 30-60 minutes); - ceftazidime (in a dose of 0.25-2.0 g in the form of iv bolus injection for 5 minutes); - cyclophosphamide (at a dose of 0.1-1.0 g in the form of intravenous bolus injection for 5 minutes); - doxorubicin (at a dose of 10-100 mg in the form of intravenous bolus injection for 5 minutes); - dexamethasone (possibly in / in the introduction of 20 mg of dexamethasone slowly over 2-5 minutes). Drugs can be administered through one dropper, while in a solution the concentration of dexamethasone can be from 32 μg to 2.5 mg / ml, ondansetron from 8 μg to 0.1 mg / ml.
special instructions
Patients who previously had allergic reactions to other selective blockers of 5HT3 receptors have an increased risk of their development during the use of ondansetron. Ondansetron can slow the motility of the large intestine, and therefore its administration to patients with signs of intestinal obstruction requires regular monitoring. Infusion solution should be prepared immediately before use. If necessary, the finished infusion solution can be stored until use for a maximum of 24 hours at a temperature of 2-8 ° C under normal illumination.No protection from light is required during the infusion; The diluted injection solution maintains its stability for at least 24 hours in natural light or normal light.